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：US20140378493A1

公开(公告)日：2014-12-25

申请号：US14480202

申请日：2014-09-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Pengcheng Patrick Shao ,  Wanying Sun ,  Revathi Reddy Katipally ,  Petr Vachal ,  Feng Ye ,  Jian Liu ,  Deyou Sha

IPC: C07D498/04 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/437 ,  A61K31/444 ,  A61K31/424 ,  A61K31/506

CPC classification number: C07D498/04 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

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：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.

公开(公告)号：US10086000B2

公开(公告)日：2018-10-02

申请号：US15532548

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Chunhui Huang

IPC: C07D471/04 ,  A61K31/5513 ,  A61K45/06 ,  C07D471/14 ,  A01N43/00 ,  C07D519/00

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes 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 cancers.

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：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：US20170360800A1

公开(公告)日：2017-12-21

申请号：US15532548

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew Lloyd Childers ,  Francesc Xavier Fradera Llinas ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Nunzio Sciammetta ,  Patrick Pengcheng Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla

IPC: A61K31/5513 ,  C07D471/14 ,  C07D471/04 ,  A61K45/06 ,  C07D519/00 ,  A01N43/00

CPC classification number: A61K31/5513 ,  A01N43/00 ,  A61K31/551 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes 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 cancers.

公开(公告)号：US09346825B2

公开(公告)日：2016-05-24

申请号：US14480202

申请日：2014-09-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Pengcheng Patrick Shao ,  Wanying Sun ,  Revathi Reddy Katipally ,  Petr Vachal ,  Feng Ye ,  Jian Liu ,  Deyou Sha

IPC: C07D498/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/424 ,  A61K31/444 ,  A61K31/506

CPC classification number: C07D498/04 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。