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公开(公告)号：US08637537B2
公开(公告)日：2014-01-28
申请号：US13593776
申请日：2012-08-24
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D403/14 , A61K31/506 , A61K45/06
摘要： Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
摘要翻译： 具有式I的化合物，其中A，Z，R 1a，R 1b，R 2，R 3，R 4，R 5，R 6，R 7，R 9，R 10，R a，R b和n如本文所定义是PAK1的抑制剂。 还公开了用于治疗癌症和过度增殖性疾病的组合物和方法。
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公开(公告)号：US20130225620A1
公开(公告)日：2013-08-29
申请号：US13593776
申请日：2012-08-24
IPC分类号： C07D403/14 , A61K45/06 , A61K31/506
CPC分类号： C07D403/14 , A61K31/506 , A61K45/06
摘要： Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
摘要翻译： 具有式I的化合物，其中A，Z，R 1a，R 1b，R 2，R 3，R 4，R 5，R 6，R 7，R 9，R 10，R a，R b和n如本文所定义是PAK1的抑制剂。 还公开了用于治疗癌症和过度增殖性疾病的组合物和方法。
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公开(公告)号：US20130018033A1
公开(公告)日：2013-01-17
申请号：US13393116
申请日：2010-08-27
申请人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Wendy Lee , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Guiling Zhao , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen Laird , David Moreno , Li Ren , Steven Mark Wenglowsky
发明人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Wendy Lee , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Guiling Zhao , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen Laird , David Moreno , Li Ren , Steven Mark Wenglowsky
IPC分类号： A61K31/517 , C07D471/04 , A61K31/519 , C07D405/12 , A61P35/02 , C07D401/12 , C07D413/12 , A61K31/5377 , C07D239/72 , A61P35/00 , C07D239/94 , C07D403/12
CPC分类号： C07D239/94 , C07D403/12 , C07D405/12 , C07D471/04
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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：US20110110889A1
公开(公告)日：2011-05-12
申请号：US12920045
申请日：2009-02-27
申请人： Kateri A. Ahrendt et al. , Alexander J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt et al. , Alexander J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K38/21 , C07D471/04 , C07D401/10 , C07D401/02 , A61K31/437 , A61K31/5377 , A61K31/497 , A61K39/395 , A61P35/00
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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）的化合物可用于抑制Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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：US20120157453A1
公开(公告)日：2012-06-21
申请号：US13393111
申请日：2010-08-27
申请人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Steven Mark Wenglowsky
发明人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Steven Mark Wenglowsky
IPC分类号： A61K31/519 , A61K31/52 , C07D487/04 , C07D495/04 , C07D491/048 , A61P13/12 , A61P35/00 , A61P25/28 , A61P9/00 , A61P29/00 , A61P25/06 , A61P25/00 , C07D473/34 , A61K31/5377
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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II的化合物可用于抑制Raf激酶。 公开了使用式II化合物和其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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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![Pyrazole [3, 4-B] pyridine Raf inhibitors](/abs-image/US/2013/03/12/US08394795B2/abs.jpg.150x150.jpg)
公开(公告)号：US08394795B2
公开(公告)日：2013-03-12
申请号：US12920050
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven Mark Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K31/535 , A61K31/44 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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：US08338452B2
公开(公告)日：2012-12-25
申请号：US12920045
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , David Moreno , Brad Newhouse , Li Ren , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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）的化合物可用于抑制Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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：US20120214811A1
公开(公告)日：2012-08-23
申请号：US13393138
申请日：2010-08-27
申请人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Rebecca Pulk , Joachim Rudolph , Zhaoyang Wen
发明人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Rebecca Pulk , Joachim Rudolph , Zhaoyang Wen
IPC分类号： A61K31/5377 , A61K31/505 , A61P35/00 , C07D403/12 , C07D251/42 , A61K31/53 , C07D239/48 , C07D413/12
CPC分类号： C07D239/48 , C07D413/12
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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公开(公告)号：US20120157439A1
公开(公告)日：2012-06-21
申请号：US13393163
申请日：2010-08-27
申请人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Rebecca Pulk , Joachim Rudolph , Zhaoyang Wen , Jonas Grina , Joshua D. Hansen , Ellen Laird , David Moreno , Li Ren , Steven Mark Wenglowsky
发明人： Ignacio Aliagas , Stefan Gradl , Janet Gunzner , Simon Mathieu , Rebecca Pulk , Joachim Rudolph , Zhaoyang Wen , Jonas Grina , Joshua D. Hansen , Ellen Laird , David Moreno , Li Ren , Steven Mark Wenglowsky
IPC分类号： A61K31/519 , C07D495/04 , A61P35/00 , A61K31/5377 , A61K31/53 , C07D487/04 , C07D513/04
CPC分类号： C07D487/04 , C07D495/04 , C07D513/04
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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化合物可用于抑制Raf激酶。 公开了使用式I化合物和其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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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![PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS](/abs-image/US/2011/04/21/US20110092479A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110092479A1
公开(公告)日：2011-04-21
申请号：US12920050
申请日：2009-02-27
申请人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
发明人： Kateri A. Ahrendt , Alexandre J. Buckmelter , Jason De Meese , Jonas Grina , Joshua D. Hansen , Ellen R. Laird , Paul Lunghofer , David Moreno , Brad Newhouse , Li Ren , Jeongbeob Seo , Hongqi Tian , Steven M. Wenglowsky , Bainian Feng , Janet Gunzner , Kim Malesky , Simon Mathieu , Joachim Rudolph , Zhaoyang Wen , Wendy B. Young
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61K31/496 , A61P35/00 , A61P35/02 , A61P13/12
CPC分类号： C07D471/04 , C07C311/08
摘要： Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，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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