公开(公告)号：US10357481B2

公开(公告)日：2019-07-23

申请号：US15579878

申请日：2016-06-27

Applicant: MERCK SHARP & DOHME CORP. ,  Gregori J. Morriello ,  Lehua Chang ,  Ashley Forster ,  Yili Chen ,  Michael P. Dwyer ,  Zack Zhiqiang Guo ,  Ming Wang ,  Shimin Xu ,  Yingjian Bo ,  Jianmin Fu

Inventor： Gregori J. Morriello ,  Lehua Chang ,  Ashley Forster ,  Yili Chen ,  Michael P. Dwyer ,  Zack Zhiqiang Guo ,  Ming Wang ,  Shimin Xu ,  Yingjian Bo ,  Jianmin Fu

IPC: A61K31/4196 ,  C07D471/04 ,  C07D487/04 ,  A61P25/28 ,  A61P25/22 ,  A61P25/18 ,  A61P25/16 ,  A61P25/06 ,  A61K31/52

Abstract: The present invention is directed to substituted triazolo bicyclic compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：US09499534B2

公开(公告)日：2016-11-22

申请号：US14786466

申请日：2014-04-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kenneth L. Arrington ,  Byron DuBois ,  John S. Debenham ,  Ping Liu ,  Alan B. Northrup ,  Jason W. Szewczyk ,  Liping Wang ,  Ming Wang

IPC: C07D417/14 ,  A61K31/427 ,  C07D417/12 ,  A61K31/506 ,  A61K31/5377

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

公开(公告)号：US10472344B2

公开(公告)日：2019-11-12

申请号：US15780134

申请日：2016-11-29

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Anthony K. Ogawa ,  Linda Brockunier ,  James Tata ,  Dann L. Parker, Jr. ,  Ming Wang

IPC: C07D401/10 ,  C07D401/14 ,  C07D409/14 ,  A61P7/02

Abstract: 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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：US20180009796A1

公开(公告)日：2018-01-11

申请号：US15104537

申请日：2015-01-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Richard Berger ,  Timothy A. Blizzard ,  Brian T. Campbell ,  Helen Y. Chen ,  John S. Debenham ,  Sunita V. Dewnani ,  Byron Dubois ,  Candido Gude ,  Zack Zhiqiang Guo ,  Bart Harper ,  Zhiyong Hu ,  Songnian Lin ,  Ping Liu ,  Ming Wang ,  Feroze Ujjainwalla ,  Jiayi Xu ,  Libo Xu ,  Rui Zhang

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

公开(公告)号：US20160207922A1

公开(公告)日：2016-07-21

申请号：US14908222

申请日：2014-07-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Barbara Pio ,  Jinlong Jiang ,  Alexander Pasternak ,  Shuzhi Dong ,  Ronald Dale Ferguson, II ,  Zack Zhiqiang Guo ,  Harry Chobanian ,  Jessica Frie ,  Yan Guo ,  Zhicai Wu ,  Yang Yu ,  Ming Wang

IPC: C07D471/10 ,  A61K45/06 ,  A61K31/435 ,  A61K31/506 ,  A61K31/5386 ,  C07D451/00 ,  A61K31/46 ,  A61K31/497 ,  C07D498/10 ,  A61K31/444 ,  A61K31/501

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/444 ,  A61K31/46 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5386 ,  A61K45/06 ,  C07D451/00 ,  C07D493/04 ,  C07D498/10

Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。 这些化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭和慢性肾脏疾病以及与过量的盐和水保留有关的病症的医学病症。

公开(公告)号：US10450335B2

公开(公告)日：2019-10-22

申请号：US16061732

申请日：2016-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Wenlang Fu ,  Zhiqiang Guo ,  Ning Qi ,  Izzat T. Raheem ,  Petr Vachal ,  Ming Wang ,  John D. Schreier

IPC: C07F9/655 ,  A61K31/675 ,  A61P31/18 ,  C07F9/6561 ,  A61K45/06

Abstract: Compounds of Formula I: I and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

公开(公告)号：US20180362563A1

公开(公告)日：2018-12-20

申请号：US16061732

申请日：2016-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Wenlang Fu ,  Zhiqiang Guo ,  Ning Qi ,  Izzat T. Raheem ,  Petr Vachal ,  Ming Wang ,  John D. Schreier

IPC: C07F9/6561 ,  A61K45/06 ,  A61P31/18 ,  A61K31/675

CPC classification number: C07F9/65616 ,  A61K31/675 ,  A61K45/06 ,  A61P31/18

Abstract: Compounds of Formula I: I and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

公开(公告)号：US20180162874A1

公开(公告)日：2018-06-14

申请号：US15579115

申请日：2016-06-20

Applicant: Gregori J. MORRIELLO ,  Lehua CHANG ,  Ashley FORSTER ,  Yili CHEN ,  Michael P. DWYER ,  Richard BERGER ,  Ming WANG ,  Kausik K. NADA ,  Jaime L. BUNDA ,  William D. SHIPE ,  Merck Sharp & Dohme Corp.

Inventor： Gregori J. Morriello ,  Michael P. Dwyer ,  Lehua Chang ,  Yili Chen ,  Ming Wang ,  Ashley Forster ,  Richard Berger ,  Kausik k Nanda ,  Jaime L Bunda ,  William D Shipe

IPC: C07D498/04 ,  C07D473/34 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28

CPC classification number: C07D498/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D473/34 ,  C07D487/04

Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：US20180370947A1

公开(公告)日：2018-12-27

申请号：US15780134

申请日：2016-11-29

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Anthony K. Ogawa ,  Linda Brockunier ,  James Tata ,  Dann L. Parker, Jr. ,  Ming Wang

IPC: C07D401/10 ,  A61P7/02 ,  C07D401/14 ,  C07D409/14

Abstract: 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 XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：US10065945B2

公开(公告)日：2018-09-04

申请号：US15104537

申请日：2015-01-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Richard Berger ,  Timothy A. Blizzard ,  Brian T. Campbell ,  Helen Y. Chen ,  John S. Debenham ,  Sunita V. Dewnani ,  Byron Dubois ,  Candido Gude ,  Zack Zhiqiang Guo ,  Bart Harper ,  Zhiyong Hu ,  Songnian Lin ,  Ping Liu ,  Ming Wang ,  Feroze Ujjainwalla ,  Jiayi Xu ,  Libo Xu ,  Rui Zhang

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12

Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.