公开(公告)号：US20190100529A1

公开(公告)日：2019-04-04

申请号：US16087317

申请日：2017-03-20

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC分类号： C07D495/04 ,  A61P3/10

摘要： 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.

公开(公告)号：US20190031678A1

公开(公告)日：2019-01-31

申请号：US16087318

申请日：2017-03-22

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC分类号： C07D495/04 ,  A61P3/10

摘要： 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

公开(公告)号：US20180030066A1

公开(公告)日：2018-02-01

申请号：US15549918

申请日：2016-02-03

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： Hong LIU ,  Jian WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Shengbin ZHOU ,  Mingbo SU ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC分类号： C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519 ,  C07B2200/13

摘要： 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.