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91. 发明授权

US06211154B1 Ketoheterocyclic inhibitors of factor Xa 失效
标题翻译：因子Xa的酮基杂环抑制剂
公开(公告)号：US06211154B1
公开(公告)日：2001-04-03
申请号：US08480491
申请日：1995-06-07
申请人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
发明人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
IPC分类号： C07K508
CPC分类号： C07K5/06095 , A61K38/00
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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。该化合物在体外或体内可用于预防或治疗凝血障碍。

92. 发明授权

US06197748B1 Ketoheterocyclic inhibitors of factor Xa 失效
标题翻译：因子Xa的酮基杂环抑制剂
公开(公告)号：US06197748B1
公开(公告)日：2001-03-06
申请号：US09077002
申请日：1998-05-15
申请人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
发明人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
IPC分类号： A61K3700
CPC分类号： C07K5/06 , A61K38/00 , C07K5/06078 , C07K5/06095 , C07K5/06139
摘要： Ketoheterocyclic compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are usefull in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译：公开了具有针对哺乳动物因子Xa的活性的酮类杂环化合物，其盐和与其相关的组合物。这些化合物在体外或体内是有用的用于预防或治疗凝血障碍。

93. 发明授权

US6043212A Recombinant C140 receptor, its agonists and antagonists, and nucleic acids encoding the receptor 失效
公开(公告)号：US6043212A
公开(公告)日：2000-03-28
申请号：US474410
申请日：1995-06-07
申请人： Johan Sundelin , Robert M. Scarborough
发明人： Johan Sundelin , Robert M. Scarborough
IPC分类号： A61K38/00 , A61K48/00 , C07K7/06 , C07K7/08 , C07K14/72 , C12N15/12 , A61K38/03 , A61K38/08 , A61K38/10
CPC分类号： C07K7/06 , C07K14/705 , C07K14/723 , C07K7/08 , A61K38/00 , A61K48/00 , G01N2333/726 , G01N2500/00
摘要： Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.

94. 发明授权

US06022861A Ketoheterocyclic inhibitors of factor Xa 失效
公开(公告)号：US06022861A
公开(公告)日：2000-02-08
申请号：US486213
申请日：1995-06-07
申请人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
发明人： Robert M. Scarborough , Charles K. Marlowe , Bing-Yan Zhu
IPC分类号： A61K38/00 , C07K5/068
CPC分类号： C07K5/06086 , A61K38/00
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

95. 发明授权

US5935926A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5935926A
公开(公告)日：1999-08-10
申请号：US482275
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
摘要： An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formulaR.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO--wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C);and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatomare prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
摘要翻译：描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂（PAI）的测定法。使用该测定，完成了广泛的蛇毒样品中PAIs的鉴定和表征。描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。另外，缺乏Arg-Gly-Asp（RGD）粘附序列但含有K * - （G / Sar）-D的PAI，其中K *是式R 12 N（CH 2）4 CHNHCO-的修饰的赖氨酰残基，其中每个R 1独立地为H ，烷基（1-6C）或至多一个R1是R2-C = NR3，其中R2是H，烷基（1-6C），苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（1-6C ）和R 3是H，烷基（1-6C），苯基或苄基，或者R 2 -C = NR 3是选自以下的基团：其中m是2-3的整数，并且每个R 5独立地是H或烷基（1-6C）; 并且其中一个或两个（CH 2）可以被O或S替代，条件是所述O或S不与另一个杂原子相邻，并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。

96. 发明授权

US5851839A Platelet aggregation inhibitors 失效
公开(公告)号：US5851839A
公开(公告)日：1998-12-22
申请号：US465551
申请日：1995-06-05
申请人： Robert M. Scarborough
发明人： Robert M. Scarborough
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , G01N33/543
CPC分类号： C07K14/46 , A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/75 , C07K14/755 , C07K14/78
摘要： Peptides useful in inhibiting platelet aggregation are disclosed. These peptides contain the binding sequence Har-G-D and are disulfide-bridged cyclic compounds.

