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公开(公告)号：EP3016951A1
公开(公告)日：2016-05-11
申请号：EP14741757.0
申请日：2014-07-01
发明人： QUAN, Mimi L. , HU, Zilun , WANG, Cailan , PATIL, Sharanabasappa
IPC分类号： C07D471/04 , C07D498/04 , A61K31/519 , A61P9/00 , A61P11/00
CPC分类号： C07D491/052 , C07D471/04 , C07D491/048 , C07D498/04 , C07D519/00
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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2.发明公开TETRAHYDROQUINOLINE DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开AS APPROPRIATE丝氨酸蛋白酶抑制剂的四氢喹啉
公开(公告)号：EP1601656A1
公开(公告)日：2005-12-07
申请号：EP04719245.5
申请日：2004-03-10
发明人： QUAN, Mimi, L. , WANG, Cailan , ZHOU, Jinglan , HANGELAND, Jon, J. , SEIFFERT, Dietmar, A. , KNABB, Robert, M.
IPC分类号： C07D217/02 , C07D217/12 , A61K31/47
CPC分类号： C07D401/12 , C07D215/12 , C07D215/20 , C07D215/48
摘要： The present invention provides compounds of Formula (I) ; or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, R4, R5, R13, R14, R15 and R16 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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公开(公告)号：EP3016951B1
公开(公告)日：2017-05-31
申请号：EP14741757.0
申请日：2014-07-01
发明人： QUAN, Mimi L. , HU, Zilun , WANG, Cailan , PATIL, Sharanabasappa
IPC分类号： C07D471/04 , C07D498/04 , A61K31/519 , A61P9/00 , A61P11/00
CPC分类号： C07D491/052 , C07D471/04 , C07D491/048 , C07D498/04 , C07D519/00
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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公开(公告)号：EP2961745A1
公开(公告)日：2016-01-06
申请号：EP14710732.0
申请日：2014-02-28
发明人： QUAN, Mimi L. , HU, Zilun , WANG, Cailan , GLUNZ, Peter W.
IPC分类号： C07D403/12 , C07D217/12 , C07D231/12 , C07D401/12 , C07D405/12 , C07D513/04 , A61K31/415 , A61P9/00 , A61P29/00 , A61P37/00
CPC分类号： C07D231/12 , C07D217/12 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
摘要翻译： 本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性ROCK抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其治疗心血管，平滑肌，肿瘤学，神经病理学，自身免疫性，纤维化和/或炎症性疾病的方法。
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5.发明授权
公开(公告)号：EP3016950B1
公开(公告)日：2017-06-07
申请号：EP14740124.4
申请日：2014-07-01
发明人： QUAN, Mimi L. , HU, Zilun , WANG, Cailan
IPC分类号： C07D471/04 , C07D498/04 , A61K31/4353 , A61K31/519 , A61P9/00 , A61P11/00
CPC分类号： C07D491/052 , C07D471/04 , C07D498/04
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公开(公告)号：EP2534152A1
公开(公告)日：2012-12-19
申请号：EP11704895.9
申请日：2011-02-10
IPC分类号： C07D487/06 , C07D498/06 , C07D471/08 , C07D471/18 , C07D487/08 , C07D487/18 , C07D498/08
CPC分类号： C07D487/04 , C07D471/14 , C07D471/18 , C07D487/06 , C07D487/08 , C07D487/14 , C07D487/16 , C07D487/18 , C07D498/04 , C07D498/06 , C07D498/08
摘要： or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译： 本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
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公开(公告)号：EP3481816B1
公开(公告)日：2020-06-24
申请号：EP17740240.1
申请日：2017-07-06
发明人： HU, Zilun , WANG, Cailan , QUAN, Mimi L. , GLUNZ, Peter W. , LADZIATA, Vladimir
IPC分类号： C07D401/14 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D413/10 , C07D405/14 , C07D417/14 , C07D495/04 , A61K31/5025 , A61P9/00
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公开(公告)号：EP2961745B1
公开(公告)日：2017-03-29
申请号：EP14710732.0
申请日：2014-02-28
发明人： QUAN, Mimi L. , HU, Zilun , WANG, Cailan , GLUNZ, Peter W.
IPC分类号： C07D403/12 , C07D217/12 , C07D231/12 , C07D401/12 , C07D405/12 , C07D513/04 , A61K31/415 , A61P9/00 , A61P29/00 , A61P37/00
CPC分类号： C07D231/12 , C07D217/12 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
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9.发明公开
公开(公告)号：EP3481816A1
公开(公告)日：2019-05-15
申请号：EP17740240.1
申请日：2017-07-06
发明人： HU, Zilun , WANG, Cailan , QUAN, Mimi L. , GLUNZ, Peter W.
IPC分类号： C07D401/14 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D413/10 , C07D405/14 , C07D417/14 , C07D495/04 , A61K31/5025 , A61P9/00
摘要： The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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公开(公告)号：EP2534152B1
公开(公告)日：2018-05-02
申请号：EP11704895.9
申请日：2011-02-10
IPC分类号： C07D487/06 , C07D498/06 , C07D471/08 , C07D471/18 , C07D487/08 , C07D487/18 , C07D498/08
CPC分类号： C07D487/04 , C07D471/14 , C07D471/18 , C07D487/06 , C07D487/08 , C07D487/14 , C07D487/16 , C07D487/18 , C07D498/04 , C07D498/06 , C07D498/08
摘要： or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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