公开(公告)号：EP3371162A1

公开(公告)日：2018-09-12

申请号：EP16860557.4

申请日：2016-10-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： ALI, Amjad ,  LIM, Yeon-Hee ,  XU, Jiayi ,  ZHOU, Wei

IPC: C07D401/06 ,  C07D487/04 ,  A61K31/4747 ,  C07D491/10

CPC classification number: C07D519/00 ,  C07D498/10

Abstract: The present invention provides a compound of Formula (I) and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds and said stereoisomers, and pharmaceutical compositions thereof, and methods for using said compounds and compositions 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：EP3131897A1

公开(公告)日：2017-02-22

申请号：EP15780578.9

申请日：2015-04-10

Applicant: Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

Inventor： SAKURADA, Isao ,  HIRABAYASHI, Tomokazu ,  MAEDA, Yoshitaka ,  NAGASUE, Hiroshi ,  MIZUNO, Takashi ,  XU, Jiayi ,  ZHANG, Ting ,  SMITH, Cameron ,  PARKER, Dann

IPC: C07D413/14 ,  C07D261/20 ,  C07D207/02

CPC classification number: C07D413/14 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/52 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00

Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.

Abstract translation: 在其许多实施方案中，本发明提供了由式（I）表示的新一类苯甲酰胺化合物或其药学上可接受的盐或溶剂合物，或包含一种或多种所述化合物或其药学上可接受的盐或溶剂合物的药物组合物，以及使用 所述化合物或其药学上可接受的盐或溶剂化物用于治疗或预防血栓形成，栓塞，高凝状态或纤维变性。

公开(公告)号：EP3131896B1

公开(公告)日：2019-01-30

申请号：EP15779184.9

申请日：2015-04-10

Applicant: Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

Inventor： SAKURADA, Isao ,  HIRABAYASHI, Tomokazu ,  MAEDA, Yoshitaka ,  NAGASUE, Hiroshi ,  MIZUNO, Takashi ,  XU, Jiayi ,  ZHANG, Ting ,  SMITH, Cameron ,  PARKER, Dann

IPC: C07D413/14 ,  C07D261/20 ,  C07D207/02 ,  A61K31/439

公开(公告)号：EP3134408B1

公开(公告)日：2020-08-12

申请号：EP15783339.3

申请日：2015-04-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIM, Yeon-Hee ,  GUO, Zhuyan ,  ALI, Amjad ,  EDMONDSON, Scott D. ,  LIU, Weiguo ,  GALLO-ETIENNE, Gioconda V. ,  WU, Heping ,  GAO, Ying-Duo ,  STAMFORD, Andrew M. ,  YU, Younong ,  KEVIN, Nancy J. ,  ANAND, Rajan ,  SHA, Deyou ,  NEELAMKAVIL, Santhosh F. ,  HUSSAIN, Zahid ,  KUMAR, Puneet ,  MONINGKA, Remond ,  DUFFY, Joseph L. ,  XU, Jiayi ,  JIANG, Yu ,  SONE, Hiroki ,  CHAKRABARTI, Anjan

IPC: C07D471/10 ,  A61K31/438 ,  C07D498/20

公开(公告)号：EP3258929A1

公开(公告)日：2017-12-27

申请号：EP16752841.3

申请日：2016-02-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： MENG, Dongfang ,  LI, Hong ,  YANG, Meng ,  RUIZ, Manuel de Lera ,  DEWNANI, Sunita, V. ,  JIAN, Tianying ,  PARKER, Dann, L., Jr. ,  ZHANG, Ting ,  CAMPEAU, Louis-Charles ,  HARPER, Bart ,  WOOD, Harold, B. ,  XU, Jiayi ,  BERGER, Richard ,  WU, Jane Yang ,  ORR, Robert, K. ,  WALSH, Shawn, P.

