公开(公告)号：US20240002359A1

公开(公告)日：2024-01-04

申请号：US18254190

申请日：2021-12-01

申请人： Stephane L. BOGEN ,  Ping CHEN ,  Dane James CLAUSSEN ,  Xianhai HUANG ,  Michael T. RUDD ,  Shawn P. WALSH ,  Lan WEI ,  Dexi YANG ,  Merck Sharp & Dohme LLC

发明人： Stephane L. Bogen ,  Ping Chen ,  Dane James Claussen ,  Xianhai Huang ,  Michael T. Rudd ,  Shawn P. Walsh ,  Lan Wei ,  Dexi Yang

IPC分类号： C07D401/04 ,  C07D417/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07D417/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14

摘要： The present invention is directed to 3-heteroaryl pyrrolidine and piperidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：US20230365533A1

公开(公告)日：2023-11-16

申请号：US18040896

申请日：2021-08-16

申请人： Stephane L. BOGEN ,  Dane James CLAUSEN ,  Deodial Guy GUIADEEN ,  Jinsong HAO ,  Shishi LIN ,  Michael T. RUDD ,  Lan WEI ,  Li XIAO ,  Dexi YANG ,  MERCK SHARP & DOHME CORP.

发明人： Stephane L. Bogen ,  Dane James Clausen ,  Deodial Guy Guiadeen ,  Jinsong Hao ,  Shishi Lin ,  Michael T. Rudd ,  Lan Wei ,  Li Xiao ,  Dexi Yang

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D491/048

CPC分类号： C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D491/048

摘要： The present invention is directed to bicyclo[4.1 0]heptane pyrrolidine compounds of formula (I) which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.




where




is




wherein n is 0 or 1;

公开(公告)号：US20230167085A1

公开(公告)日：2023-06-01

申请号：US17920943

申请日：2021-05-07

申请人： Wei LAN ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian ,  Merck Sharp & Dohme LLC

发明人： Jacqueline D. HICKS ,  John S. Debenham ,  Amjad Ali ,  Ying-Duo Gao ,  Lan Wei ,  Dexi Yang ,  Rongze Kuang ,  Alan Hruza ,  Peter Nizner ,  Daniel A. Tatosian

IPC分类号： C07D401/14 ,  C07D417/14

CPC分类号： C07D401/14 ,  C07D417/14

摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XI activation inhibitors.

公开(公告)号：US20200375987A1

公开(公告)日：2020-12-03

申请号：US16769670

申请日：2018-12-20

申请人： Alexander PASTERNAK ,  Shuzhi DONG ,  Jack D. SCOTT ,  Haiqun TANG ,  Zhiqiang ZHAO ,  Dexi YANG ,  Li XIAO ,  Xin GU ,  Merck Sharp & Dohme Corp.

发明人： Alexander Pasternak ,  Shuzhi Dong ,  Jack D. Scott ,  Haiqun Tang ,  Zhiqiang Zhao ,  Dexi Yang ,  Li Xiao ,  Xin Gu ,  Jinlong Jiang

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4439 ,  A61K31/519 ,  A61K31/4188 ,  C07D513/04 ,  C07D403/10 ,  A61K31/4178 ,  A61K31/407 ,  A61K31/496 ,  A61K31/165 ,  A61K31/7048 ,  A61K31/546 ,  A61P31/04

摘要： The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein RA, R1, and Z are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.