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公开(公告)号：US06919369B2
公开(公告)日：2005-07-19
申请号：US10224114
申请日：2002-08-19
申请人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
IPC分类号： C07D333/34 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/381 , A61P7/02 , A61P9/10 , C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US06472393B1
公开(公告)日：2002-10-29
申请号：US09509104
申请日：2000-03-21
申请人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean R. Artis , Michael S. Dina , John A. Flygare , Richard A. Goldsmith , Regina A. Munroe , Alan G. Olivero , Richard Pastor , Thomas E. Rawson , Kirk D. Robarge , Daniel P. Sutherlin , Kenneth J. Weese , Aihe Zhou , Yan Zhu
IPC分类号： A61K3118
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译： 具有下述结构的化合物其中A，B，N1，N2，X，Y，Q，R2，R5和R6如本文所定义，可用于抑制丝氨酸蛋白酶，如TF /因子VIIa因子Xa，凝血酶和激肽释放酶 。 这些化合物可用于预防和/或治疗凝血障碍的方法。
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公开(公告)号：US08101610B2
公开(公告)日：2012-01-24
申请号：US12093530
申请日：2006-11-14
IPC分类号： A61K31/505 , A61K31/4965 , A61K31/4196 , A61K31/4164 , C07D213/81
CPC分类号： A61K31/167 , A61K31/381 , A61K31/4164 , A61K31/4196 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/505 , A61K31/5375 , A61K31/538 , C07D213/82 , C07D231/14 , C07D233/06 , C07D239/28 , C07D249/08 , C07D265/36 , C07D277/56 , C07D285/06 , C07D295/155 , C07D307/68 , C07D333/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/12
摘要： The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2, R3, R4, R5, m and n are as defined herein.
摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导抑制剂，其中化合物具有通式I：其中环A，环B，R 1，R 2，R 3，R 4，R 5，m和n如本文所定义 。
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公开(公告)号：US20080269215A1
公开(公告)日：2008-10-30
申请号：US12093530
申请日：2006-11-14
IPC分类号： A61K31/44 , A61P35/00 , C07D213/82 , C07D401/02 , C07D413/02 , A61K31/426 , C07D277/20 , A61K31/5377 , A61K31/496 , A61K31/4545
CPC分类号： A61K31/167 , A61K31/381 , A61K31/4164 , A61K31/4196 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61K31/505 , A61K31/5375 , A61K31/538 , C07D213/82 , C07D231/14 , C07D233/06 , C07D239/28 , C07D249/08 , C07D265/36 , C07D277/56 , C07D285/06 , C07D295/155 , C07D307/68 , C07D333/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/12
摘要： The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein ring A, ring B, R1, R2, R3, R4, R5, m and n are as defined herein.
摘要翻译： 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导抑制剂，其中化合物具有通式I：其中环A，环B，R 1，R 2， R 3，R 3，R 4，R 5，m和n如本文所定义。
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5.发明申请公开(公告)号：US20110130363A1
公开(公告)日：2011-06-02
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/69 , C07D313/06 , C07D333/00 , C07D491/14 , C07F5/02 , C07D249/10 , C07D405/14 , A61K31/335 , A61K31/381 , A61K31/4196 , A61K31/443 , A61K31/497 , C12N9/99 , A61P35/00 , A61P35/02
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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I和II的苯并吡喃和苯并辛菌素化合物，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II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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6.发明申请公开(公告)号：US20090247567A1
公开(公告)日：2009-10-01
申请号：US12414403
申请日：2009-03-30
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/4353 , A61K31/429 , A61K31/38 , C07D491/044 , C07D513/04 , C07D495/04
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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I和II的苯并吡喃和苯并辛菌素化合物，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II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：US20120035208A1
公开(公告)日：2012-02-09
申请号：US13129091
申请日：2009-11-19
申请人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
发明人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
IPC分类号： A61K31/437 , C12N9/99 , A61P35/00 , A61P35/02 , A61P29/00 , A61P3/10 , A61P25/00 , A61P9/00 , A61P1/16 , A61P31/12 , A61P7/00 , C07D471/04 , A61P37/02
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) 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（I）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，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导 通过脂质激酶。 公开了使用式（I）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条件中的这种疾病的方法。
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公开(公告)号：US20110112085A1
公开(公告)日：2011-05-12
申请号：US13006217
申请日：2011-01-13
申请人： Georgette M. Castanedo , Janet L. Gunzner , Kimberly Malesky , Simon Mathieu , Alan G. Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan-Chi Wan
发明人： Georgette M. Castanedo , Janet L. Gunzner , Kimberly Malesky , Simon Mathieu , Alan G. Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan-Chi Wan
IPC分类号： A61K31/5377 , A61P35/00 , A61P35/02
CPC分类号： C07D513/04
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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![4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene compounds](/abs-image/US/2013/03/19/US08399690B2/abs.jpg.150x150.jpg)
9.发明授权公开(公告)号：US08399690B2
公开(公告)日：2013-03-19
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： C07D313/00 , C07D333/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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I和II的苯并吡喃和苯并辛菌素化合物，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II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：US08653098B2
公开(公告)日：2014-02-18
申请号：US13129091
申请日：2009-11-19
申请人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
发明人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
IPC分类号： A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) 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（I）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，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导 通过脂质激酶。 公开了使用式（I）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条件中的这种疾病的方法。
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