公开(公告)号：US20200095212A1

公开(公告)日：2020-03-26

申请号：US16483957

申请日：2018-02-19

申请人： Merck Sharp & Dohme Corp.

发明人： Kun Liu ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Qinglin Pu ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07D271/08 ,  C07D413/12

摘要： Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. 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：US08993756B2

公开(公告)日：2015-03-31

申请号：US14363097

申请日：2012-11-30

申请人： Merck Sharp & Dohme Corp.

发明人： Sean P. Ahearn ,  Matthew Christopher ,  Christopher Dinsmore ,  Joon Jung ,  Qinglin Pu ,  Alexey Rivkin ,  Mark E. Scott ,  David J. Witter ,  Hyun Chong Woo ,  Brandon Cash

IPC分类号： C07D487/04 ,  C07D417/04 ,  C07D413/04 ,  A61K31/519 ,  A61P19/02 ,  C07D519/00 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

摘要翻译： 本发明提供了作为JAK3抑制剂的式I化合物。 具体地，式I化合物是吡咯并[2,3-d]嘧啶衍生物化合物。 本发明还提供了通过给予式I的吡咯并[2,3-d]嘧啶衍生物化合物来治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的方法。

公开(公告)号：US20140349998A1

公开(公告)日：2014-11-27

申请号：US14363097

申请日：2012-11-30

申请人： Merck Sharp & Dohme Corp.

发明人： Sean P Ahearn ,  Matthew Christopher ,  Christopher Dinsmore ,  Joon Jung ,  Qinglin Pu ,  Alexey Rivkin ,  Mark E. Scott ,  David J. Witter ,  Hyun Chong Woo ,  Brandon Cash

IPC分类号： C07D487/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

摘要翻译： 本发明提供了作为JAK3抑制剂的式I化合物。 具体地，式I化合物是吡咯并[2,3-d]嘧啶衍生物化合物。 本发明还提供了通过给予式I的吡咯并[2,3-d]嘧啶衍生物化合物来治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症的方法。

公开(公告)号：US11478461B2

公开(公告)日：2022-10-25

申请号：US17047247

申请日：2019-04-15

申请人： Merck Sharp & Dohme Corp.

发明人： Liangqin Guo ,  Hongjun Zhang ,  Ping Chen ,  Dane Clausen ,  Xavier Fradera ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Li Xiao ,  Feng Ye

IPC分类号： A61K31/44 ,  A61K45/06 ,  C07C237/22 ,  C07C255/60 ,  C07D213/75 ,  C07C271/36 ,  C07C233/78 ,  C07C271/24 ,  C07C233/79 ,  C07D213/81 ,  C07D271/06 ,  C07D239/28 ,  C07D215/48 ,  C07C275/30 ,  C07C275/28 ,  C07D239/42 ,  C07D305/06 ,  C07D261/08 ,  C07D471/04 ,  C07D261/20 ,  C07D209/34 ,  C07D277/56 ,  C07D217/02 ,  C07D231/14 ,  C07D237/28 ,  C07D241/24 ,  C07D217/26 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4245 ,  A61K31/47 ,  A61K31/17 ,  A61K31/505 ,  A61K31/337 ,  A61K31/437 ,  A61K31/42 ,  A61K31/426 ,  A61K31/472 ,  A61K31/415 ,  A61K31/4965

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (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：US20210040127A1

公开(公告)日：2021-02-11

申请号：US16977253

申请日：2019-03-08

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07F5/02 ,  C07K16/28

摘要： 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：US09957265B2

公开(公告)日：2018-05-01

申请号：US14778052

申请日：2014-03-19

申请人： Merck Sharp & Dohme Corp.

发明人： Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Christopher F. Thompson ,  Qinglin Pu ,  Mark E. Scott ,  Jason David Katz ,  Ravi Kurukulasuriya ,  Joshua T. Close ,  Danielle Falcone ,  Jason Brubaker ,  Hongbo Zeng ,  Yunfeng Bai ,  Jianmin Fu ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.

公开(公告)号：US11352320B2

公开(公告)日：2022-06-07

申请号：US17057921

申请日：2019-05-28

申请人： Merck Sharp & Dohme Corp.

发明人： Shuwen He ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Dong Xiao ,  Li Xiao ,  Feng Ye ,  Hongjun Zhang

IPC分类号： C07C13/06 ,  C07C233/65 ,  C07C233/80 ,  A61K31/166 ,  C07C271/14 ,  A61P35/00 ,  C07D213/74 ,  C07D237/34 ,  C07D239/42 ,  C07D239/94 ,  C07D241/20 ,  C07D471/04 ,  A61K45/06

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (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：US20210393600A1

公开(公告)日：2021-12-23

申请号：US17047247

申请日：2019-04-15

申请人： Merck Sharp & Dohme Corp.

发明人： Liangqin Guo ,  Hongjun Zhang ,  Ping Chen ,  Dane Clausen ,  Xavier Fradera ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Li Xiao ,  Feng Ye

IPC分类号： A61K31/44 ,  A61K45/06 ,  C07C237/22 ,  C07C255/60 ,  C07D213/75 ,  C07C271/36 ,  C07C233/78 ,  C07C271/24 ,  C07C233/79 ,  C07D213/81 ,  C07D271/06 ,  C07D239/28 ,  C07D215/48 ,  C07C275/30 ,  C07C275/28 ,  C07D239/42 ,  C07D305/06 ,  C07D261/08 ,  C07D471/04 ,  C07D261/20 ,  C07D209/34 ,  C07D277/56 ,  C07D217/02 ,  C07D231/14 ,  C07D237/28 ,  C07D241/24 ,  C07D217/26 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4245 ,  A61K31/47 ,  A61K31/17 ,  A61K31/505 ,  A61K31/337 ,  A61K31/437 ,  A61K31/42 ,  A61K31/426 ,  A61K31/472 ,  A61K31/415 ,  A61K31/4965

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (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：US20210198190A1

公开(公告)日：2021-07-01

申请号：US17057921

申请日：2019-05-28

申请人： Merck Sharp & Dohme Corp.

发明人： Shuwen He ,  Dane Clausen ,  Liangqin Guo ,  Yongxin Han ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Dong Xiao ,  Li Xiao ,  Feng Ye ,  Hongjun Zhang

IPC分类号： C07C271/14 ,  C07D239/42 ,  C07D237/34 ,  C07D241/20 ,  C07D239/94 ,  C07D213/74 ,  C07D471/04 ,  A61P35/00

摘要： Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (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：US20200231606A1

公开(公告)日：2020-07-23

申请号：US16326408

申请日：2017-08-24

申请人： Merck Sharp & Dohme Corp.

发明人： Kun Liu ,  Abdelghani Achab ,  Purakkattle Biju ,  Timothy A. Cernak ,  Yongqi Deng ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Guoqing Li ,  Qinglin Pu ,  Zhi-Cai Shi ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07F5/02 ,  C07D271/08 ,  C07D413/12

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