Abstract: The present invention relates to a bisulfate of a Janus kinase (JAK) inhibitor and a preparation method therefor. More specifically, the present invention relates to a (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazole-5-group)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-group)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate shown in the formula (I), a preparation method therefor, and an application thereof. The bisulfate shown in the formula (I) can be well suitable as a Janus kinase (JAK) inhibitor in clinical work for treating rheumatism or rheumatoid arthritis.

Abstract: Provided are crystalline Form I of (R,E)-N-(4-(3-chloro-4-(pyridin-2-yl-methoxy)-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl)-3-(1-methylpyrrolidin-2-yl) propenamide dimaleate (called SHR1258 dimaleate for short), preparation methods thereof, and pharmaceutical compositions containing the same. The crystalline Form I of SHR1258 dimaleate has good crystal stability and chemical stability, and can be used in the preparation of medicaments for treating diseases related to EGFR receptor tyrosine kinase or HER-2 receptor tyrosine kinase.

Abstract: The present invention relates to a pyrrole sulfonamide derivative, a preparation method for the same, and medical applications thereof. Specifically, the present invention relates to a novel pyrrole sulfonamide derivative as represented by formula (I), a preparation method for the derivative, a pharmaceutical composition comprising the derivative, and uses of the same as therapeutic agents, and particularly as gastric acid secretion inhibitors and potassium-competitive acid blockers (P-CABs), wherein each substituent of formula (I) is as defined in the description.

Abstract: New imidazoline derivatives represented by formula (I): preparation methods thereof, pharmaceutical compositions comprising such derivatives, and applications of such derivatives in preparing androgen receptor antagonists and medicaments for treating diseases such as prostate cancer are described.

Abstract: Provided are crystalline Form I of (R,E)-N-(4-(3-chloro-4-(pyridin-2-yl -methoxy)-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl)-3-(1-methylpyrr olidin-2-yl) propenamide dimaleate (called SHR1258 dimaleate for short), preparation methods thereof, and pharmaceutical compositions containing the same. The crystalline Form I of SHR1258 dimaleate has good crystal stability and chemical stability, and can be used in the preparation of medicaments for treating diseases related to EGFR receptor tyrosine kinase or HER-2 receptor tyrosine kinase.

Abstract: A dronedarone solid dispersion and preparation method thereof are disclosed. The solid dispersion is composed of active ingredient dronedarone or its pharmaceutically acceptable salt and a carrier material, wherein the carrier material is povidone, copovidone, hydroxypropyl cellulose, or a mixture thereof.

Abstract: The present invention provides a human insulin analogue, an acylated derivative thereof and a physiologically acceptable salt. The present invention further provides a preparation method for the insulin analogue and an application of the insulin analogue as a therapeutic agent, and particularly as a diabetes mellitus therapeutic agent.

Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.

Abstract: Disclosed is a process for preparing single enantiomers of beta-amino phenylbutyric acid derivatives and pharmaceutically acceptable salts thereof, which affords the desired compounds having special optical configuration. The process comprises a step of chemical synthesis and a step of resolving the optical isomers of beta-amino phenylbutyric acid derivatives with a resolving agent. The resolving step comprises reacting the optical isomers with resolving agents, such as di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%.

Abstract: Methods for the preparation of Ivabradine sulfate and form I crystal thereof. In particular, the Ivabradine sulfate and the preparation methods thereof, and the stable form I crystal of Ivabradine sulfate and the preparation methods thereof.

Abstract: Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed. Of the many acceptable salts, one example is the following.

Abstract: The present invention provides a pharmaceutical composition for the treatment of 2 type diabetes, wherein the pharmaceutical composition contains (R)-7-[3-amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid methyl ester or its pharmaceutically acceptable salts and metformin or its pharmaceutically acceptable salts (such as hydrochlorate), preparation method thereof and method of treating 2 type diabetes with the composition.

Abstract: A dronedarone solid dispersion and preparation method thereof are disclosed. The solid dispersion is composed of active ingredient dronedarone or its pharmaceutically acceptable salt and a carrier material, wherein the carrier material is povidone, copovidone, hydroxypropyl cellulose, or a mixture thereof.

Abstract: The present invention relates to the salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridine carboxamide, especially hydrochloride and mesylate thereof, and the use of said salts in the preparation of an antineoplastic medicament.

Abstract: Taxol derivatives or their salts having the formula as following: Wherein, R1, R2, Z1, Z2, Z3 and Z4 are defined as the description. Their preparation methods and their use as antitumor agent are also disclosed.

Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.

Abstract: The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).

Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.

Abstract: A method of resolving an important chemical intermediate, 4,5-dimethoxy-1-(methylaminomethyl)-benzocyclobutane, comprises the following steps: reacting its two enantiomers of 4,5-dimethoxy-1-(methylaminomethyl)-benzocyclobutane with di-p-toluoyl-L-tartaric acid (LDTTA) or di-p-toluoyl-D-tartaric acid (DDTTA) in an alcoholic solution or an alcohol in water solution to give the corresponding salts, and then resolving the salts. This method gives high enantiomer excess value, high yield which is more than 80% in total with normal resolution and reverse resolution.

Abstract: The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R1, R2, R3, R4, R5, R6, Q, Z, L, m, n are defined as the description, the methods for preparation thereof, the uses thereof and the pharmaceutical compositions comprising the effective amount of compounds of formula (I). The compounds of formula (I) and their salts can be used as protein kinase inhibitors.