公开(公告)号：US20180179180A1

公开(公告)日：2018-06-28

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 ,  C07D401/04

CPC classification number: C07D401/14 ,  C07C269/06 ,  C07D401/04 ,  C07D401/10 ,  C07D413/14

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：US20160376272A1

公开(公告)日：2016-12-29

申请号：US15116547

申请日：2015-02-06

Applicant: Santhosh F. NEELAKAVIL ,  Scott D. EDMONDSON ,  Alan W. HRUZA ,  Zahid HUSSAIN ,  Charles LESBURG ,  Remond MONINGKA ,  Merck Sharp & Dohme Corp.

Inventor： Santhosh F. Neelamkavil ,  Scott D. Edmondson ,  Alan W. Hruza ,  Zahid Hussain ,  Charles Lesburg ,  Remond Moningka

IPC: C07D471/08 ,  C07D487/08

CPC classification number: C07D471/08 ,  C07D487/08

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：US20130217695A1

公开(公告)日：2013-08-22

申请号：US13847646

申请日：2013-03-20

Applicant: Merck Sharp & Dohme Corp.

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

IPC: C07D487/04

CPC classification number: A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

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.

Abstract translation: 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20170210732A1

公开(公告)日：2017-07-27

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 ,  C07D401/06 ,  C07D401/14 ,  C07D417/14 ,  C07D413/14

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：US20170197953A1

公开(公告)日：2017-07-13

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 ,  C07D413/10 ,  C07D401/12 ,  C07D401/14 ,  C07D401/10 ,  C07D213/89

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：US10214512B2

公开(公告)日：2019-02-26

申请号：US15771538

申请日：2016-10-24

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Jiayi Xu ,  Amjad Ali ,  Wei Zhou ,  Ying-Duo Gao ,  Scott D. Edmondson ,  Eric Mertz ,  Santhosh F. Neelamkavil ,  Weiguo Liu ,  Wanying Sun ,  Dong-Ming Shen ,  Bart Harper ,  Cheng Zhu ,  Thomas Bara ,  Yeon-Hee Lim ,  Meng Yang

IPC: C07D471/08 ,  C07D471/18 ,  C07D401/14 ,  A61P7/02 ,  C07D487/08 ,  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：US10123995B2

公开(公告)日：2018-11-13

申请号：US15542948

申请日：2016-01-15

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Eric Mertz ,  Weiguo Liu ,  Scott D. Edmondson ,  Amjad Ali ,  Ying-Duo Gao ,  Santhosh F. Neelamkavil ,  Sung-Sau So ,  Remond Moningka ,  Wanying Sun ,  Alan Hruza ,  Linda L. Brockunier

IPC: A61K31/435 ,  A61K31/4375 ,  A61K31/195 ,  A61P7/02 ,  A61P7/04 ,  C07D221/18 ,  C07D221/04 ,  C07D401/10

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：US20180079743A1

公开(公告)日：2018-03-22

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 ,  C07D409/14 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D413/14

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：US20180000795A1

公开(公告)日：2018-01-04

申请号：US15542948

申请日：2016-01-15

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Eric Mertz ,  Weiguo Liu ,  Scott D. Edmondson ,  Amjad Ali ,  Ying-Duo Gao ,  Santhosh F. Neelamkavil ,  Sung-Sau So ,  Remond Moningka ,  Wanying Sun ,  Alan Hruza ,  Linda L. Brockunier

IPC: A61K31/435 ,  A61K31/195 ,  C07D221/18 ,  C07D401/10

CPC classification number: A61K31/435 ,  A61K31/195 ,  A61K31/4375 ,  A61P7/02 ,  A61P7/04 ,  C07D221/04 ,  C07D221/18 ,  C07D401/10

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：US20170348309A1

公开(公告)日：2017-12-07

申请号：US15683007

申请日：2017-08-22

Applicant: Merck Sharp & Dohme Corp.

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

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

CPC classification number: A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

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.