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公开(公告)号：EP2978425B1
公开(公告)日：2017-09-27
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: C07D401/14 , C07D405/14 , C07D413/14 , A61K31/435 , A61K31/551 , A61P7/02
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）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。
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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。
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公开(公告)号：EP2358200A1
公开(公告)日：2011-08-24
申请号：EP09826651.3
申请日：2009-11-11
Applicant: Merck Sharp & Dohme Corp.
Inventor： HE, Jiafang , BAWIEC, John , LIU, Weiguo , LIANG, Gui-Bai , YANG, Lihu
CPC classification number: C07D401/12 , C07D209/52 , C07D403/12 , C07D413/12 , C07D417/12
Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
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公开(公告)号：EP3634964A1
公开(公告)日：2020-04-15
申请号：EP18735038.4
申请日：2018-06-06
Applicant: Merck Sharp & Dohme Corp.
Inventor： ARASAPPAN, Ashok , COX, Jason, M. , DEBENHAM, John, S. , GUO, Zhuyan , HE, Jiafang , HUSSAIN, Zahid , LAI, Zhong , LI, Derun , MENG, Dongfang , RAGHAVAN, Subharekha , TYAGARAJAN, Sriram
IPC: C07D487/04 , A61P25/00 , A61P9/00 , A61P25/18 , A61P13/12 , A61K31/519
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公开(公告)号：EP3180325A1
公开(公告)日：2017-06-21
申请号：EP15827513.1
申请日：2015-07-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： MERTZ, Eric , EDMONDSON, Scott D. , GUO, Zhuyan , HRUZA, Alan, W. , HE, Jiafang , SO, Sung-Sau , ALI, Amjad , GAO, Ying-Duo
IPC: C07D401/02 , C07D401/10 , A61P7/02
CPC classification number: C07D401/10 , C07D401/14 , C07D405/14
Abstract: The present invention provides a compound of Formula (I) (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（式（I））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。
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Patent Agency Ranking
公开(公告)号：EP3180325B1
公开(公告)日：2019-03-20
申请号：EP15827513.1
申请日：2015-07-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： MERTZ, Eric , EDMONDSON, Scott D. , GUO, Zhuyan , HRUZA, Alan, W. , HE, Jiafang , SO, Sung-Sau , ALI, Amjad , GAO, Ying-Duo
IPC: C07D401/10 , C07D405/14 , C07D401/14 , A61P7/02 , A61K31/4439
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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.
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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。
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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。
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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.
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