公开(公告)号：EP2882754A1

公开(公告)日：2015-06-17

申请号：EP13748245.1

申请日：2013-08-06

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： BARA, Thomas ,  BHAT, Sathesh ,  BISWAS, Dipshika ,  BROCKUNIER, Linda ,  BURNETTE, Duane ,  CHACKALAMANNIL, Samuel ,  CHELIAH, Mariappan, V. ,  CHEN, Austin ,  CLASBY, Martin ,  COLANDREA, Vince, J. ,  GUO, Zhuyan ,  HAN, Yongxin ,  JAYNE, Charles ,  JOSIEN, Hubert ,  MARCANTONIO, Karen ,  MIAO, Shouwu ,  NEELAMKAVIL, Santhosh ,  PINTO, Patrick ,  RAJAGOPALAN, Murali ,  SHAH, Unmesh ,  VELAZQUEZ, Francisco ,  VENKATRAMAN, Srikanth ,  XIA, Yan

IPC: C07D491/107 ,  A61K31/343 ,  A61K31/407 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07K5/08 ,  A61K38/06 ,  A61K45/06 ,  C07D419/00 ,  C07D491/22

Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

Abstract translation: 本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途以及这些化合物的合成。

公开(公告)号：EP2882754B1

公开(公告)日：2018-10-03

申请号：EP13748245.1

申请日：2013-08-06

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： BARA, Thomas ,  BHAT, Sathesh ,  BISWAS, Dipshika ,  BROCKUNIER, Linda ,  BURNETTE, Duane ,  CHACKALAMANNIL, Samuel ,  CHELIAH, Mariappan, V. ,  CHEN, Austin ,  CLASBY, Martin ,  COLANDREA, Vince, J. ,  GUO, Zhuyan ,  HAN, Yongxin ,  JAYNE, Charles ,  JOSIEN, Hubert ,  MARCANTONIO, Karen ,  MIAO, Shouwu ,  NEELAMKAVIL, Santhosh ,  PINTO, Patrick ,  RAJAGOPALAN, Murali ,  SHAH, Unmesh ,  VELAZQUEZ, Francisco ,  VENKATRAMAN, Srikanth ,  XIA, Yan

IPC: C07D491/22 ,  C07D419/00 ,  A61K45/06 ,  A61K31/343 ,  A61K31/407 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07K5/08 ,  A61K38/06 ,  A61K45/06 ,  C07D419/00 ,  C07D491/22

Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

公开(公告)号：EP2473491B1

公开(公告)日：2013-07-17

申请号：EP10722268.9

申请日：2010-06-01

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

Inventor： NISHIDA, Hidemitsu ,  SAITOH, Fumihiko ,  HIRABAYASHI, Tomokazu ,  CHACKALAMANNIL, Samuel ,  CHAN, Tin-Yau ,  CHELLIAH, Mariappan, V. ,  CLASBY, Martin, C. ,  DWYER, Michael, P. ,  GREENLEE, William, J. ,  XIA, Yan ,  NEELAMKAVIL, Santhosh ,  SHAH, Unmesh, G.

IPC: C07D265/32 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  A61K31/5377 ,  A61P7/02

CPC classification number: C07D413/12 ,  C07D265/32 ,  C07D413/04 ,  C07D413/14

公开(公告)号：EP3049435A1

公开(公告)日：2016-08-03

申请号：EP14847937.1

申请日：2014-09-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： MERTZ, Eric ,  EDMONDSON, Scott D. ,  SHAO, Ning ,  NEELAMKAVIL, Santhosh ,  POKER, Corey ,  HUSSAIN, Zahid ,  GUO, Zhuyan ,  KEVIN, Nancy Jo ,  ZANG, Yi ,  HE, Jiafang

IPC: C07K14/745

CPC classification number: C07D401/14 ,  A01N1/0226 ,  C07D211/60 ,  C07D401/06 ,  C07D401/10 ,  C12N9/6443 ,  C12Y304/21027

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.

Abstract translation: 本发明提供了式（I）化合物：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：EP3054944A1

公开(公告)日：2016-08-17

申请号：EP14851664.4

申请日：2014-10-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： SHAO, Ning ,  EDMONDSON, Scott D. ,  NEELAMKAVIL, Santhosh ,  GUO, Zhuyan ,  MERTZ, Eric ,  ZANG, Yi ,  HE, Jiafang

IPC: A61K31/397 ,  A61K31/7088 ,  C07D413/14

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.

Abstract translation: 本发明提供式（I）化合物（结构表示）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，高凝血性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：EP2190820B1

公开(公告)日：2013-04-10

申请号：EP08797693.2

申请日：2008-08-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： NEELAMKAVIL, Santhosh ,  BOYLE, Craig, D. ,  CHACKALAMANNIL, Samuel

IPC: C07D223/04 ,  C07D409/04 ,  A61K31/55 ,  A61P3/00

CPC classification number: C07D223/08 ,  C07D223/04 ,  C07D223/12 ,  C07D223/30 ,  C07D243/08 ,  C07D401/12 ,  C07D409/04