Chinese Academy of Sciences

Shanghai Lead Discovery Pharmaceuticals Limited Company

Xiaomin Luo

Hong Tao Liu

Hualiang Jiang

Kaixian Chen

Jian Li

Jiang Wang

Jingya Li

Jing Lan Chen

Jian Wang

Jia Tao Li

Fei Ye

Jingkang Shen

Tao Sun

Jianping Zuo

Jianhua Shen

Mingbo Su

Xu Shen

Bing Xiong

Lili Chen

Shengbin Zhou

Hong Liu

Donglu Bai

Yiming Yang

Haibin Luo

Chunshan Gui

Yifu Yang

Xianhan Zhuang

Xuchang He

Jia Li

The invention describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.

Polymorph of DPPIV inhibitor maleate and preparation method therefor

The invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid and a preparation method for the salt form. Also disclosed is a pharmaceutical composition of the formula I compound salt form. The salt form of the invention provides powerful in vivo hypoglycemic activity and is expected to be a novel pharmaceutical active ingredient for treating or preventing diabetes mellitus type 2 and/or complications of diabetes mellitus type 2 

Salt form of DPPIV inhibitor and preparation method thereof

The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.

Crystal form A of compound and preparation method thereof

The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL Protease are found. Cinanserin was tested at molecular and viral levels, and it was found to be able to inhibit the SARS-CoV viral 3CL protease and SARS-CoV viruses. Cinanserin analogs were synthesized and tested at molecular and viral levels, they were found to be able to inhibit the SARS-CoV virus 3CL Protease and SARS-CoV viruses, and may be used for treating and/or preventing SARS-CoV virus infection.

3D-structure model of SARS coronavirus 3CL protease and anti-SARS drugs

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Shanghai, China

Xiaomin Luo