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91. 发明授权

US07312235B2 Benzamide inhibitors of factor Xa 有权
标题翻译：因子Xa的苯甲酰胺抑制剂
公开(公告)号：US07312235B2
公开(公告)日：2007-12-25
申请号：US10115135
申请日：2002-04-01
申请人： Bing-Yan Zhu , Penglie Zhang , Erick A. Goldman , Zhaozhong Jon Jia , Shawn Bauer , Wenrong Huang , John Woolfrey , Robert M. Scarborough
发明人： Bing-Yan Zhu , Penglie Zhang , Erick A. Goldman , Zhaozhong Jon Jia , Shawn Bauer , Wenrong Huang , John Woolfrey , Robert M. Scarborough
IPC分类号： A61K31/497 , A61K31/445 , A61K31/44 , A61K31/00
CPC分类号： C07D213/75 , C07C237/42 , C07C255/57 , C07C257/18 , C07D205/04 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/62 , C07D233/22 , C07D233/64 , C07D295/13 , C07D295/195 , C07D307/54 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , G02B6/2746
摘要： Novel benzamide 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具有活性的新型苯甲酰胺化合物，其盐和与其有关的组合物。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

US07285565B2 Benzamides and related inhibitors of factor Xa 有权
标题翻译：苯甲酰胺和相关因子Xa抑制剂
公开(公告)号：US07285565B2
公开(公告)日：2007-10-23
申请号：US11035767
申请日：2005-01-14
申请人： Bing-Yan Zhu , Penglie Zhang , Lingyan Wang , Wenrong Huang , Erick A. Goldman , Wenhao Li , Jingmei Zuckett , Yonghong Song , Robert M. Scarborough
发明人： Bing-Yan Zhu , Penglie Zhang , Lingyan Wang , Wenrong Huang , Erick A. Goldman , Wenhao Li , Jingmei Zuckett , Yonghong Song , Robert M. Scarborough
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C07D213/75 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Novel benzamide 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有活性的新型苯甲酰胺化合物，其盐和与其有关的组合物。该化合物在体外或体内可用于预防或治疗凝血障碍。

93. 发明授权

US07179790B2 Brain natriuretic peptide 有权
标题翻译：脑利钠肽
公开(公告)号：US07179790B2
公开(公告)日：2007-02-20
申请号：US11234424
申请日：2005-09-23
申请人： J. Jeffrey Seilhamer , John A. Lewicki , Robert M. Scarborough , J. Gordon Porter
发明人： J. Jeffrey Seilhamer , John A. Lewicki , Robert M. Scarborough , J. Gordon Porter
IPC分类号： A61K38/00
CPC分类号： C12P21/02 , A61K38/00 , C07K14/58 , C07K14/582 , C07K16/241 , C07K16/2803 , C07K2317/622 , G01N33/74
摘要： Peptides comprising the effective portion of human brain natriuretic peptide are provided in pharmaceutical compositions and methods to effect vasodilation and/or natriuresis.
摘要翻译：包含人脑钠肽的有效部分的肽在药物组合物和方法中提供以实现血管舒张和/或利尿。

94. 发明授权

US06974861B2 Pharmaceutical compositions and methods using natriuretic peptides 失效
公开(公告)号：US06974861B2
公开(公告)日：2005-12-13
申请号：US10402021
申请日：2003-03-27
申请人： J. Jeffrey Seilhamer , John Lewicki , Robert M. Scarborough , J. Gordon Porter
发明人： J. Jeffrey Seilhamer , John Lewicki , Robert M. Scarborough , J. Gordon Porter
IPC分类号： C12N15/09 , A61K38/00 , A61K38/22 , A61P9/08 , A61P9/12 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/12 , C12N15/16 , C12P21/02 , C12R1/19 , C07K17/00
CPC分类号： C12P21/02 , A61K38/00 , C07K14/58 , C07K14/582 , C07K16/241 , C07K16/2803 , C07K2317/622 , G01N33/74
摘要： The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically. The invention peptides have the formula: R1-Cys-Phe-Gly-Arg- Arg/ - Leu/ -Asp-Arg- Lys Met (1) Ile- Gly/ -Ser- Leu/ -Ser-Gly-Leu-Gly-Cys-R-2 Ser Ser wherein R1 is selected from the group consisting of: (H); Gly-; Ser-Gly-; Asp/ Lys/ -Ser-Gly-; Gly Arg/ Asp/ His/ - Lys/ -Ser-Gly-; Gln Gly Arg/ Asp/ Met/ - His/ - Lys/ -Ser-Gly-; Val Gln Gly Arg/ Asp/ Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Pro-Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly Arg/ Asp/ Ser-Pro-Lys- Thr/ - Met/ - His/ - Lys/ -Ser-Gly-; Met Val Gln Gly or a 10- to 109-amino acid sequence shown as the native upstream sequence for porcine, canine or human BNP in FIG. 8, or a composite thereof; R2 is (OH), NH2, or NR′R″ wherein R′ and R″ are independently lower alkyl (1-4C) or is Asn/ Lys Asn/ -Val Lys Asn/ -Val-Leu Lys Asn/ -Val-Leu-Arg Lys Asn/ -Val-Leu-Arg- Arg/ Lys Lys Asn/ -Val-Leu-Arg- Arg/ - Tyr/ Lys Lys His or the amides (NH2 or NR′R″) thereof, with the proviso that if formula (1) is R1-Cys-Phe-Gly-Arg-Arg-Leu-Asp-Arg- Ile-Gly-Ser-Leu-Ser-Gly-Leu-Gly-Cys-R2 and R1 is Asp-Ser-Gly-, R2 cannot be Asn-Val-Leu-Arg-Arg-Tyr. The peptides of the invention can be formulated into pharmaceutical compositions and used to treat conditions associated with high extracellular fluid levels, especially congestive heart failure.

