公开(公告)号：US20210122764A1

公开(公告)日：2021-04-29

申请号：US17081477

申请日：2020-10-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： Indu Bharathan ,  Symon Gathiaka ,  Yongxin Han ,  Xiaoshen Ma ,  Ryan D. Otte ,  David L. Sloman ,  Thomas H. Graham ,  Timothy Henderson ,  Elizabeth Hennessy ,  Anandan Palani

IPC: C07D498/22 ,  A61P35/00 ,  A61K31/519 ,  C07D471/22 ,  C07D519/00

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.

公开(公告)号：US20220402916A1

公开(公告)日：2022-12-22

申请号：US17761433

申请日：2020-09-18

Applicant: Merck Sharp & Dohme Corp.

Inventor： Andrew J. Hoover ,  Thomas H. Graham ,  Xiaoshen Ma ,  Zahid Hussain ,  Mihir Mandal ,  Symon Gathiaka ,  Yongxin Han ,  David L. Sloman

IPC: C07D471/04 ,  A61P35/00

Abstract: Provided are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein Y, CY, R1, R3, R4, R5, R6, R2a, R2b, RMa, RMb, and the subscripts m, n, and q 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 treatment of cancer. Also provided are pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. Also provided are 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.

公开(公告)号：US20220056051A1

公开(公告)日：2022-02-24

申请号：US17312480

申请日：2019-12-13

Applicant: Abdelghani Abe ACHAB ,  Matthew L. CHILDERS ,  Jared N. CUMMING ,  Symon GATHIAKA ,  Charles A. LESBURG ,  Derun LI ,  Min LU ,  Matthew J. MITCHELTREE ,  Anandan PALANI ,  Rachel L. PALTE ,  Hongjun ZHANG ,  Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  Hongjun Zhang

IPC: C07F5/02

Abstract: 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.

公开(公告)号：US20210163505A1

公开(公告)日：2021-06-03

申请号：US16973623

申请日：2019-06-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Jared N. Cumming ,  Christian Fischer ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  David L. Sloman ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: 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.

公开(公告)号：US20210040127A1

公开(公告)日：2021-02-11

申请号：US16977253

申请日：2019-03-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Matthew L. Childers ,  Jared N. Cumming ,  Christian A. Fischer ,  Symon Gathiaka ,  Hakan Gunaydin ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Anandan Palani ,  Rachel L. Palte ,  Qinglin Pu ,  David L. Sloman ,  Sung-Sau So ,  Chunrui Sun ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: 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.

公开(公告)号：US11274111B2

公开(公告)日：2022-03-15

申请号：US16973623

申请日：2019-06-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Jared N. Cumming ,  Christian Fischer ,  Symon Gathiaka ,  Charles A. Lesburg ,  Derun Li ,  Min Lu ,  Matthew J. Mitcheltree ,  Anandan Palani ,  Rachel L. Palte ,  David L. Sloman ,  Hongjun Zhang

IPC: C07F5/02 ,  C07K16/28

Abstract: 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.