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公开(公告)号：US20050186198A1
公开(公告)日：2005-08-25
申请号：US11088511
申请日：2005-03-24
申请人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
IPC分类号： C07D333/34 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51 , A61K38/48 , A61K31/445 , A61K31/54 , A61K31/60
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
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2.发明授权Nonpeptidyl integrin inhibitors having specificity for the GPII.sub.b III.sub.a 失效对GPIIbIIIa具有特异性的非肽基整合素抑制剂
公开(公告)号：US5674865A
公开(公告)日：1997-10-07
申请号：US451794
申请日：1995-05-26
申请人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
发明人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
IPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14 , A61K31/55
CPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14
摘要： A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： 提供作为非肽基血小板聚集抑制剂的苯并二氮二酮衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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公开(公告)号：US20070037813A1
公开(公告)日：2007-02-15
申请号：US11537482
申请日：2006-09-29
申请人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
IPC分类号： A61K31/50 , A61K31/44 , A61K31/165 , C07D237/02
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US5705890A
公开(公告)日：1998-01-06
申请号：US313069
申请日：1994-09-26
申请人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
发明人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
IPC分类号： A61K31/55 , A61P7/02 , C07D487/04 , C07D498/04 , C07D507/02 , C07D513/04
CPC分类号： C07D487/04
摘要： A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： PCT No.PCT / US94 / 07989第 371日期：1994年9月26日 102（e）1994年9月26日PCT 1994年7月15日PCT公布。 第WO95 / 04057号公报 日期1995年2月9日提供作为非肽基血小板聚集抑制剂的三苯并二氮杂衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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5.发明授权Nonpeptidyl integrin inhibitors having specificity for the GPII.sub.b III.sub.a receptor 失效对GPIIbIIIa受体具有特异性的非肽基整联蛋白抑制剂
公开(公告)号：US5565449A
公开(公告)日：1996-10-15
申请号：US452479
申请日：1995-05-26
申请人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
发明人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
IPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14 , A61K31/55
CPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14
摘要： A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： 提供作为非肽基血小板聚集抑制剂的苯并二氮二酮衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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公开(公告)号：US5493020A
公开(公告)日：1996-02-20
申请号：US99019
申请日：1993-07-29
申请人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
发明人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
IPC分类号： A61K31/55 , A61P7/02 , C07D487/04 , C07D498/04 , C07D507/02 , C07D513/04
CPC分类号： C07D487/04
摘要： A trycylic benzodiazepine derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： 提供作为非肽基血小板聚集抑制剂的三环苯并二氮杂衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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公开(公告)号：US5716951A
公开(公告)日：1998-02-10
申请号：US438143
申请日：1995-05-08
申请人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
发明人： Brent K. Blackburn , Kirk Robarge , Todd C. Somers
IPC分类号： A61K31/55 , A61P7/02 , C07D487/04 , C07D498/04 , C07D507/02 , C07D513/04 , C07D243/14
CPC分类号： C07D487/04
摘要： A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： 提供作为非肽基血小板聚集抑制剂的三苯并二氮杂衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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公开(公告)号：US20140066453A1
公开(公告)日：2014-03-06
申请号：US14011501
申请日：2013-08-27
申请人： Jim Blake , Huifen Chen , Mark Chicarelli , John Gaudino , Lewis Gazzard , Sam Kintz , Pete Mohr , Kirk Robarge , Jacob Schwarz , Aihe Zhou
发明人： Jim Blake , Huifen Chen , Mark Chicarelli , John Gaudino , Lewis Gazzard , Sam Kintz , Pete Mohr , Kirk Robarge , Jacob Schwarz , Aihe Zhou
IPC分类号： C07D471/04 , C07D401/14 , C07D217/22 , C07D401/12 , C07D405/14 , C07D405/12
CPC分类号： C07D405/14 , C07D217/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D471/04
摘要： Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译： 具有式I的化合物，其中本文定义的R2，X和Z是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。
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公开(公告)号：US07109326B2
公开(公告)日：2006-09-19
申请号：US10854388
申请日：2004-05-25
申请人： Brent Blackburn , Alan G. Olivero , Kirk Robarge
发明人： Brent Blackburn , Alan G. Olivero , Kirk Robarge
IPC分类号： C07D243/24
CPC分类号： C07D223/16 , C07D243/14 , C07D243/24
摘要： Halo-alkoxycarbonyl derivatives are provided as prodrug moieties for pharmaceutical agents containing a basic or polar nitrogen containing functionality. The prodrugs are provided as pharmaceutical compositions as well as in methods of treatment.
摘要翻译： 提供卤代 - 烷氧基羰基衍生物作为含有碱性或极性含氮官能团的药物的前药部分。 前药作为药物组合物以及治疗方法提供。
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10.发明授权Nonpeptidyl integrin inhibitors having specificity for the GPII.sub.b III.sub.a receptor 失效对GPIIbIIIa受体具有特异性的非肽基整联蛋白抑制剂
公开(公告)号：US5674863A
公开(公告)日：1997-10-07
申请号：US451849
申请日：1995-05-26
申请人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
发明人： Brent Blackburn , Peter Barker , Thomas Gadek , Robert McDowell , Lawrence McGee , Todd Somers , Rob Webb , Kirk Robarge
IPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14 , C07D285/36 , A61K31/55 , C07D513/04
CPC分类号： C07D223/16 , C07D243/10 , C07D243/14 , C07D267/14
摘要： A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
摘要翻译： 提供作为非肽基血小板聚集抑制剂的苯并二氮二酮衍生物。 该抑制剂有效地抑制纤维蛋白原与GPIIbIIIa受体的结合，并且提供在用于治疗阻断血小板聚集的疾病的治疗组合物中。 这些非肽基抑制剂与溶血栓剂和抗凝剂组合提供。
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