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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: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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公开(公告)号:US20070259924A1
公开(公告)日:2007-11-08
申请号:US11744735
申请日:2007-05-04
IPC分类号: A61K31/4439 , A61K31/4178 , A61K31/4172 , C07D403/02 , C07D409/02 , C07D405/02
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以及抑制血液样品凝固的方法。
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公开(公告)号:US20120088795A1
公开(公告)日:2012-04-12
申请号:US13270170
申请日:2011-10-10
IPC分类号: A61K31/4439 , A61P7/02 , C12N9/99
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:US20090030045A1
公开(公告)日:2009-01-29
申请号:US12166944
申请日:2008-07-02
IPC分类号: A61K31/4439 , C07D409/14 , A61P7/00 , A61P7/02
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: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
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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公开(公告)号:US20080293704A1
公开(公告)日:2008-11-27
申请号:US11969758
申请日:2008-01-04
IPC分类号: A61K31/4439 , C07D409/14 , A61K31/4545 , A61K31/541 , A61P7/00 , A01N1/00 , A61K31/496 , C07D279/12
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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公开(公告)号:US08063058B2
公开(公告)日:2011-11-22
申请号:US12386525
申请日:2009-04-16
申请人: Zhaozhong J. Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
发明人: Zhaozhong J. Jia , Chandrasekar Venkataramani , Wolin Huang , Mukund Mehrotra , Yonghong Song , Qing Xu , Shawn M. Bauer , Jack W. Rose , Brian Kane , Anjali Pandey
IPC分类号: A01N43/54 , A61K31/505 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号: A61K31/506 , C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
摘要翻译: 本发明涉及作为syk激酶抑制剂的式I-V化合物及其互变异构体或其药学上可接受的盐,酯和前体药物。 本发明还涉及用于制备这种化合物的中间体,这种化合物的制备,含有这种化合物的药物组合物,抑制syk激酶活性的方法,抑制血小板聚集的方法,以及预防或治疗数字的方法 至少部分通过syk激酶活性介导的病症,例如不期望的血栓形成和非霍奇金淋巴瘤。
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公开(公告)号:US07767697B2
公开(公告)日:2010-08-03
申请号:US12166944
申请日:2008-07-02
申请人: Yonghong Song , Zhaozhong J. Jia , Anjali Pandey
发明人: Yonghong Song , Zhaozhong J. Jia , 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:US07109332B2
公开(公告)日:2006-09-19
申请号:US10956004
申请日:2004-09-29
申请人: Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
发明人: Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
IPC分类号: C07D409/12 , C07D409/14 , A61K31/517 , A61P7/02
CPC分类号: C07D409/12 , C07D409/14
摘要: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds 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: 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物,其具有下式:其中R是选自H和C 1-6烷基的成员; R 1是选自H,C 1-6烷基,C 1-6卤代烷基,C 1 -C 6烷基,C 1 -C 6烷基, 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H,卤素,C 1-6 - 烷基,C 2-6 - 烯基,C 1 -C 6烷基, C 1-6烷基,C 1-6烷氧基,氰基和-C(O)R 2a, 其中R 2a是选自C 1-6烷氧基和(C 1-6烷基)烷基的成员, 0-2氨基; L是选自-CH 2 - , - CH(CH 3 CH 3) - , - CH 2 - , - CH 2 CH 2(CH 3 CH 3) - 和-CH 2 CH 2 u> CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。 和Ar 1是选自苯,吡啶和嘧啶的芳环; 被提供。 该化合物可用于抑制ADP-血小板聚集,特别是在治疗血栓形成和血栓相关病症或病症中。
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