- 专利标题: Small Molecule Inhibitors of KRAS G12C Mutant
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申请号: US18311646申请日: 2023-05-03
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公开(公告)号: US20240043448A1公开(公告)日: 2024-02-08
- 发明人: Indu Bharathan , Symon Gathiaka , Yongxin Han , Xiaoshen Ma , Ryan D. Otte , David L. Sloman , Thomas H. Graham , Timothy Henderson , Elisabeth Hennessy , Anandan Palani
- 申请人: Merck Sharp & Dohme LLC
- 申请人地址: US NJ Rahway
- 专利权人: Merck Sharp & Dohme LLC
- 当前专利权人: Merck Sharp & Dohme LLC
- 当前专利权人地址: US NJ Rahway
- 分案原申请号: US17081477 2020.10.27
- 主分类号: C07D498/22
- IPC分类号: C07D498/22 ; A61P35/00 ; A61K31/519 ; C07D471/22 ; C07D519/00
摘要:
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.
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.
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