公开(公告)号：US20180289718A1

公开(公告)日：2018-10-11

申请号：US16005488

申请日：2018-06-11

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Tetsuji SAITO ,  Masato HIGASHINO ,  Soichi KAWAHARADA ,  Arwel LEWIS ,  Mark Stuart CHAMBERS ,  Alastair RAE ,  Kim Louise HIRST ,  Charles David HARTLEY

IPC分类号： A61K31/5383 ,  C07D487/04 ,  A61K31/4439 ,  C07D519/00 ,  C07D498/04 ,  C07D473/32 ,  C07D471/04 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/538 ,  A61K31/517 ,  A61K31/4709 ,  A61K45/06

摘要： The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABAA α5) and act as GABAA α5 negative allosteric modulators (GABAA α5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABAA α5 such as Alzheimer's disease.

公开(公告)号：US20160331757A1

公开(公告)日：2016-11-17

申请号：US15112647

申请日：2015-01-30

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Tetsuji SAITO ,  Masato HIGASHINO ,  Soichi KAWAHARADA ,  Arwel LEWIS ,  Mark Stuart CHAMBERS ,  Alastair RAE ,  Kim Louise HIRST ,  Charles David HARTLEY

IPC分类号： A61K31/5383 ,  A61K31/538 ,  C07D471/04 ,  A61K31/517 ,  C07D487/04 ,  A61K31/4985 ,  C07D473/32 ,  C07D498/04 ,  C07D413/12 ,  C07D413/14 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/423 ,  A61K31/4184 ,  C07D403/12 ,  C07D401/12 ,  A61K31/4709 ,  A61K31/437 ,  C07D519/00 ,  A61K45/06

CPC分类号： A61K31/5383 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/517 ,  A61K31/538 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D473/32 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

摘要： The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABAA α5) and act as GABAA α5 negative allosteric modulators (GABAA α5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABAA α5 such as Alzheimer's disease.

摘要翻译： 本发明提供由式（I）表示的化合物，其药学上可接受的盐，其N-氧化物，其溶剂合物或其前药（其中字符如说明书中所定义）。 由式（I）表示的化合物对γ-氨基丁酸A受体亚基α5（GABAAα5）具有亲和性和选择性，并且作为GABAAα5负变构调节剂（GABAAα5NAM），因此它们可用于预防和 /或治疗与GABAAα5相关的疾病如阿尔茨海默病。