Inhibitors of KRAS G12C mutant proteins

US10689356B2 · kind B2 · utility

Assignee

• Araxes Pharma LLC · US

Inventors

• Liansheng Li · San Diego, US
• Jun Feng · San Diego, US
• Yun Oliver Long · San Diego, US
• Yuan Liu · Billerica, US
• Pingda Ren · San Diego, US
• Yi Liu · San Diego, US

Key dates

• Filing date: Sep 28, 2016
• Grant date: Jun 23, 2020
• Expiry date: Sep 28, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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 A, R1, R3a, R3b, R4a, R4b, 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.