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公开(公告)号：US08524907B2
公开(公告)日：2013-09-03
申请号：US12446954
申请日：2007-11-01
申请人： Robert M. Scarborough , James P Kanter , Keiko Sujino , Sharique Sami Zuberi , Carroll Scarborough
IPC分类号： C07D213/74 , C07D215/38
CPC分类号： C07D213/90 , C07D213/75
摘要： Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.
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公开(公告)号：US20130172310A1
公开(公告)日：2013-07-04
申请号：US13612597
申请日：2012-09-12
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 , C07D401/12
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.
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公开(公告)号：US20120178733A1
公开(公告)日：2012-07-12
申请号：US13213927
申请日：2011-08-19
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： A61K31/422 , C07D413/14 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K31/4545 , A61K31/4439 , A61K31/496 , A61K31/506 , C07D417/14 , A61K31/541 , A61K31/553 , A61K31/551 , C07D409/14 , C07D409/12 , A61K31/4192 , C07D417/12 , A61K31/427 , A61K31/4178 , A61K31/4709 , A61P9/00 , A61P9/10 , A01N1/02 , A61P7/02 , C07D413/12
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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公开(公告)号：US08067428B2
公开(公告)日：2011-11-29
申请号：US12559389
申请日：2009-09-14
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-McGuire
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-McGuire
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) to (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）至（VIII）的新型化合物，其更具体地包括作为有效的血小板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，磺酰氰基胍衍生物，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：US07678790B2
公开(公告)日：2010-03-16
申请号：US11286259
申请日：2005-11-23
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D417/12 , C07D411/12 , C07D417/14 , C07D401/04 , A61K31/40 , A61K31/38 , A61K31/44 , A61K31/425 , A61K31/495 , A61K31/55
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), 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)-(VI), or a pharmaceutically acceptable salt thereof.
摘要翻译： 式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板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） - （VI）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：US07342013B2
公开(公告)日：2008-03-11
申请号：US11442060
申请日：2006-05-26
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： C07D401/02 , 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.
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公开(公告)号：US07294635B2
公开(公告)日：2007-11-13
申请号：US10956006
申请日：2004-09-29
申请人： Robert M. Scarborough , Kim A. Kane-MaGuire , Charles K. Marlowe , Mark S. Smyth , Xiaoming Zhang
发明人： Robert M. Scarborough , Kim A. Kane-MaGuire , Charles K. Marlowe , Mark S. Smyth , Xiaoming Zhang
IPC分类号： C07D407/04 , A61K31/506 , A61K31/4709
CPC分类号： C07D409/14 , C07D217/24 , C07D401/04 , C07D409/12
摘要： Isoquinolinone compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译： 提供了可用于抑制ADP-血小板聚集的异喹啉酮化合物，特别是在治疗血栓形成和血栓形成相关病症或病症中。
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公开(公告)号：US07119182B1
公开(公告)日：2006-10-10
申请号：US08481896
申请日：1995-06-07
CPC分类号： C07K14/705
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.
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公开(公告)号：US07022731B2
公开(公告)日：2006-04-04
申请号：US10759396
申请日：2004-01-15
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D409/12 , A61K31/4025 , A61P7/02
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), 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)–(VI), or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US06906063B2
公开(公告)日：2005-06-14
申请号：US09920325
申请日：2001-08-02
IPC分类号： C07D239/96 , A61K31/16 , A61K31/175 , A61K31/381 , A61K31/4196 , A61K31/4725 , A61K31/519 , A61K31/54 , A61K31/64 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/14 , A61P43/00 , C07D209/48 , C07D213/70 , C07D239/22 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D521/00 , A61K31/40 , C07D411/12 , C07D417/14
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) to (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）至（VIII）的新型化合物，其更具体地包括作为有效的血小板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，磺酰氰基胍衍生物，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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