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公开(公告)号：US4935492A
公开(公告)日：1990-06-19
申请号：US174739
申请日：1988-03-29
IPC分类号： A61K38/00 , A61K38/22 , A61P7/10 , A61P9/08 , C07K1/02 , C07K1/04 , C07K1/113 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58
摘要： Compounds and compositions comprising cyclic synthetic analogs of Atrial Natriuretic Peptides are provided, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.
摘要翻译： 提供包含心房钠尿肽的环合成类似物的化合物和组合物，以及其生产和用作利尿剂，利尿剂和/或血管扩张剂的方法，或作为这些有用化合物或天然心房钠尿肽的中间体或调节剂。
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公开(公告)号：US08524721B2
公开(公告)日：2013-09-03
申请号：US13270193
申请日：2011-10-10
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-Maguire
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-Maguire
IPC分类号： C07D521/00 , C07D409/12 , C07D209/48 , A61K31/4035 , A61P7/02
CPC分类号： C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要： Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译： 式（I）和（VIII）的新型化合物，其更具体地包括作为有效血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I）至（VIII）化合物或其药学上可接受的盐的步骤。
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公开(公告)号：US08518977B2
公开(公告)日：2013-08-27
申请号：US13247937
申请日：2011-09-28
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： C07D213/75 , A61K31/44
CPC分类号： A61K31/44 , A61K9/20 , A61K9/2013 , A61K9/2054 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K31/616 , A61K45/06 , A61K2201/094 , C07C237/42 , C07C255/60 , C07C257/18 , C07C259/18 , C07C311/16 , C07C311/46 , C07C317/40 , C07C317/44 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D295/125 , C07D333/38 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译： 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。
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公开(公告)号：US08153670B2
公开(公告)日：2012-04-10
申请号：US12348879
申请日：2009-01-05
申请人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
发明人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
IPC分类号： A61K31/415 , A61K31/4164 , A61K31/4192 , C07D249/04 , C07D233/66 , C07D207/34
CPC分类号： C07D413/14 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, 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： 本发明涉及由式I表示的化合物及其作为因子Xa抑制剂的药学上可接受的盐，溶剂合物，水合物和前药。 本发明还涉及用于制备这种化合物的中间体，含有这些化合物的药物组合物，预防或治疗多种不想要的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。
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65.发明申请INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR 审中-公开直接作用和可逆的P2Y12抑制剂的口服和口服剂量公开(公告)号：US20120009172A1
公开(公告)日：2012-01-12
申请号：US13235305
申请日：2011-09-16
申请人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Carroll Anna Crew Scarborough , Wolin Huang
发明人： Daniel D. Gretler , Pamela B. Conley , Patrick Andre , Athiwat Hutchaleelaha , David R. Phillips , Anjali Pandey , Robert M. Scarborough , Carroll Anna Crew Scarborough , Wolin Huang
IPC分类号： A61K38/45 , A61K38/48 , A61P9/00 , A61K31/517 , C07D409/12 , A61P7/00 , A61K38/46 , A61K31/60
CPC分类号： A61K31/517 , A61K31/216 , A61K2300/00
摘要： The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: alone or in combination with a second agent which can be aspirin or a thrombolytic agent.
摘要翻译： 本发明提供了通过施用下式的化合物单独或与可以是阿司匹林或溶栓剂的第二药剂组合来快速和可逆地抑制有需要的人受试者血小板聚集的方法和组合物。
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公开(公告)号：US08063077B2
公开(公告)日：2011-11-22
申请号：US12777956
申请日：2010-05-11
申请人： Yonghong Song , Zhaozhong J. Jia , Robert M. Scarborough , Carroll Scarborough, legal representative , Anjali Pandey
IPC分类号： A61K31/4412 , C07D401/14
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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公开(公告)号：US08022071B2
公开(公告)日：2011-09-20
申请号：US11959341
申请日：2007-12-18
申请人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
发明人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
IPC分类号： A61K31/5377 , A61K31/517
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
摘要翻译： 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化症。
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公开(公告)号：US20110160196A1
公开(公告)日：2011-06-30
申请号：US12976602
申请日：2010-12-22
IPC分类号： A61K31/4439 , C07D409/14 , C12N9/99 , C07D413/14 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/496 , C07D417/14 , A61K31/541 , A61P7/02 , A61P9/10
CPC分类号： C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，酯或前药，其是因子Xa的抑制剂。 本发明还涉及用于制备这些化合物的中间体，含有这些化合物的药物组合物，预防或治疗特征在于不想要的血栓形成的某些病症的方法以及抑制血液样品凝固的方法。
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69.发明申请公开(公告)号：US20110098247A1
公开(公告)日：2011-04-28
申请号：US12912367
申请日：2010-10-26
IPC分类号： A61K31/727 , A61K31/517 , A61K31/5355 , A61K31/4725 , A61P7/02
CPC分类号： C07D409/12 , C07D239/96 , C07D265/22 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
摘要翻译： 提供式I化合物：其中Ar 1和Ar 2是取代的芳环，且L 1和L 2是独立的二价连接基团。 该化合物可用作血小板ADP受体抑制剂，用于治疗血栓形成和降低患者中二次缺血事件的可能性和/或严重性。
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公开(公告)号：US20100113468A1
公开(公告)日：2010-05-06
申请号：US12471280
申请日：2009-05-22
申请人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
发明人： Anjali Pandey , Robert M. Scarborough , Kenji Matsuno , Michio Ichimura , Yuji Nomoto , Shinichi Ide , Eiji Tsukuda , Junko Sasaki , Shoji Oda
IPC分类号： A61K31/497
CPC分类号： C07D239/94 , A61K31/517 , C07D401/12 , C07D403/12
摘要： The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
摘要翻译： 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化症。
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