Merck Sharp + Dohme Corp.

Symon Gathiaka

Anandan Palani

David L Sloman

Jared N Cumming

Yongxin Han

Hongjun Zhang

Thomas H Graham

Ryan D Otte

Derun Li

Abdelghani Achab

Timothy J Henderson

Charles A Lesburg

Min Lu

Indu T Bharathan

Elisabeth Hennessy

Xiaoshen Ma

Rachel L Palte

Christian Fischer

Matthew Lloyd Childers

Matthew J Mitcheltree

Sung-Sau So

Qinglin Pu

Hakan Gunaydin

Chunrui Sun

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, R, 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.

Small molecule inhibitors of KRAS G12C mutant

Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

Arginase inhibitors and methods of use

Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, Rand 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.

Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases. 

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Waltham, MA, United States of America

Symon Gathiaka