97. 发明授权

US5759999A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5759999A
公开(公告)日：1998-06-02
申请号：US482280
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
摘要： An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formula R.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO-- wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C); and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
摘要翻译：描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂（PAI）的测定法。使用该测定，完成了广泛的蛇毒样品中PAIs的鉴定和表征。描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。另外，缺乏Arg-Gly-Asp（RGD）粘附序列但含有K * - （G / Sar）-D的PAI，其中K *是式R 12 N（CH 2）4 CHNHCO-的修饰的赖氨酰残基，其中每个R 1独立地为H ，烷基（1-6C）或至多一个R1是R2-C = NR3，其中R2是H，烷基（1-6C），苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（1-6C ）和R 3是H，烷基（1-6C），苯基或苄基，或者R 2 -C = NR 3是选自下组的基团：A 5 R 5独立地是H或烷基（1-6C）; 并且其中一个或两个（CH 2）可以被O或S替代，条件是所述O或S不与另一个杂原子相邻，并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。

98. 发明授权

US5688768A Recombinant thrombin receptor and related pharmaceuticals 失效
标题翻译：重组凝血酶受体和相关药物
公开(公告)号：US5688768A
公开(公告)日：1997-11-18
申请号：US789184
申请日：1991-11-07
申请人： Shaun R. Coughlin , Robert M. Scarborough
发明人： Shaun R. Coughlin , Robert M. Scarborough
IPC分类号： A61K38/00 , A61K39/00 , A61K39/395 , A61K49/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P43/00 , C07K7/02 , C07K7/06 , C07K14/705 , C07K16/00 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/74 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12R1/19 , G01N33/53 , A61K36/00 , C07K7/08 , C07K7/10
CPC分类号： C12N9/6429 , C07K14/705 , C07K16/28 , C12Y304/21005 , A61K38/00 , A61K39/00 , Y10S530/837
摘要： The DNA encoding the cell surface receptor for thrombin has been cloned and sequenced. The availability of this DNA permits the recombinant production of thrombin receptor which can be produced at cell surfaces and is useful in assay systems both for the detection of thrombin and for the evaluation of candidate thrombin agonists and antagonists. Further, the elucidation of the structure of the thrombin receptor permits the design of agonist and antagonist compounds which are useful diagnostically and therapeutically. The availability of the thrombin receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof which are also useful diagnostically or therapeutically.
摘要翻译：编码凝血酶细胞表面受体的DNA已被克隆并测序。该DNA的可用性允许重组产生可在细胞表面产生的凝血酶受体，并且可用于检测凝血酶和用于评价候选凝血酶激动剂和拮抗剂的测定系统。此外，阐明凝血酶受体的结构允许设计在诊断和治疗上有用的激动剂和拮抗剂化合物。凝血酶受体的可用性还允许产生与受体本身或其特异性区域特异性免疫反应的抗体，其在诊断或治疗上也是有用的。

99. 发明授权

US5385840A DNA encoding analogs of human alveolar surfactant protein SP-5 失效
标题翻译：编码人肺泡表面活性蛋白SP-5类似物的DNA
公开(公告)号：US5385840A
公开(公告)日：1995-01-31
申请号：US965745
申请日：1992-10-23
申请人： Bradley J. Benson , Robert T. White , James W. Schilling, Jr. , Douglas I. Buckley , Robert M. Scarborough
发明人： Bradley J. Benson , Robert T. White , James W. Schilling, Jr. , Douglas I. Buckley , Robert M. Scarborough
IPC分类号： A61K38/00 , C07K14/785 , C12N1/21 , C12N5/18 , C12N15/12 , C12N15/70 , C12N15/85 , C12P21/04 , C12N5/10 , C12N15/63
CPC分类号： C12N15/70 , C07K14/785 , C12N15/85 , A61K38/00 , C12N2830/002 , C12N2830/30 , C12N2830/55 , C12N2830/60
摘要： Various specific human SP-18 and human SP-5 derived peptides have alveolar surfactant protein (ASP) activity. These peptides are prepared using synthetic methods or by recombinant techniques.
摘要翻译：各种特异性人SP-18和人SP-5衍生肽具有肺泡表面活性蛋白（ASP）活性。使用合成方法或通过重组技术制备这些肽。

100. 发明授权

US08349873B2 Factor XA inhibitors 有权
标题翻译：因子XA抑制剂
公开(公告)号：US08349873B2
公开(公告)日：2013-01-08
申请号：US13270170
申请日：2011-10-10
申请人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough, legal representative
发明人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough
IPC分类号： A61K31/4412
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

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