公开(公告)号：US09884048B2

公开(公告)日：2018-02-06

申请号：US15531759

申请日：2015-12-10

申请人： Merck Sharp & Dohme Corp.

发明人： Phieng Siliphaivanh ,  Joey Methot ,  Kathryn Ann Lipford ,  Danielle Molinari ,  David L. Sloman ,  David Witter ,  Hua Zhou ,  Christopher Boyce ,  Xianhai Huang ,  Jongwon Lim ,  David Guerin ,  Ganesh Babu Karunakaran ,  Raman Kumar Bakshi ,  Ziping Liu ,  Jianmin Fu ,  Zhilong Wan ,  Wei Liu

IPC分类号： A61K31/437 ,  A61K31/4545 ,  A61K31/444 ,  C07D471/04 ,  C07D519/00

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  C07D471/04 ,  C07D519/00

摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.

公开(公告)号：US10072025B2

公开(公告)日：2018-09-11

申请号：US15519740

申请日：2015-10-21

申请人： Merck Sharp & Dohme Corp.

发明人： Mark E. Scott ,  David Guerin ,  Danielle Molinari ,  Sam Kattar ,  Peter Fuller ,  Christopher Dinsmore ,  Norman Kong ,  Yunfeng Bai ,  Jianmin Fu ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D519/00 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61K31/541

CPC分类号： C07D519/00 ,  A61K31/00 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P11/06 ,  A61P19/02 ,  A61P35/00 ,  C07D471/04

摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.

公开(公告)号：US20170266167A1

公开(公告)日：2017-09-21

申请号：US15531759

申请日：2015-12-10

申请人： Merck Sharp & Dohme Corp.

发明人： Phieng Siliphaivanh ,  Joey Methot ,  Kathryn Ann Lipford ,  Danielle Molinari ,  David L. Sloman ,  David Witter ,  Hua Zhou ,  Christopher Boyce ,  Xianhai Huang ,  Jongwon Lim ,  David Guerin ,  Ganesh Babu Karunakaran ,  Raman Kumar Bakshi ,  Ziping Liu ,  Jianmin Fu ,  Zhilong Wan ,  Wei Liu

IPC分类号： A61K31/437 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/444

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  C07D471/04 ,  C07D519/00

摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.