KRAS G12C INHIBITORS

AR112797B1Active Publication Date: 2026-08-26AMGEN INC
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Patent Information

Application Number
ARP20180102553
Authority / Receiving Office
AR · AR
Patent Type
Patents
Current Assignee / Owner
Priority Date
2017-09-08
Filing Date
2018-09-07
Publication Date
2026-08-26
Estimated Expiration
2038-09-07
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Abstract

This document provides KRAS G12C inhibitors, their compositions, and methods for their use. These inhibitors are useful for the treatment of multiple disorders, including pancreatic, colorectal, and lung cancer. A compound with a structure of formula (1) wherein A is independently N or CH; W is independently N or CH; wherein one or both of A and W is N; R 1 and R 2 are independently an alkyl C 1-4 linear or branched; R 3 is phenyl substituted with 1 or 2 R substituents 5 ; R 5 is selected independently of one or more halo, -OH or NH2; R 4 is a halo; or a stereoisomer of this, an atropisomer of this, a pharmaceutically acceptable salt of this, a pharmaceutically acceptable salt of the stereoisomer of this, or a pharmaceutically acceptable salt of the atropisomer of this.
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Claims

1. A compound characterized in that it has a structure of Formula (I) or Formula (II) wherein R1 and R2 are methyl, isopropyl, or cyclopropyl; A is independently N or CH; W is independently N or CH; wherein one or both of A and W are N; R3 is phenyl substituted with one or two R5 substituents; R5 is independently selected from one or more halo, -OH, or -NH2; and R4 is F or Cl; or a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, or a pharmaceutically acceptable salt of the atropisomer thereof. Sixteen claims follow.