Small molecule inhibitors of KRAS G12C mutant

US11697657B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Indu T. Bharathan · Somerville, US
• Symon Gathiaka · Waltham, US
• Yongxin Han · Kirkland, CA
• Xiaoshen Ma · Boston, US
• Ryan D. Otte · Natick, US
• David L. Sloman · Brookline, US
• Thomas H. Graham · Somerville, US
• Timothy J. Henderson · Natick, US
• Elisabeth Hennessy · Weston, US
• Anandan Palani · Bound Brook, US

Key dates

• Filing date: Oct 27, 2020
• Grant date: Jul 11, 2023
• Expiry date: Jun 4, 2041

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/05
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.