公开(公告)号：EP3283464A1

公开(公告)日：2018-02-21

申请号：EP16780505.0

申请日：2016-04-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： MERTZ, Eric ,  EDMONDSON, Scott D. ,  SO, Sung-Sau ,  SUN, Wanying ,  LIU, Weiguo ,  NEELAMKAVIL, Santhosh F. ,  GAO, Ying-Duo ,  HRUZA, Alan ,  ZANG, Yi ,  ALI, Amjad ,  MAL, Rudrajit ,  HE, Jiafang ,  KUANG, Rongze ,  WU, Heping ,  OGAWA, Anthony K. ,  NOLTING, Andrew F.

IPC: C07D233/68 ,  A61K31/426 ,  A61K31/4178 ,  A61P9/00 ,  C07D241/00

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：EP2978425A2

公开(公告)日：2016-02-03

申请号：EP14776100.1

申请日：2014-03-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： OGAWA, Anthony ,  EDMONDSON, Scott ,  ERION, Mark ,  NEELAMKAVIL, Santosh ,  GUO, Zhuyan ,  MAL, Rudrajit ,  HE, Jiafang ,  LIU, Weiguo ,  VANDE BUNTE, Ellen, K.

IPC: A61K31/435

CPC classification number: C07D213/64 ,  A61K31/551 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/044 ,  C07D491/052 ,  C07F9/65583

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.

Abstract translation: 本发明提供了式（I）的化合物; 以及包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。

公开(公告)号：EP2021327B1

公开(公告)日：2012-04-04

申请号：EP07794762.0

申请日：2007-05-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： GE, Min ,  HE, Jiafang ,  LAU, Fiona Wai Yu ,  LIANG, Gui-Bai ,  LIN, Songnian ,  LIU, Weiguo ,  WALSH, Shawn, P. ,  YANG, Lihu

IPC: C07D213/643 ,  C07D307/93 ,  C07D311/94 ,  C07D333/78 ,  C07D405/04 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07C62/34 ,  C07C62/38 ,  C07C229/50 ,  A61K31/343 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4412 ,  A61K31/427 ,  A61P1/18

CPC classification number: C07D213/643 ,  C07C62/34 ,  C07C62/38 ,  C07C229/50 ,  C07C2603/08 ,  C07D307/93 ,  C07D311/94 ,  C07D333/78 ,  C07D405/04 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12

Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP3368036A1

公开(公告)日：2018-09-05

申请号：EP16860556.6

申请日：2016-10-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： XU, Jiayi ,  ALI, Amjad ,  ZHOU, Wei ,  GAO, Ying-Duo ,  EDMONDSON, Scott, D. ,  MERTZ, Eric ,  NEELAMKAVIL, Santhosh, F. ,  LIU, Weiguo ,  SUN, Wanying ,  SHEN, Dong-Ming ,  HARPER, Bart ,  ZHU, Cheng ,  BARA, Thomas ,  LIM, Yeon-Hee ,  YANG, Meng

IPC: A61K31/44 ,  A61K31/4418 ,  A61K31/4427 ,  C07D213/02 ,  C07D213/04 ,  C07D401/06

CPC classification number: C07D401/14 ,  A61K45/06 ,  A61P7/02 ,  C07D401/04 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D513/08

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：EP3148542A1

公开(公告)日：2017-04-05

申请号：EP15800524.9

申请日：2015-05-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIU, Weiguo ,  EDMONDSON, Scott D. ,  GUO, Zhuyan ,  MERTZ, Eric ,  OGAWA, Anthony K. ,  SO, Sung-Sau ,  SUN, Wanying ,  BROCKUNIER, Linda L. ,  ALI, Amjad ,  KUANG, Rongze ,  WU, Heping

IPC: A61K31/44 ,  A61K31/4192 ,  A61K31/167

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.

Abstract translation: 本发明提供了式I化合物（化学式应插入此处）和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。 这些化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。

公开(公告)号：EP3978472A1

公开(公告)日：2022-04-06

申请号：EP21204101.6

申请日：2016-12-12

Applicant: MERCK SHARP & DOHME CORP.

Inventor： TANG, Haifeng ,  LIU, Weiguo ,  DING, Fa-Xiang ,  SUN, Wanying ,  ZANG, Yi ,  PAN, Weidong ,  OGAWA, Anthony ,  BROCKUNIER, Linda ,  HUANG, Xianhai ,  WANG, Hongwu ,  MAL, Rudrajit ,  BIFTU, Tesfaye ,  PARK, Min ,  GUO, Yan ,  JIANG, Jinlong ,  CHEN, Helen ,  PLUMMER, Christopher, W.

IPC: C07D205/08 ,  A61K31/397 ,  A61P31/04 ,  C07F9/6558 ,  C07C53/18

Abstract: The present invention relates to biaryl monobactam compounds of Formula I:

and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A 1 , Q, A 2 , M, W, R X and R z 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：EP3694330A1

公开(公告)日：2020-08-19

申请号：EP18867260.4

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： CANDITO, David Annunziato ,  GRAHAM, Thomas, H. ,  ACTON, John ,  CHAU, Ryan Wing-Kun ,  CHEN, Joanna, L. ,  ELLIS, J. Michael ,  FULLER, Peter, H. ,  GULATI, Anmol ,  GUNAYDIN, Hakan ,  KATTAR, Solomon ,  KEYLOR, Mitchell Henry ,  LAPOINTE, Blair, T. ,  LIU, Ping ,  LIU, Weiguo ,  METHOT, Joey, L. ,  NEELAMKAVIL, Santhosh, F. ,  SIMOV, Vladimir ,  TONG, Ling ,  WOOD, Harold, B.

IPC: A01N43/42 ,  C07D487/04

公开(公告)号：EP3180327B1

公开(公告)日：2019-05-08

申请号：EP15827597.4

申请日：2015-07-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIU, Weiguo ,  EDMONDSON, Scott D. ,  GUO, Zhuyan ,  HRUZA, Alan ,  SO, Sung-Sau ,  SUN, Wanying ,  ALI, Amjad ,  KUANG, Rongze ,  GAO, Ying-Duo ,  OGAWA, Anthony K.

IPC: C07D401/14

公开(公告)号：EP3148542B1

公开(公告)日：2019-02-27

申请号：EP15800524.9

申请日：2015-05-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIU, Weiguo ,  EDMONDSON, Scott D. ,  GUO, Zhuyan ,  MERTZ, Eric ,  OGAWA, Anthony K. ,  SO, Sung-Sau ,  SUN, Wanying ,  BROCKUNIER, Linda L. ,  ALI, Amjad ,  KUANG, Rongze ,  WU, Heping

IPC: C07D401/10 ,  C07D213/89 ,  C07D401/14 ,  C07D401/12 ,  C07D413/10 ,  C07D417/10 ,  A61K31/4427 ,  A61P7/02

公开(公告)号：EP3426248A1

公开(公告)日：2019-01-16

申请号：EP17763763.4

申请日：2017-03-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIU, Weiguo ,  DING, Fa-Xiang ,  SUN, Wanying ,  DEJESUS, Reynalda, Keh ,  TANG, Haifeng ,  HUANG, Xianhai ,  JIAN, Jinlong ,  GUO, Yan ,  WANG, Hongwu

IPC: A61K31/454 ,  A61K31/427 ,  A61K31/501 ,  C07D417/12