公开(公告)号：US20220242875A1

公开(公告)日：2022-08-04

申请号：US17716707

申请日：2022-04-08

申请人： Araxes Pharma LLC

发明人： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

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.

公开(公告)号：US20180319775A1

公开(公告)日：2018-11-08

申请号：US15764076

申请日：2016-09-27

申请人： ARAXES PHARMA LLC

发明人： Liansheng LI ,  Jun FENG ,  Yun Oliver LONG ,  Pingda REN ,  Yi LIU

IPC分类号： C07D403/04 ,  C07D403/14 ,  A61P35/04

CPC分类号： C07D403/04 ,  A61K9/0019 ,  A61K9/0053 ,  A61P35/04 ,  C07D205/04 ,  C07D403/12 ,  C07D403/14

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, tautomer, stereoisomer or prodrug thereof, wherein R1, R3a, R3b, R4a, R4b, G1, G2, G3, G4, m1, m2, m3, m4, L1, L2 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.