公开(公告)号：WO2022251576A1

公开(公告)日：2022-12-01

申请号：PCT/US2022/031256

申请日：2022-05-27

申请人： MERCK SHARP & DOHME CORP.

发明人： SHIBATA, Kazuaki ,  KOBAYAKAWA, Yu ,  IMAOKA, Tadashi ,  SAKAMOTO, Toshihiro ,  MIURA, Risako ,  HENNESSY, Elisabeth ,  DEL POZO, Juan

IPC分类号： C07D498/04 ,  C07D491/052 ,  A61K31/519 ,  A61K31/5377 ,  A61P35/00

摘要： Compounds of Formula (I) 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：WO2022232320A1

公开(公告)日：2022-11-03

申请号：PCT/US2022/026601

申请日：2022-04-27

申请人： MERCK SHARP & DOHME CORP.

发明人： SHIBATA, Kazuaki ,  KONDO, Hitomi ,  YAMAMOTO, Tomohiro ,  SAKAMOTO, Toshihiro ,  ASAKURA, Hiroki ,  AKEMOTO, Kei ,  MIURA, Risako ,  SUGIMOTO, Tetsuya ,  DEL POZO, Juan ,  GIAMBUSU, George Madalin ,  GRAHAM, Thomas H. ,  HAN, Yongxin ,  HENNESSY, Elisabeth T. ,  KAWAMURA, Shuhei ,  RYAN, Michael

IPC分类号： A61K31/41 ,  A61K31/4184 ,  A61K31/4353 ,  C07D235/02 ,  C07D235/04 ,  C07D235/08

摘要： 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 disclosed herein 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：WO2022232318A1

公开(公告)日：2022-11-03

申请号：PCT/US2022/026599

申请日：2022-04-27

申请人： MERCK SHARP & DOHME CORP.

发明人： SHIBATA, Kazuaki ,  ASAKURA, Hiroki ,  AKEMOTO, Kei ,  SAKAMOTO, Toshihiro ,  KONDO, Hitomi ,  YAMAMOTO, Tomohiro ,  MIURA, Risako ,  SCHÖPF, Patrick ,  DEL POZO, Juan ,  GIAMBUSU, George Madalin ,  GRAHAM, Thomas H. ,  HAN, Yongxin ,  HENNESSY, Elisabeth T. ,  PALANI, Anandan ,  RYAN, Michael ,  SLOMAN, David L. ,  HOWARD, Steven

IPC分类号： A61K31/409 ,  A61K31/495 ,  A61P35/00 ,  C07D471/14 ,  C07D471/22

摘要： Compounds of Formula (I) or (la) 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 (la) 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.