基本信息:
- 专利标题： COVALENT INHIBITORS OF KRAS
- 申请号：US15989015 申请日：2018-05-24
- 公开(公告)号：US20190062313A1 公开(公告)日：2019-02-28
- 发明人： Liansheng Li , Jun Feng , Tao Wu , Yuan Liu , Yi Wang , Pingda Ren , Yi Liu
- 申请人： Araxes Pharma LLC
- 主分类号： C07D403/14
- IPC分类号： C07D403/14 ; A61P35/00 ; C07D403/04 ; C07D401/14 ; C07D487/08 ; C07D413/14 ; C07D471/04 ; C07D405/14
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 R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5, L1, L2, L3, E, m1, m2 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:
- US10745385B2 Covalent inhibitors of KRAS 公开/授权日：2020-08-18
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D403/00 | 杂环化合物，含有两个或更多的杂环，以氮原子作为仅有的杂环原子，C07D401/00组不包含的 |
| --------C07D403/14 | .含有3个或更多个杂环 |