公开(公告)号：EP2786998B1

公开(公告)日：2018-07-25

申请号：EP12853993.9

申请日：2012-10-23

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Cisen Pharmaceutical Co., Ltd.

发明人： LIU, Hong ,  LI, Jia ,  LI, Jian ,  LI, Jingya ,  WANG, Jiang ,  SU, Mingbo ,  LIAN, Jie ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/55 ,  A61P3/10

CPC分类号： C07D495/04

摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

公开(公告)号：EP2786998A1

公开(公告)日：2014-10-08

申请号：EP12853993.9

申请日：2012-10-23

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

发明人： LIU, Hong ,  LI, Jia ,  LI, Jian ,  LI, Jingya ,  WANG, Jiang ,  SU, Mingbo ,  LIAN, Jie ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/55 ,  A61P3/10

CPC分类号： C07D495/04

摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

摘要翻译： 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 这些化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱发一系列生理作用来治疗II型糖尿病。 因此，这些化合物可以作为治疗糖尿病的新药物开发。