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1.发明授权
公开(公告)号：US6034215A
公开(公告)日：2000-03-07
申请号：US950270
申请日：1997-10-14
申请人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
发明人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
IPC分类号： A61K38/55 , A61K38/00 , A61K38/05 , A61P7/02 , C07K20060101 , C07K5/06 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , A61K38/06
CPC分类号： C07K5/06139 , A61K38/05 , C07K5/06191
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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2.发明授权
公开(公告)号：US5703208A
公开(公告)日：1997-12-30
申请号：US484720
申请日：1995-06-07
申请人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
发明人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
IPC分类号： A61K38/55 , A61K38/00 , A61K38/05 , A61P7/02 , C07K20060101 , C07K5/06 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , A61K38/06 , C07D225/02 , C07F9/06
CPC分类号： C07K5/06139 , A61K38/05 , C07K5/06191
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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公开(公告)号：US5883077A
公开(公告)日：1999-03-16
申请号：US168964
申请日：1993-12-15
CPC分类号： C07K5/06078 , C07K5/0207 , A61K38/00
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor xa in vitro or as a therapeutic agent for the prevention and treatment of conditions characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.
摘要翻译： 公开了与哺乳动物因子Xa具有活性的新型化合物，其盐和与其相关的组合物。 新化合物包括具有显着效力和特异性的肽醛类似物，作为哺乳动物因子Xa的抑制剂被进一步公开。 这些化合物被认为可用作体外因子xa的抑制剂或作为预防和治疗哺乳动物异常血栓形成特征的治疗剂。 还公开了可用于制备新化合物的中间体。
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公开(公告)号：US5739112A
公开(公告)日：1998-04-14
申请号：US465115
申请日：1995-06-05
CPC分类号： C07K5/06078 , C07K5/0207 , A61K38/00
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor Xa in vitro or as a therapeutic agent for the prevention and treatment of conditions: characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.
摘要翻译： 公开了与哺乳动物因子Xa具有活性的新型化合物，其盐和与其相关的组合物。 新化合物包括具有显着效力和特异性的肽醛类似物，作为哺乳动物因子Xa的抑制剂被进一步公开。 这些化合物被认为可用作体外因子Xa的抑制剂或作为用于预防和治疗哺乳动物异常血栓形成的病症的治疗剂。 还公开了可用于制备新化合物的中间体。
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公开(公告)号：US06342504B1
公开(公告)日：2002-01-29
申请号：US09194855
申请日：1999-12-21
申请人： Terence Kevin Brunck , Susan Y. Tamura , Joseph Edward Semple , Robert John Ardecky , Yu Ge , William Charles Ripka
发明人： Terence Kevin Brunck , Susan Y. Tamura , Joseph Edward Semple , Robert John Ardecky , Yu Ge , William Charles Ripka
IPC分类号： A61K31505
CPC分类号： C07K5/06191 , A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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