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公开(公告)号：US08604056B2
公开(公告)日：2013-12-10
申请号：US13540871
申请日：2012-07-03
申请人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
发明人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
IPC分类号： A61K31/47 , A61K31/44 , A61K31/415 , C07D215/00 , C07D233/00 , C07D233/54
CPC分类号： C07D403/04 , C07D233/68 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are 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 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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2.发明授权Arylpropionamide, arylacrylamide, ayrlpropynamide, or arylmethylurea analogs as factor XIa inhibitors 有权芳基丙酰胺，芳基丙烯酰胺，芳基丙酰胺或芳基甲基脲类似物作为因子XIa抑制剂公开(公告)号：US07626039B2
公开(公告)日：2009-12-01
申请号：US11610027
申请日：2006-12-13
申请人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
发明人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
IPC分类号： A61K31/41
CPC分类号： C07D403/04 , C07D233/68 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are 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 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： 本发明提供了式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，L1，M和R11如本文所定义。 式（I）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 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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3.发明授权Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIa inhibitors 有权芳基丙酰胺，芳基丙烯酰胺，芳基丙酰胺或芳基甲基脲类似物作为因子XIa抑制剂公开(公告)号：US08252830B2
公开(公告)日：2012-08-28
申请号：US12900542
申请日：2010-10-08
申请人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
发明人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D403/04 , C07D233/68 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are 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 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： 本发明提供了式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，L1，M和R11如本文所定义。 式（I）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 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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4.发明授权Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIa inhibitors 有权芳基丙酰胺，芳基丙烯酰胺，芳基丙酰胺或芳基甲基脲类似物作为因子XIa抑制剂公开(公告)号：US07842708B2
公开(公告)日：2010-11-30
申请号：US12573230
申请日：2009-10-05
申请人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith
发明人： Donald J. P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith
IPC分类号： A01N43/50
CPC分类号： C07D403/04 , C07D233/68 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are 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 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： 本发明提供了式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，L1，M和R11如本文所定义。 式（I）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 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：US08940720B2
公开(公告)日：2015-01-27
申请号：US13024544
申请日：2011-02-10
申请人： James R. Corte , Tianan Fang , Carl P. Decicco , Donald J. P. Pinto , Karen A. Rossi , Zilun Hu , Yoon Jeon , Mimi L. Quan , Joanne M. Smallheer , Yufeng Wang , Wu Yang
发明人： James R. Corte , Tianan Fang , Carl P. Decicco , Donald J. P. Pinto , Karen A. Rossi , Zilun Hu , Yoon Jeon , Mimi L. Quan , Joanne M. Smallheer , Yufeng Wang , Wu Yang
IPC分类号： C07D487/08 , C07D487/02 , A61K31/33 , A61K31/395 , 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： The present invention provides compounds of Formula (I): 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：US07645799B2
公开(公告)日：2010-01-12
申请号：US12266659
申请日：2008-11-07
IPC分类号： A61K31/165 , A61K31/4409 , A61K31/27 , A61K31/40 , A61K31/195 , A61K31/18 , A61K31/41 , A61K31/5375 , A61K31/44 , A61K31/381 , A61K31/426 , A61K31/415 , C07C237/24 , C07C311/11 , C07C271/28 , C07D213/04 , C07D207/30 , C07D257/04 , C07D295/033 , C07D211/98 , C07D333/38 , C07D277/40 , C07D233/88
CPC分类号： C07C255/44 , C07C237/24 , C07C271/28 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/73 , C07D213/75 , C07D215/04 , C07D215/227 , C07D231/56 , C07D233/88 , C07D257/04 , C07D277/40 , C07D295/135 , C07D333/40 , C07D409/04 , C07D413/12
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B 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.
摘要翻译： 本发明提供式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂化物形式，其中变量A，L，Z，R 3和环B如本文所定义。 式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂的化合物。 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：US08367709B2
公开(公告)日：2013-02-05
申请号：US12663861
申请日：2008-06-11
CPC分类号： C07D257/04 , C07C237/22 , C07D231/56 , C07D249/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.
摘要翻译： 公开了式（I），（II）或（III）的新型二肽类似物化合物：或作为因子XIa和/或血浆的抑制剂的立体异构体，互变异构体，药学上可接受的盐，溶剂合物或前药 激肽释放酶，含有它们的组合物，以及使用它们的方法，例如用于治疗或预防血栓形成疾病。
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公开(公告)号：US09221818B2
公开(公告)日：2015-12-29
申请号：US14236973
申请日：2012-08-06
申请人： Donald J. P. Pinto , James R. Corte , Paul J. Gilligan , Tianan Fang , Leon M. Smith, II , Yufeng Wang , Wu Yang , William R. Ewing
发明人： Donald J. P. Pinto , James R. Corte , Paul J. Gilligan , Tianan Fang , Leon M. Smith, II , Yufeng Wang , Wu Yang , William R. Ewing
IPC分类号： C07D487/08 , C07D471/06 , C07D487/06 , C07D498/06
CPC分类号： C07D519/00 , C07D471/06 , C07D471/08 , C07D487/06 , C07D487/08 , C07D498/06 , C07D498/08
摘要： The present invention provides compounds of Formula (Ia): 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（Ia）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：US20140221338A1
公开(公告)日：2014-08-07
申请号：US14236973
申请日：2012-08-06
申请人： Donald J. P. Pinto , James R. Corte , Paul J. Gilligan , Tianan Fang , Leon M. Smith, II , Yufeng Wang , Wu Yang , William R. Ewing
发明人： Donald J. P. Pinto , James R. Corte , Paul J. Gilligan , Tianan Fang , Leon M. Smith, II , Yufeng Wang , Wu Yang , William R. Ewing
IPC分类号： C07D471/06 , C07D498/06 , C07D487/06
CPC分类号： C07D519/00 , C07D471/06 , C07D471/08 , C07D487/06 , C07D487/08 , C07D498/06 , C07D498/08
摘要： The present invention provides compounds of Formula (Ia): 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（Ia）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：US5998424A
公开(公告)日：1999-12-07
申请号：US99752
申请日：1998-06-18
申请人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
发明人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
IPC分类号： C07D231/14 , C07D257/04 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , A01N43/54 , C07D211/32 , C07D277/64
CPC分类号： C07D257/04 , C07D231/14 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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