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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：US20110105464A1
公开(公告)日：2011-05-05
申请号：US12916125
申请日：2010-10-29
申请人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
发明人： Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson , Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss
CPC分类号： C07D491/04 , C07D495/04
摘要： Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US07749994B2
公开(公告)日：2010-07-06
申请号：US11503405
申请日：2006-08-14
申请人： Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
发明人： Thomas E. Rawson , Brian Safina , Jennafer Dotson , Aihe Zhou , Ignacio Aliagas-Martin , Jason Halladay , Jun Liang , Matthias Rueth , Bing-Yan Zhu , Frederick Brookfield , Michael Prime , Birong Zhang , Jun M. Li
IPC分类号： A61K31/55 , A61K31/538 , A61K31/424 , A61K31/4188 , C07D498/22
CPC分类号： C07D487/04 , C07D491/04
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
摘要翻译： 本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I，其中A，X，Y，Z，R a，R b，R c，R 1，R 2，R 3和m定义 这里。
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公开(公告)号：US20100144732A1
公开(公告)日：2010-06-10
申请号：US12520194
申请日：2007-12-13
IPC分类号： A61K31/5377 , A61K31/505 , C07D413/02 , C07D239/02 , A61P35/04
CPC分类号： C07D239/48
摘要： The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein Q, X, Y, Z, R1, R2, R4, m and n are as defined herein.
摘要翻译： 本发明提供新的激酶抑制剂，其可用作例如治疗恶性肿瘤的治疗剂，其中化合物具有通式I，其中Q，X，Y，Z，R 1，R 2，R 4，m和n如本文所定义。
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公开(公告)号：US20080242665A1
公开(公告)日：2008-10-02
申请号：US11951203
申请日：2007-12-05
申请人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
发明人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
IPC分类号： A61K31/5377 , C07D495/04 , A61P35/04
CPC分类号： A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的 其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。 公开了使用式Ia-d的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US20080076758A1
公开(公告)日：2008-03-27
申请号：US11789468
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Bing-Yan Zhu
发明人： Adrian Folkes , Stephen Shuttleworth , Irina Chuckowree , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Bing-Yan Zhu
IPC分类号： A61K31/5377 , A61K31/551 , A61P25/00 , A61P29/00 , A61P3/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P9/00 , C07D491/048 , C07D495/04
CPC分类号： A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
摘要： Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式Ia和Ib的化合物及其立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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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：US20080039459A1
公开(公告)日：2008-02-14
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： C07D413/14 , A61K31/5377 , A61P17/00 , A61P25/00 , A61P3/00 , A61P3/10 , C12N9/99 , A61P31/00 , A61P35/00 , A61P41/00 , A61P9/00
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 式Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号：US20060160840A1
公开(公告)日：2006-07-20
申请号：US11284805
申请日：2005-11-21
申请人： Yonghong Song , Bing-Yan Zhu , Shumei Wang , Shawn Bauer , Robert Scarborough
发明人： Yonghong Song , Bing-Yan Zhu , Shumei Wang , Shawn Bauer , Robert Scarborough
IPC分类号： C07D498/02 , C07D217/12 , C07D217/06 , C07D209/42 , A61K31/4743 , A61K31/47 , A61K31/405
CPC分类号： C07D209/44 , C07D217/26 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D495/04
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.
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公开(公告)号：US20060100193A1
公开(公告)日：2006-05-11
申请号：US11158274
申请日：2005-06-20
申请人： Bing-Yan Zhu , Shawn Bauer , Zhaozhong Jia , Gary Probst , Yanchen Zhang , Robert Scarborough
发明人： Bing-Yan Zhu , Shawn Bauer , Zhaozhong Jia , Gary Probst , Yanchen Zhang , Robert Scarborough
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/453 , A61K31/4745 , A61K31/422 , A61K31/397 , A61K31/381 , C07D413/02 , C07D409/02
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.
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