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公开(公告)号:US09133187B2
公开(公告)日:2015-09-15
申请号:US14002079
申请日:2012-02-28
申请人: James F. Blake , Huifen Chen , Mark Joseph Chicarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwarz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky , Steven Boyd
发明人: James F. Blake , Huifen Chen , Mark Joseph Chicarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwarz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky , Steven Boyd
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00 , C07D471/04 , C07D491/052 , A61K45/06
CPC分类号: C07D471/04 , A61K31/519 , A61K45/06 , C07D491/052
摘要: Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译: 具有式I的化合物,其中Z,Z 1 Z 2 Z 3,R 3a,R 3b和R b如本文所定义是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。
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公开(公告)号:US20130338140A1
公开(公告)日:2013-12-19
申请号:US14002079
申请日:2012-02-28
申请人: James F. Blake , Huifen Chen , Mark Joseph Chcarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwartz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky
发明人: James F. Blake , Huifen Chen , Mark Joseph Chcarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwartz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky
IPC分类号: C07D471/04 , A61K45/06 , A61K31/519
CPC分类号: C07D471/04 , A61K31/519 , A61K45/06 , C07D491/052
摘要: Compounds having the formula I wherein Z, Z1 Z2 Z, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译: 具有式I的化合物,其中Z,Z 1 Z 2 Z,R 3a,R 3b和R b如本文所定义,是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。
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公开(公告)号:US08003662B2
公开(公告)日:2011-08-23
申请号:US11699830
申请日:2007-01-30
申请人: James F. Blake , Steven Boyd , Jason De Meese , John J. Gaudino , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian
发明人: James F. Blake , Steven Boyd , Jason De Meese , John J. Gaudino , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian
IPC分类号: A61K31/4365
CPC分类号: C07D495/04 , C07D519/00
摘要: Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I 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化合物及其药学上可接受的盐可用于抑制受体酪氨酸激酶和用于治疗由此介导的病症。 公开了使用式I化合物及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:US20100256356A1
公开(公告)日:2010-10-07
申请号:US12693975
申请日:2010-01-26
申请人: James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
发明人: James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
IPC分类号: C07D471/04 , C07D451/04
CPC分类号: C07D471/04
摘要: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates 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受体酪氨酸激酶和用于治疗由此介导的病症。 使用式Ia和Ib化合物及其立体异构体,几何异构体,互变异构体,溶剂化物及其药学上可接受的盐的方法用于体外,原位和体内诊断,预防或治疗哺乳动物细胞中的这种病症或相关病理学 条件被公开。
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公开(公告)号:US07723330B2
公开(公告)日:2010-05-25
申请号:US11714342
申请日:2007-03-06
申请人: James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
发明人: James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
IPC分类号: A61K31/437 , A61K31/5025 , A61K31/4985 , A61K31/519 , A61K31/55 , A61K31/541 , A61K31/5355 , C07D487/04 , A61K31/551 , A61K31/501 , A61K31/497 , A61P35/00
CPC分类号: C07D471/04
摘要: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates 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受体酪氨酸激酶和用于治疗由此介导的病症。 使用式Ia和Ib化合物及其立体异构体,几何异构体,互变异构体,溶剂化物及其药学上可接受的盐的方法用于体外,原位和体内诊断,预防或治疗哺乳动物细胞中的这种病症或相关病理学 条件被公开。
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公开(公告)号:US06423710B1
公开(公告)日:2002-07-23
申请号:US09717956
申请日:2000-11-21
申请人: Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
发明人: Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
IPC分类号: A61K31535
CPC分类号: C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译: 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统(CNS)病症中的用途。
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公开(公告)号:US06362213B1
公开(公告)日:2002-03-26
申请号:US09737987
申请日:2000-12-15
申请人: John J. Gaudino
发明人: John J. Gaudino
IPC分类号: A61K31415
CPC分类号: C07D403/04
摘要: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
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公开(公告)号:US06586467B2
公开(公告)日:2003-07-01
申请号:US09899654
申请日:2001-07-05
申请人: Laurence E. Burgess , John J. Gaudino , Robert D. Groneberg , Mark H. Norman , Martha E. Rodriguez , Xicheng Sun , Eli M. Wallace
发明人: Laurence E. Burgess , John J. Gaudino , Robert D. Groneberg , Mark H. Norman , Martha E. Rodriguez , Xicheng Sun , Eli M. Wallace
IPC分类号: C07C25500
CPC分类号: C07D213/40 , C07C237/22 , C07C311/13 , C07C311/19 , C07C311/29 , C07D209/14 , C07D209/16 , C07D257/04 , C07D307/52
摘要: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B; R1, R2, R3, R4 and R5 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.
摘要翻译: 公开了式I化合物及其药学上可接受的盐和前药,其中A,B; R1,R2,R3,R4和R5如本说明书中所定义。这些化合物是酪氨酸磷酸酶抑制剂,可用于治疗或预防II型糖尿病。 本发明还包括包含所述化合物的制剂,制备这些化合物的方法,治疗或预防II型糖尿病的方法。
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公开(公告)号:US06444671B1
公开(公告)日:2002-09-03
申请号:US10002867
申请日:2001-11-15
申请人: John J. Gaudino
发明人: John J. Gaudino
IPC分类号: C07D41314
CPC分类号: C07D403/04
摘要: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
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公开(公告)号:US06258833B1
公开(公告)日:2001-07-10
申请号:US09471846
申请日:1999-12-23
申请人: Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
发明人: Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
IPC分类号: A61K31415
CPC分类号: C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译: 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统(CNS)病症中的用途。
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