Patent · US Active

Substituted quinazolines as inhibitors of KRAS G12C

US9840516B2 · kind B2 · utility

64Cited by
17References
33Claims
0Family size

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Key dates

Filing dateOct 10, 2014
Grant dateDec 12, 2017
Priority date
Expiry dateOct 10, 2034

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D487/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

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, 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.