IPC: A61K31/33 ,  A61K31/41 ,  A61K31/395 ,  A61K31/4164 ,  A61K31/4184

CPC classification number: C07D471/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/14 ,  C07D498/04 ,  C07D513/04

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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

公开(公告)号：EP3097101A1

公开(公告)日：2016-11-30

申请号：EP15740935.0

申请日：2015-01-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： BERGER, Richard ,  BLIZZARD, Timothy A. ,  CAMPBELL, Brian T. ,  CHEN, Helen Y. ,  DEBENHAM, John S. ,  DEWNANI, Sunita V. ,  DUBOIS, Byron ,  GUDE, Candido ,  GUO, Zhiqiang ,  HARPER, Bart ,  HU, Zhiyong ,  LIN, Songnian ,  LIU, Ping ,  WANG, Ming ,  UJJAINWALLA, Feroze ,  XU, Jiayi ,  XU, Libo ,  ZHANG, Rui

IPC: C07D471/04

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

Abstract translation: 式I的化合物作为MGAT2抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

公开(公告)号：EP2931734B1

公开(公告)日：2020-12-02

申请号：EP13864999.1

申请日：2013-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： LIN, Songnian ,  CAMPBELL, Brian ,  DEWNANI, Sunita, V. ,  KATS-KAGAN, Roman ,  XU, Jiayi ,  XU, Libo ,  ZHANG, Rui

IPC: C07F9/32 ,  C07D401/14 ,  A61K31/444 ,  A61P3/10

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：EP2903977B1

公开(公告)日：2017-09-20

申请号：EP13776702.6

申请日：2013-10-07

Applicant: Merck Sharp & Dohme Corp.

Inventor： ARRINGTON, Kenneth, L. ,  BURGEY, Christopher ,  GILFILLAN, Robert ,  HAN, Yongxin ,  PATEL, Mehul ,  LI, Chun Sing ,  LI, Yaozong ,  LUO, Yunfu ,  XU, Jiayi

IPC: C07D401/14 ,  C07D239/56 ,  C07D403/06 ,  C07D403/14 ,  C07D239/52 ,  C07D239/54 ,  C07D471/04 ,  A61K31/513 ,  A61P31/18

CPC classification number: C07D471/04 ,  A61K31/513 ,  A61K45/06 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

公开(公告)号：EP2934538A1

公开(公告)日：2015-10-28

申请号：EP13873301.9

申请日：2013-12-16

Applicant: Merck Sharp & Dohme Corp. ,  Mochida Pharmaceutical Co., Ltd.

Inventor： SMITH, Cameron, James ,  TAN, John, Qiang ,  ZHANG, Ting ,  BALKOVEC, James ,  GREENLEE, William, John ,  GUO, Liangqin ,  XU, Jiayi ,  CHEN, Yi-heng ,  CHEN, Yili ,  CHACKALAMANNIL, Samuel ,  HIRABAYASHI, Tomokazu ,  NAGASUE, Hiroshi ,  OGAWA, Kouki

IPC: A61K31/5377 ,  C07D413/12

CPC classification number: C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.

Abstract translation: 本发明提供式（I）（结构表示）的化合物，其中R 1为H或C 1-6烷基，R 2为H或C 1-6烷基或CH 2 OH，R 3为H或C 1-6烷基，且R 4为H或 条件是当R 1，R 2和R 3是H时，R 4是C 1-6烷基，并且当R 1，R 2和R 4是H时，则R 3是C 1-6烷基，并且当R 1，R 3和 R 4是H，R 2是C 1-6烷基或-CH 2 OH，并且当R 2，R 3和R 4是H时，则R 1是C 1-6烷基; A为1）具有1-3个独立地选自N，S和O的杂原子的9-10元双环杂环，该9-10元双环杂环为未取代的或被R5取代且未被取代或被R6取代且未被取代或被NH2取代 或2）未被取代或被R 5取代的未被取代或被R 6取代且未被取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 且B为1）具有1或2个独立地选自N，S或O的杂原子的5-或6-元单环杂环，其未被取代或在碳或氮原子上被R7取代，未被取代或在碳或氮上被取代 原子与R8取代，并且未被取代或在碳或氮原子上被R9取代，或2）具有1,2或3个氮原子的8-或9-元稠合双环杂环，其未被取代或在碳或氮原子上被 R7，并且未被取代或在碳或氮原子上被R8取代; 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的方法。