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.

公开(公告)号：US20170247376A1

公开(公告)日：2017-08-31

申请号：US15508387

申请日：2015-09-25

申请人： ARAXES PHARMA LLC

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

IPC分类号： C07D471/04 ,  C07D239/94 ,  A61K31/517 ,  C07D403/04 ,  C12N9/14 ,  C07D403/12 ,  C07D401/14 ,  C07D405/12 ,  A61K9/00 ,  A61K45/06 ,  C07D401/04

CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/517 ,  A61K45/06 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C12N9/14 ,  C12Y306/05

摘要： Inhibitors of Ras protein, methods to modulate the activity of Ras protein, and methods of treatment of disorders mediated by Ras protein are provided. A method for regulating activity of a K-Ras, H-Ras or N-Ras mutant protein with a compound is described. Disorders that can be treated include cancer, such as hematological cancer, pancreatic cancer, MYH associated polyposis, colorectal cancer, or lung cancer.