公开(公告)号：US09676723B2

公开(公告)日：2017-06-13

申请号：US15116576

申请日：2015-02-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Santhosh F. Neelamkavil ,  Scott D. Edmondson ,  Zhuyan Guo ,  Alan W. Hruza ,  Zahid Hussain ,  Remond Moningka ,  Nancy Jo Kevin

IPC: C07D217/24 ,  C07D401/06 ,  C07D209/46 ,  C07C55/32 ,  C07D409/14 ,  C07D401/12 ,  C07D417/12 ,  C07D401/14 ,  C07D413/12 ,  C07D405/12

CPC classification number: C07D217/24 ,  C07C55/32 ,  C07D209/46 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

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：US09663527B2

公开(公告)日：2017-05-30

申请号：US15116659

申请日：2015-02-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Santhosh F. Neelamkavil ,  Scott D. Edmondson ,  Zhuyan Guo ,  Alan W. Hruza ,  Zahid Hussain ,  Charles A. Lesburg ,  Remond Moningka ,  Anthony K. Ogawa ,  Rudrajit Mal

IPC: C07D487/08 ,  C07D471/08

CPC classification number: C07D487/08 ,  C07D471/08

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：US20200206221A1

公开(公告)日：2020-07-02

申请号：US16811728

申请日：2020-03-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott D. Edmondson ,  Michael H. Fischer ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

IPC: A61K31/4985 ,  A61K38/28 ,  C07D487/04 ,  A61K45/06 ,  A61K31/498

Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

公开(公告)号：US10239863B2

公开(公告)日：2019-03-26

申请号：US15789088

申请日：2017-10-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ning Shao ,  Scott D. Edmondson ,  Santhosh Neelamkavil ,  Zhuyan Guo ,  Eric Mertz ,  Yi Zang ,  Jiafang He

IPC: C07D401/14 ,  C07D401/10 ,  C07C269/06 ,  C07D413/14 ,  C07D401/04

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：US10081617B2

公开(公告)日：2018-09-25

申请号：US15565748

申请日：2016-04-11

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Eric Mertz ,  Scott D. Edmondson ,  Sung-Sau So ,  Wanying Sun ,  Weiguo Liu ,  Santhosh F. Neelamkavil ,  Ying-Duo Gao ,  Alan Hruza ,  Yi Zang ,  Amjad Ali ,  Rudrajit Mal ,  Jiafang He ,  Rongze Kuang ,  Heping Wu ,  Anthony K. Ogawa ,  Andrew F. Nolting

IPC: C07D401/14 ,  C07D413/14 ,  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：US09868727B2

公开(公告)日：2018-01-16

申请号：US15329634

申请日：2015-07-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Scott D. Edmondson ,  Zhuyan Guo ,  Sung-Sau So ,  Anthony K. Ogawa ,  Rongze Kuang ,  Heping Wu ,  Amjad Ali ,  Ying-Duo Gao ,  Yu Jiang ,  Chunsing Li ,  Tingting Yu

IPC: C07D409/14 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  C07D401/06 ,  A61K31/4439 ,  A61K31/444

CPC classification number: C07D409/14 ,  A61P7/02 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

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：US09783530B2

公开(公告)日：2017-10-10

申请号：US15312839

申请日：2015-05-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Scott D. Edmondson ,  Zhuyan Guo ,  Eric Mertz ,  Anthony K. Ogawa ,  Sung-Sau So ,  Wanying Sun ,  Linda L. Brockunier ,  Amjad Ali ,  Rongze Kuang ,  Heping Wu

IPC: C07D417/10 ,  C07D401/10 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10

CPC classification number: C07D417/10 ,  C07D213/89 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10

Abstract: The present invention provides a compound of Formula I (The chemical formula should be inserted here.) 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：US20150274664A1

公开(公告)日：2015-10-01

申请号：US14431366

申请日：2013-09-25

Applicant: John J. ACTON ,  Scott D. EDMONDSON ,  Ping LIU ,  Michael W. MILLER ,  Harold B. WOOD ,  Byron G. DUBOIS ,  William B. GEISS ,  MERCK SHARP & DOHME CORP.

Inventor： John J. Acton ,  Scott D. Edmondson ,  Ping Liu ,  Michael W. Miller ,  Harold B. Wood ,  Byron G. DuBois ,  William B. Geiss

IPC: C07D211/60 ,  C07D401/12 ,  C07D413/04 ,  C07D401/14 ,  C07D401/04

CPC classification number: C07D211/60 ,  A61K31/506 ,  C07D211/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

Abstract: Substituted cyclopropyl piperidinyl compounds and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 公开了用于治疗或预防2型糖尿病和类似病症的取代的环丙基哌啶基化合物及其药学上可接受的盐。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US20180353507A1

公开(公告)日：2018-12-13

申请号：US15780462

申请日：2016-12-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： David E. Kelley ,  Ping Liu ,  Harold B. Wood ,  Scott D. Edmondson ,  Hideo Makimura ,  Xiaoyan Li ,  Timothy Joseph Kowalski

IPC: A61K31/506 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/18

CPC classification number: A61K31/506 ,  A61K31/00 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/18 ,  C12Q1/02 ,  G01N33/74 ,  G01N2333/726 ,  G01N2800/042

Abstract: Use of a GPR119 agonist in the prevention or treatment of hypoglycemia is disclosed, addition, pharmaceutical compositions and combinations of a GPR1 19 agonist with insulin, insulin analog, insulin secretagogue or or other drug(s) that reduces plasma glucose levels to below 70 mg/dL described herein.

公开(公告)号：US10093683B2

公开(公告)日：2018-10-09

申请号：US15305421

申请日：2015-04-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： Yeon-Hee Lim ,  Zhuyan Guo ,  Amjad Ali ,  Scott D. Edmondson ,  Weiguo Liu ,  Gioconda V. Gallo-Etienne ,  Heping Wu ,  Ying-Duo Gao ,  Andrew W. Stamford ,  Younong Yu ,  Nancy J. Kevin ,  Rajan Anand ,  Deyou Sha ,  Santhosh F. Neelamkavil ,  Zahid Hussain ,  Puneet Kumar ,  Remond Moningka ,  Joseph L. Duffy ,  Jiayi Xu ,  Yu Jiang ,  Anjan Chakrabarti ,  Hiroki Sone

IPC: C07D498/20 ,  C07F9/6561 ,  C07D487/10 ,  C07D498/10 ,  C07D471/10

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) 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.