公开(公告)号：EP3185865B1

公开(公告)日：2020-07-15

申请号：EP15836358.0

申请日：2015-08-24

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

发明人： ARASAPPAN, Ashok ,  BUNGARD, Christopher James ,  FRIE, Jessica L. ,  HAN, Yongxin ,  HOYT, Scott B. ,  MANLEY, Peter J. ,  MEISSNER, Robert S. ,  PERKINS, James J. ,  SEBHAT, Iyassu K. ,  WILKENING, Robert R. ,  LEAVITT, Kenneth J.

IPC分类号： A61K31/4375

公开(公告)号：EP3145915A1

公开(公告)日：2017-03-29

申请号：EP15795833.1

申请日：2015-05-19

申请人： Merck Sharp & Dohme Corp.

发明人： BIFU, Tesfaye ,  BIJU, Purakkattle ,  BLIZZARD, Timothy A. ,  CHEN, Zhengxia ,  CLEMENTS, Matthew J. ,  CUI, Mingxiang ,  FRIE, Jessica L. ,  HAGMANN, William K. ,  HU, Bin ,  JOSIEN, Hubert ,  NAIR, Anilkumar G. ,  PLUMMER, Christopher W. ,  ZHU, Cheng

IPC分类号： C07D221/16 ,  C07D401/12 ,  C07D405/12 ,  A61K31/438 ,  A61K31/415 ,  A61P3/10

CPC分类号： C07D221/16 ,  A61K31/192 ,  A61K31/366 ,  A61K31/397 ,  A61K31/435 ,  A61K31/438 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/538 ,  A61K31/55 ,  A61K45/06 ,  C07C61/39 ,  C07C2602/08 ,  C07C2603/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP3185865A1

公开(公告)日：2017-07-05

申请号：EP15836358.0

申请日：2015-08-24

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

发明人： ARASAPPAN, Ashok ,  BUNGARD, Christopher James ,  FRIE, Jessica L. ,  HAN, Yongxin ,  HOYT, Scott B. ,  MANLEY, Peter J. ,  MEISSNER, Robert S. ,  PERKINS, James J. ,  SEBHAT, Iyassu K. ,  WILKENING, Robert R. ,  LEAVITT, Kenneth J.

IPC分类号： A61K31/4375

摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.

摘要翻译： 本发明提供式（I）的喹啉甲酰胺和喹啉腈化合物或其药学上可接受的盐，其中R 1，R 2，L，X 1，X 2和X 3如本文所定义。 本发明的药物组合物包含它们的化合物，以及它们的药学上可接受的盐，以及，是非竞争性的mGluR2拮抗剂，或mGluR2的负变构调节剂（NAMs中）是有用的，并在有需要治疗的人，其用于的方法可能是有用的 疾病或病症，其中mGluR2的-NAM受体发挥致病作用，如阿尔茨海默氏症，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。