公开(公告)号：US10160726B2

公开(公告)日：2018-12-25

申请号：US15500870

申请日：2015-08-03

Applicant: NOVARTIS AG

Inventor： Javier de Vicente Fidalgo ,  Haiying He ,  Cheng Hu ,  Zhigan Jiang ,  Xiaolin Li ,  Peichao Lu ,  Wosenu Mergo ,  Daniel Mutnick ,  Folkert Reck ,  Alexey Rivkin ,  Colin Keith Skepper ,  Xiaojing Michael Wang ,  Jianhua Xia ,  Yongjin Xu

IPC: C07D215/38 ,  C07D215/22 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10

Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.

公开(公告)号：US09566312B2

公开(公告)日：2017-02-14

申请号：US14717872

申请日：2015-05-20

Applicant: Novartis AG

Inventor： Jiping Fu ,  Subramanian Karur ,  Xiaolin Li ,  Peichao Lu ,  Wosenu Mergo ,  Alexey Rivkin ,  Zachary Kevin Sweeney ,  Meiliana Tjandra ,  Andrew Weiss ,  Aregahegn Yifru

IPC: A61K38/12 ,  A61K38/13 ,  C07K7/64 ,  A61K45/06

CPC classification number: A61K38/13 ,  A61K38/12 ,  A61K45/06 ,  C07K7/64 ,  C07K7/645 ,  A61K2300/00

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, and A-B are as defined herein, which are non-immunosuppressive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.

Abstract translation: 本发明提供式I化合物; 或其药学上可接受的盐，其中本文定义的变量R1，R2，R3，R4，R5和AB是非免疫抑制性亲环蛋白结合的mPTP阻断剂，因此可用于预防或治疗疾病或 疾病如HCV感染，中风，多发性硬化，HBV感染，HPV感染，哮喘，癌症，肌营养不良，败血症，缺血/再灌注损伤和心力衰竭。