发明公开
- 专利标题: INHIBITORS OF KRAS G12C
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申请号: US18178452申请日: 2023-03-03
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公开(公告)号: US20230303586A1公开(公告)日: 2023-09-28
- 发明人: Liansheng LI , Jun FENG , Tao WU , Pingda REN , Yi LIU , Yuan Liu , Yun Oliver Long
- 申请人: Araxes Pharma LLC
- 申请人地址: US CA San Diego
- 专利权人: Araxes Pharma LLC
- 当前专利权人: Araxes Pharma LLC
- 当前专利权人地址: US CA San Diego
- 分案原申请号: US16449967 2019.06.24
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; C07D239/94 ; C07D401/12 ; C07D217/22 ; C07D215/46 ; C07D215/54 ; C07D239/84 ; C07D487/04 ; C07D239/95 ; C07D403/04 ; C07D241/44 ; C07D401/04 ; C07D409/04
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, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z 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.
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z 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.
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