95. 发明授权

US06693109B2 Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation 失效
标题翻译：螺环化合物作为纤维蛋白原依赖性血小板聚集的抑制剂
公开(公告)号：US06693109B2
公开(公告)日：2004-02-17
申请号：US10354265
申请日：2003-01-29
申请人： Matthew J. Fisher , Joseph A. Jakubowski , John J. Masters , Jeffrey T. Mullaney , Michael Paal , Gerd Ruhter , Kenneth J. Ruterbories , Robert M. Scarborough , Theo Schotten , Wolfgang Stenzel
发明人： Matthew J. Fisher , Joseph A. Jakubowski , John J. Masters , Jeffrey T. Mullaney , Michael Paal , Gerd Ruhter , Kenneth J. Ruterbories , Robert M. Scarborough , Theo Schotten , Wolfgang Stenzel
IPC分类号： C07D22120
CPC分类号： C07D221/20 , A61K31/423 , A61K31/437 , C07D263/52 , C07D471/10
摘要： This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
摘要翻译：本发明涉及用碱性和酸性官能团取代的某些螺环化合物，其可用于抑制血小板聚集。

96. 发明授权

US06667306B1 Platelet ADP receptor inhibitors 失效
标题翻译：血小板ADP受体抑制剂
公开(公告)号：US06667306B1
公开(公告)日：2003-12-23
申请号：US09226103
申请日：1999-01-07
申请人： Alan M. Laibelman , Hans-Michael Jantzen , Pamela B. Conley , Larry J. Fretto , Robert M. Scarborough
发明人： Alan M. Laibelman , Hans-Michael Jantzen , Pamela B. Conley , Larry J. Fretto , Robert M. Scarborough
IPC分类号： C07D51314
CPC分类号： C07D513/04
摘要： The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.
摘要翻译：本发明涉及含有作为有效血小板ADP受体抑制剂的稠合杂环体系的式（I）化合物：式（I）中W是碳或氮，其中至少一个W是碳; Y是氮，氧或硫。包括药学上可接受的盐的这些化合物可用于预防和/或治疗心血管疾病，特别是血栓形成相关的各种药物组合物。

97. 发明授权

US06552079B2 Integrin antagonists 失效
标题翻译：整合素拮抗剂
公开(公告)号：US06552079B2
公开(公告)日：2003-04-22
申请号：US09855448
申请日：2001-05-15
申请人： Robert M. Scarborough , Mark Smyth , Ting Su , Matthew J. Fisher , Joseph A. Jakubowski , John J. Masters , Jeffry Bernard Franciskovich
发明人： Robert M. Scarborough , Mark Smyth , Ting Su , Matthew J. Fisher , Joseph A. Jakubowski , John J. Masters , Jeffry Bernard Franciskovich
IPC分类号： C07C31104
CPC分类号： C07D211/62 , C07C311/06 , C07C311/19 , C07C2601/14
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.
摘要翻译：公开了与哺乳动物整联蛋白有关的新型化合物，其盐和与其有关的组合物。该化合物在体外或体内可用于预防或治疗血栓形成或再狭窄病症。

98. 发明授权

US06297026B1 Nucleic acids encoding the C140 receptor 失效
标题翻译：编码C140受体的核酸
公开(公告)号：US06297026B1
公开(公告)日：2001-10-02
申请号：US08486673
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： C12N1512
CPC分类号： C07K7/06 , A61K38/00 , A61K48/00 , C07K7/08 , C07K14/705 , C07K14/723 , 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.
摘要翻译：编码C140细胞表面受体的核酸分子已被克隆并测序。 C140受体DNA的可用性允许重组产生可在细胞表面（包括卵母细胞）上产生的C140受体。核酸分子可用于检测影响C140受体活性的物质，即受体激动剂或拮抗剂。此外，阐明C140受体的结构允许设计可用于此类测定中的激动剂和拮抗剂化合物。 C140受体的可用性还允许产生与C140受体的一个或多个抗原表位特异性免疫反应的抗体。

99. 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。

100. 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。

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