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公开(公告)号:US06613776B2
公开(公告)日:2003-09-02
申请号:US09952836
申请日:2001-09-14
申请人: Ronald Knegtel , David Bebbington , Hayley Binch , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
发明人: Ronald Knegtel , David Bebbington , Hayley Binch , Julian Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert Davies , Pan Li , Marion Wannamaker , Cornelia Forster , Albert Pierce
IPC分类号: C07D40112
CPC分类号: C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译: 本发明描述了包含药学上可接受的载体和式V化合物的新型吡唑组合物:其中Z1是N,CRa或CH,Z2是N或CH,其中Z1和Z2之一是氮; G是环C或环D; 环C选自苯基,吡啶基,嘧啶基,哒嗪基,吡嗪基或1,2,4-三嗪基,其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基,杂芳基,杂环基或碳环基的5-7元单环或8-10元双环; Rx和Ry独立地选自T-R3,或Rx和Ry与它们的插入原子一起形成稠环; R1,R2,R2',R3和T如说明书所述。 这些化合物可用作蛋白激酶抑制剂,特别是作为用于治疗诸如癌症,糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
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82.
公开(公告)号:US08853244B2
公开(公告)日:2014-10-07
申请号:US11805418
申请日:2007-05-23
申请人: Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
发明人: Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
IPC分类号: A61K31/4436 , C07D409/04
CPC分类号: C07D409/04
摘要: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病,病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号:US08841308B2
公开(公告)日:2014-09-23
申请号:US12642447
申请日:2009-12-18
申请人: Jean-Damien Charrier , David Kay , Ronald Knegtel , Somhairle MacCormick , Michael O'Donnell , Joanne Pinder , Philip Michael Reaper
发明人: Jean-Damien Charrier , David Kay , Ronald Knegtel , Somhairle MacCormick , Michael O'Donnell , Joanne Pinder , Philip Michael Reaper
IPC分类号: A61K31/4965
CPC分类号: C07D413/14 , A61P35/00 , C07D241/28 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.
摘要翻译: 本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病,病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法,如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式I:其中变量如本文所定义。
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84.
公开(公告)号:US08822469B2
公开(公告)日:2014-09-02
申请号:US13531461
申请日:2012-06-22
申请人: Somhairle MacCormick , Pierre-Henri Storck , Michael Paul Mortimore , Jean-Damien Charrier , Ronald Knegtel , Stephen Clinton Young , Joanne Pinder , Steven John Durrant
发明人: Somhairle MacCormick , Pierre-Henri Storck , Michael Paul Mortimore , Jean-Damien Charrier , Ronald Knegtel , Stephen Clinton Young , Joanne Pinder , Steven John Durrant
IPC分类号: A61K31/4985 , C07D241/36
CPC分类号: C07D487/04
摘要: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.
摘要翻译: 本发明涉及可用作ATR蛋白激酶抑制剂的吡咯并吡嗪化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病,病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法,如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式I:其中变量如本文所定义。
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公开(公告)号:US20130261114A1
公开(公告)日:2013-10-03
申请号:US13623970
申请日:2012-09-21
IPC分类号: C07D453/02 , A61K45/06 , A61K31/5377 , A61K31/439 , A61K31/496
CPC分类号: C07D453/02 , A61K31/439 , A61K31/496 , A61K31/5377 , A61K45/06
摘要: The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
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公开(公告)号:US20120165367A1
公开(公告)日:2012-06-28
申请号:US13193739
申请日:2011-07-29
申请人: Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Sharn Ramaya , Shazia Keily , Jingrong Cao
发明人: Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Sharn Ramaya , Shazia Keily , Jingrong Cao
IPC分类号: A61K31/437 , A61K31/4545 , A61P37/00 , A61P29/00 , A61P35/00 , A61P25/28 , C07D471/04 , A61P37/06
CPC分类号: C07D471/02 , C07D471/04 , C07D487/02
摘要: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病,病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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87.
公开(公告)号:US08188134B2
公开(公告)日:2012-05-29
申请号:US12891973
申请日:2010-09-28
申请人: Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
发明人: Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
IPC分类号: A61K31/4155 , A61K31/4178
CPC分类号: C07D409/04
摘要: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供药学上可接受的组合物,其包含化合物和使用该组合物治疗各种疾病,病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号:US08022202B2
公开(公告)日:2011-09-20
申请号:US12569237
申请日:2009-09-29
申请人: David Kay , Ronald Knegtel , Jean-Damien Charrier , Heather Twin
发明人: David Kay , Ronald Knegtel , Jean-Damien Charrier , Heather Twin
IPC分类号: C07D401/12
CPC分类号: C07D487/04 , A61K31/551 , A61K45/06 , C07D487/14
摘要: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病,病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号:US20110178146A1
公开(公告)日:2011-07-21
申请号:US12891973
申请日:2010-09-28
申请人: Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
发明人: Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
IPC分类号: A61K31/4178 , A61K31/4155 , A61P35/00 , A61P29/00 , A61P19/00 , A61P9/00 , A61P3/00 , C12N9/99
CPC分类号: C07D409/04
摘要: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病,病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号:US07982037B2
公开(公告)日:2011-07-19
申请号:US12545347
申请日:2009-08-21
IPC分类号: C07D403/12
CPC分类号: C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译: 本发明描述了式IIIa的新型吡唑化合物:其中R1是T环D,其中环D是5-7元单环或选自芳基,杂芳基,杂环基或碳环基的8-10元双环; Rx,Ry,R2和R2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂,特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症,糖尿病和阿尔茨海默病的疾病。
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