发明申请
- 专利标题: COVALENT INHIBITORS OF KRAS
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申请号: PCT/US2018/034471申请日: 2018-05-24
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公开(公告)号: WO2018218070A2公开(公告)日: 2018-11-29
- 发明人: LI, Liansheng , FENG, Jun , WU, Tao , LIU, Yuan , WANG, Yi , REN, Pingda , LIU, Yi
- 申请人: ARAXES PHARMA LLC
- 申请人地址: 3033 Science Park Road, Suite 220 San Diego, California 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, California 92121 US
- 代理机构: HARWOOD, Eric, A. et al.
- 优先权: US62/511,163 20170525; US62/625,889 20180202
- 主分类号: C07D401/14
- IPC分类号: C07D401/14 ; C07D413/14 ; C07D403/14 ; C07D417/14 ; A61P35/00 ; A61K31/517
摘要:
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R 1 , R 2a , R 2b , R 2c , R 3a , R 3b , R 4a , R 4b , R 5 , L 1 , L 2 , L 3 , E, m 1 , m 2 and * 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
- WO2018218070A3 COVALENT INHIBITORS OF KRAS 公开/授权日:2018-11-29