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：US10407421B2

公开(公告)日：2019-09-10

申请号：US16076781

申请日：2017-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Reynalda Keh Dejesus ,  Haifeng Tang ,  Xianhai Huang ,  Jinlong Jiang ,  Yan Guo ,  Hongwu Wang

IPC: C07D417/14 ,  A61K45/06 ,  C07D471/04 ,  C07C53/18 ,  A61P31/04 ,  A61K31/424 ,  A61K31/431 ,  A61K31/439

Abstract: The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.

公开(公告)号：US20190071436A1

公开(公告)日：2019-03-07

申请号：US16076781

申请日：2017-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Reynalda Keh Dejesus ,  Haifeng Tang ,  Xianhai Huang ,  Jinglong Jiang ,  Yan Guo ,  Hongwu Wang

IPC: C07D417/14 ,  A61P31/04

CPC classification number: C07D417/14 ,  A61K31/424 ,  A61K31/431 ,  A61K31/439 ,  A61K45/06 ,  A61P31/04 ,  C07C53/18 ,  C07D471/04

Abstract: The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.

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.

公开(公告)号：US10011585B2

公开(公告)日：2018-07-03

申请号：US15329635

申请日：2015-07-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Weiguo Liu ,  Scott D Edmondson ,  Zhuyan Guo ,  Alan Hruza ,  Sung-Sau So ,  Wanying Sun ,  Amjad Ali ,  Rongze Kuang ,  Ying-Duo Gao ,  Anthony K Ogawa

IPC: C07D401/06 ,  C07D401/14

CPC classification number: C07D401/06 ,  C07D401/14

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, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：US11230543B2

公开(公告)日：2022-01-25

申请号：US16912146

申请日：2020-06-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Yi Zang ,  Weidong Pan ,  Anthony Ogawa ,  Linda Brockunier ,  Xianhai Huang ,  Hongwu Wang ,  Rudrajit Mal ,  Tesfaye Biftu ,  Min Park ,  Yan Guo ,  Jinlong Jiang ,  Helen Y. Chen ,  Christopher W. Plummer

IPC: C07D417/14 ,  C07D471/04 ,  C07C53/18 ,  C07F9/6558 ,  A61K31/433 ,  A61K31/444 ,  A61K31/4439 ,  A61K45/06 ,  A61P31/04 ,  A61K31/427 ,  A61K31/424 ,  A61K31/431 ,  A61K31/551

Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, A2, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

公开(公告)号：US11174248B2

公开(公告)日：2021-11-16

申请号：US16755177

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： John Acton ,  David Annunziato Candito ,  J. Michael Ellis ,  Peter H. Fuller ,  Hakan Gunaydin ,  Blair T. Lapointe ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Barbara Pio ,  Vladimir Simov ,  Harold B. Wood

IPC: A61K31/506 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.

公开(公告)号：US11161854B2

公开(公告)日：2021-11-02

申请号：US16755172

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp. ,  David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

Inventor： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC: C07D491/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/08 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.

公开(公告)号：US20180339983A1

公开(公告)日：2018-11-29

申请号：US15775487

申请日：2016-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Haifeng Tang ,  Weiguo Liu ,  Fa-Xiang Ding ,  Wanying Sun ,  Yi Zang ,  Weidong Pan ,  Anthony Ogawa ,  Linda Brockunier ,  Xianhai Huang ,  Hongwu Wang ,  Rudrajit Mal ,  Tesfaye Biftu ,  Min Park ,  Yan Guo ,  Jinlong Jiang ,  Helen Y. Chen ,  Christopher W. Plummer

IPC: C07D417/14 ,  A61K31/427 ,  A61P31/04

Abstract: The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A1, Q, M, W, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.