发明公开
- 专利标题: FUSED-TRICYCLIC INHIBITORS OF KRAS AND METHODS OF USE THEREOF
- 专利标题(中): KRAS的稠合三环抑制剂及其使用方法
-
申请号: EP16718179.1申请日: 2016-04-15
-
公开(公告)号: EP3283462A1公开(公告)日: 2018-02-21
- 发明人: LI, Liansheng , FENG, Jun , LONG, Yun, Oliver , LIU, Yuan , WU, Tao , REN, Pingda , LIU, Yi
- 申请人: Araxes Pharma LLC
- 申请人地址: 3033 Science Park Road, Suite 220 San Diego, CA 92121 US
- 专利权人: Araxes Pharma LLC
- 当前专利权人: Araxes Pharma LLC
- 当前专利权人地址: 3033 Science Park Road, Suite 220 San Diego, CA 92121 US
- 代理机构: Hoffmann Eitle
- 优先权: US201562147955P 20150415
- 国际公布: WO2016168540 20161020
- 主分类号: C07D219/10
- IPC分类号: C07D219/10 ; C07D219/12 ; C07D471/04 ; C07D491/056 ; C07D498/04 ; C07D513/04 ; A61K31/4375 ; A61P35/00
摘要:
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):(I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, A, G1, G2, L1, L2, m1, m2, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
公开/授权文献
信息查询