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1.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20110028446A1
公开(公告)日：2011-02-03
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： A61K31/4178 , C07D403/10 , C07D401/14 , C07D403/14 , C07D233/68 , C07D409/12 , C07D403/12 , C07D401/10 , C07D413/14 , C07D417/14 , C07D487/08 , A61K31/4439 , A61K31/4174 , A61K31/4709 , A61K31/5377 , A61K31/497 , A61P7/00 , A61P9/00 , A61P9/10
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：US20100173899A1
公开(公告)日：2010-07-08
申请号：US12663861
申请日：2008-06-11
IPC分类号： A61K31/541 , C07D257/04 , C07D215/48 , C07D277/22 , C07D401/12 , C07D413/12 , C07D279/12 , A61K31/41 , A61K31/4709 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P7/02 , A61P9/10
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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3.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20120270853A1
公开(公告)日：2012-10-25
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
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： A61K31/4178 , C07D401/14 , A61K31/4439 , C07D403/12 , A61K31/4196 , C07D401/10 , A61K31/4709 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , C07D403/14 , A61K31/551 , C07D471/08 , A61P7/02 , A61P9/10 , A61P9/00 , C07D403/10
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.发明申请LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 有权含有LACTAM的化合物及其作为因子XA抑制剂的衍生物公开(公告)号：US20090176758A1
公开(公告)日：2009-07-09
申请号：US12401401
申请日：2009-03-10
申请人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
发明人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
IPC分类号： A61K31/55 , C07D401/14 , A61P9/10
CPC分类号： C07D471/04 , A61J1/00 , A61J1/03 , A61J1/05 , A61K31/4365 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/55 , A61K45/06 , B65D81/3216 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/14 , C07D417/14
摘要： The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4 I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了含有酰胺的化合物及其式I的衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”？> P4-PM-M4 I <βin-line-formula 描述=“内联式”末端=“尾”→其药学上可接受的盐形式，其中环P（如果存在）为5-7元碳环或杂环，并且环M为5-7元碳环或杂环。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。
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公开(公告)号：US20120041190A1
公开(公告)日：2012-02-16
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： C07D487/06 , C07D513/06 , C07D498/16
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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6.发明申请LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 有权含有LACTAM的化合物及其作为因子XA抑制剂的衍生物公开(公告)号：US20110212930A1
公开(公告)日：2011-09-01
申请号：US13101536
申请日：2011-05-05
申请人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
发明人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
IPC分类号： A61K31/616 , C07D471/04 , A61K31/437 , A61P7/02 , A61P9/10 , A61K31/4365 , A61K31/55 , A61K31/496 , A61K31/513 , C07D401/12 , A61K31/4545 , A61K31/444 , A61K31/4439
CPC分类号： C07D471/04 , A61J1/00 , A61J1/03 , A61J1/05 , A61K31/4365 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/55 , A61K45/06 , B65D81/3216 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/14 , C07D417/14
摘要： The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4 I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了含有式I的化合物及其衍生物：P4-PM-M4 I或其药学上可接受的盐形式，其中环P（如果存在）为5-7元碳环或杂环，且环M为5- 7元碳环或杂环。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。
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7.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20100022506A1
公开(公告)日：2010-01-28
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： A61K31/551 , C07D487/08 , C07D471/08 , A61K31/439 , C07D417/14 , A61K31/541 , C07D413/14 , A61K31/5377
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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8.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20100016316A1
公开(公告)日：2010-01-21
申请号：US12518111
申请日：2007-12-13
申请人： Donald J.P. Pinto
发明人： Donald J.P. Pinto
IPC分类号： A61K31/5377 , C07D403/12 , C07D401/12 , A61K31/41 , A61K31/4439 , A61K31/506 , C07D413/12
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14
摘要： The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) 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： 本发明提供式（I）或（II）的化合物：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，L1，R3，R4，R8a，R11和M如本文所定义。 式（I）或（II）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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9.发明申请LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS 有权含有LACTAM的化合物及其作为因子XA抑制剂的衍生物公开(公告)号：US20100119510A1
公开(公告)日：2010-05-13
申请号：US12691895
申请日：2010-01-22
申请人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
发明人： Donald J.P. Pinto , Mimi L. Quan , Michael J. Orwat , Yun-Long Li , Wei Han , Jennifer X. Qiao , Patrick Y.S. Lam , Stephanie L. Koch
IPC分类号： A61K39/395 , A61K31/727 , A61K31/55 , A61K31/4545 , A61K31/4427 , C07D413/14 , C07D401/14 , A61P7/02 , A61P7/00
CPC分类号： C07D471/04 , A61J1/00 , A61J1/03 , A61J1/05 , A61K31/4365 , A61K31/437 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/513 , A61K31/55 , A61K45/06 , B65D81/3216 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/14 , C07D417/14
摘要： The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4 I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
摘要翻译： 本申请描述了含有式I的化合物及其衍生物：P4-PM-M4 I或其药学上可接受的盐形式，其中环P（如果存在）为5-7元碳环或杂环，且环M为5- 7元碳环或杂环。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。
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10.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20080161373A1
公开(公告)日：2008-07-03
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
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： A61K31/41 , C07D233/64 , A61K31/4164 , A61P9/00 , C07D403/12
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，L 1，M和R 11 >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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