公开(公告)号：US20240239788A1

公开(公告)日：2024-07-18

申请号：US18555640

申请日：2022-04-15

申请人： Merck Sharp & Dohme LLC

发明人： David L. Sloman ,  Gianni Chessari ,  Patrick Schöpf ,  Steven Howard ,  Yuichi Kawai ,  Kazuaki Shibata ,  Hiroki Asakura ,  Takao Uno ,  Takeshi Sagara ,  Masayuki Nakamura ,  Yu Kobayakawa ,  David Jonathan Bennett ,  Indu Bharathan ,  Thomas H. Graham ,  Yongxin Han ,  Zahid Hussain ,  Xiaoshen Ma ,  Mihir Mandal ,  Ryan D. Otte ,  Anandan Palani ,  Uma Swaminathan ,  Mycah Uehling ,  Yingchun Ye ,  Ryan Chau ,  Alec H. Christian ,  Symon Gathiaka ,  Timothy J. Henderson ,  Elisabeth T. Hennessy ,  Andrew J. Hoover ,  Shuhei Kawamura ,  Igri Kolaj ,  Thomas W. Lyons ,  Matthew J. Mitcheltree ,  Aaron Sather

IPC分类号： C07D451/06 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/08 ,  C07D519/00

CPC分类号： C07D451/06 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/08 ,  C07D519/00

摘要： Compounds or their pharmaceutically acceptable salts can inhibit the G12D 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：US12065438B2

公开(公告)日：2024-08-20

申请号：US17289062

申请日：2019-11-01

申请人： Merck Sharp & Dohme LLC

发明人： Yongxin Han ,  David Jonathan Bennett ,  Indu Bharathan ,  Liangqin Guo ,  Brett A. Hopkins ,  Xianhai Huang ,  Derun Li ,  Min Lu ,  Alexander Pasternak ,  David L. Sloman ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D471/04 ,  C07D209/94 ,  C07D215/14 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D471/04 ,  C07D209/94 ,  C07D215/14 ,  C07D401/04 ,  C07D403/04

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Formula (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20220396577A1

公开(公告)日：2022-12-15

申请号：US17782889

申请日：2020-12-14

申请人： Merck Sharp & Dohme LLC ,  IOMET PHARMA LTD.

发明人： Yongxin Han ,  Yongqi Deng ,  David Jonathan Bennett ,  Philip M. Cowley ,  Alan Wise

IPC分类号： C07D471/10 ,  A61K45/06 ,  A61K31/438

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.