Abstract: The present invention relates to a multi-target tyrosine kinase inhibitor, which is a compound having protein kinase inhibitory activity as shown in formula (I). The compound is metabolized into an active small molecule td32-4 that inhibits tumor growth in vivo, so as to achieve the anti-tumor effect. Compared with td32-4, the compound of the present invention has significantly improved solubility and oral bioavailability, and shows strong anti-tumor activity in animal in vivo experiments. The present invention relates to a synthetic method for the compound of formula (I) and an application thereof in the field of pharmaceuticals.

Abstract: Provided are a new tubulin inhibitor and applications thereof, the tubulin inhibitor being a series of compounds based on substituted heterocyclic skeletons, targeting the colchicine binding sites of tubulin. The structure is: Formula (I), wherein: formula (A), n independently expresses an integer between 0 and 5, the condition being that n?5, A represents mono- or poly-substituted groups, the groups being selected from the group consisting of H, C1-C20 amide group, C1-C20 acyloxy group, C1-C20 alkanoyl group, C1-C20 alkoxycarbonyl group, C1-C20 alkoxy group, C1-C20 alkylamino group, C1-C20 alkylcarboxyamino group, aroyl group, aralkanoyl group, carboxyl group, cyano group, halogen group, hydroxyl group, nitro group and methylthienyl group.

Abstract: Provided are a new tubulin inhibitor and applications thereof, the tubulin inhibitor being a series of compounds based on substituted heterocyclic skeletons, targeting the colchicine binding sites of tubulin. The structure is: Formula (I), wherein: formula (A), n independently expresses an integer between 0 and 5, the condition being that n?5, A represents mono- or poly-substituted groups, the groups being selected from the group consisting of H, C1-C20 amide group, C1-C20 acyloxy group, C1-C20 alkanoyl group, C1-C20 alkoxycarbonyl group, C1-C20 alkoxy group, C1-C20 alkylamino group, C1-C20 alkylcarboxyamino group, aroyl group, aralkanoyl group, carboxyl group, cyano group, halogen group, hydroxyl group, nitro group and methylthienyl group.

Abstract: Provided is a composition of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(ethoxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide p-toluene sulfonate 1.5 hydrate ?-polymorph. The ?-polymorph has a stable form, a defined melting point, a good chemical stability, and a good endurance to high temperature and light irradiation, and is suitable for pharmaceutical use.

Abstract: Provided is a composition of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(ethoxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide p-toluene sulfonate 1.5 hydrate ?-polymorph. The ?-polymorph has a stable form, a defined melting point, a good chemical stability, and a good endurance to high temperature and light irradiation, and is suitable for pharmaceutical use.

Abstract: Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3?), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3? is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.

Abstract: The present invention relates to a novel crystalline form of a Compound 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside. Crystalline form I of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.

Abstract: Disclosed is a depolymerized glycosaminoglycan from Thelenota ananas (dTHG), weight average molecular weight of which is about 8000˜20000 Da, and monosaccharide components of which are acetylgalactosamine (GalNAc), glucuronic acid (GlcUA), fucose (Fuc) or their sulfates (expressed as —OSO3?), in which molar ratio of GalNAc:GlcUA:Fuc:—OSO3? is about 1:(1±0.3):(1±0.3):(3.5±0.5). Said dTHG is a potent endogenous inhibitor of factor X, which has good anticoagulant and antithrombotic activity, and can be used for the prevention and/or treatment of thrombotic diseases. Also provided is a method for preparing said dTHG, which comprises steps of 1) extracting and obtaining fucosylated glycosaminoglycan (THG) from the body wall of Thelenota ananas; 2) depolymerizing THG to obtain dTHG by method of peroxide depolymerization or method of peroxide depolymerization catalyzed by catalyst of the fourth period transition metal ions; 3) removing impurities with lower and/or higher molecular weight in dTHG.

Abstract: The present invention relates to a novel crystalline form of a Compound 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside. Crystalline form I of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.

Abstract: A composition includes polydatin and solvent for dissolving the polydatin, wherein the solvent comprises alcohol in a range between 40 and 95% by volume, propanediol in a range between 0 and 60% by volume, and water in remaining volume. The concentration of the polydatin must be at least 6 mg/ml. The composition has good stability in cold preservation. The composition is in a pharmaceutically acceptable administrative form selected from the group consisting of an intravenous injection, and intramuscular injection, an oral administration, a spray solution, and an aerosol form.

Abstract: The present invention provides new use of 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside. 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside has efficacies of anti-myocardial ischemia by intravenous injection and/or oral administration. It is advantageous that 3,4?,5-trihydroxy-stilbene-3-?-D-glucoside as anti-myocardial ischemia drug is used to prepare the medicine for treating and/or preventing ischemic heart disease.

Abstract: The invention discloses pharmaceutical compositions containing polydatin or its pharmaceutically acceptable salts with the effect of improving microcirculation, and their application in preparing drugs which can improve microcirculation. The compositions are an non-gastrointestinal injection preparation, the preparation can be an aqueous solution which have pH 7.0-10.0 comprising 5-50% propandiol. The dosage forms of the compositions may be lyophilizing powder injection, oral form, suppository of procto-administration and other forms of administrations comprising unguent, ointment, paste film coating and the like. The compositions may be used to treat and/or prevent diseases related to microcirculation blockage. The unit form may contain 1-1000 mg polydatin or its derivatives. The invention solves the problem of using polydatin to improve microcirculation.