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公开(公告)号：US20050154204A1
公开(公告)日：2005-07-14
申请号：US10959909
申请日：2004-10-05
申请人： Bing-Yan Zhu , Erick Goldman , Wenrong Huang , Penglie Zhang
发明人： Bing-Yan Zhu , Erick Goldman , Wenrong Huang , Penglie Zhang
IPC分类号： A61K20060101 , C07D213/72 , C07D213/75 , C07D401/12 , C07D43/14 , C07D43/02
CPC分类号： C07D213/75 , C04B35/632 , C07D401/12
摘要： Thioether-substituted benzamide compounds having the formula: are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding.
摘要翻译： 提供了具有下式的硫醚取代的苯甲酰胺化合物，其表现出特异强的抑制因子Xa与弱hERG结合的组合。
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公开(公告)号：US06218382B1
公开(公告)日：2001-04-17
申请号：US09132258
申请日：1998-08-11
申请人： Bing-Yan Zhu , Robert Scarborough
发明人： Bing-Yan Zhu , Robert Scarborough
IPC分类号： A61K3155
CPC分类号： C07K5/06139 , A61K38/00
摘要： Novel 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。 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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公开(公告)号：US06211154B1
公开(公告)日：2001-04-03
申请号：US08480491
申请日：1995-06-07
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。
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公开(公告)号：US06197748B1
公开(公告)日：2001-03-06
申请号：US09077002
申请日：1998-05-15
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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公开(公告)号：US06022861A
公开(公告)日：2000-02-08
申请号：US486213
申请日：1995-06-07
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.
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公开(公告)号：US20120190665A1
公开(公告)日：2012-07-26
申请号：US13382145
申请日：2010-07-02
申请人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
发明人： Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
IPC分类号： A61K31/519 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P7/00 , A61P1/00 , A61P17/06 , A61P17/00 , A61P19/02 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
摘要翻译： 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号：US20100234352A1
公开(公告)日：2010-09-16
申请号：US12697135
申请日：2010-01-29
申请人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
发明人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
IPC分类号： A61K31/55 , A61K31/497 , A61K31/513 , A61K31/501 , A61K31/551 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/4178 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/538 , A61K31/4709 , A61P7/02 , A61P9/00
CPC分类号： C07D409/14 , C07D333/38 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , 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 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：US07727981B2
公开(公告)日：2010-06-01
申请号：US11924480
申请日：2007-10-25
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： C07D413/14 , A61K31/4439
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：US07696352B2
公开(公告)日：2010-04-13
申请号：US11620615
申请日：2007-01-05
申请人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough , Carroll Anna Crew Scarborough, legal representative
发明人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
IPC分类号： C07D409/14 , C07D401/14 , C07D409/12 , A61K31/4436
CPC分类号： C07D409/14 , C07D333/38 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , 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 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：US07521470B2
公开(公告)日：2009-04-21
申请号：US11158274
申请日：2005-06-20
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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