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1. (WO2017058792) INHIBITORS OF KRAS G12C MUTANT PROTEINS

Pub. No.:    WO/2017/058792    International Application No.:    PCT/US2016/053957
Publication Date: Fri Apr 07 01:59:59 CEST 2017 International Filing Date: Wed Sep 28 01:59:59 CEST 2016
IPC: C07D 413/14
C07D 403/04
C07D 403/14
C07D 417/14
A61K 31/40
Applicants: ARAXES PHARMA LLC
Inventors: LI, Liansheng
FENG, Jun
LONG, Yun, Oliver
REN, Pingda
LIU, Yi
Title: INHIBITORS OF KRAS G12C MUTANT PROTEINS
Abstract:
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.