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公开(公告)号:US20100130469A1
公开(公告)日:2010-05-27
申请号:US12594724
申请日:2008-04-04
申请人: Maurice van Eis , Walter Schuler , Anette Von Matt , Nicolas Soldermann , Lauren G. Monovich , Christoph Gaul
发明人: Maurice van Eis , Walter Schuler , Anette Von Matt , Nicolas Soldermann , Lauren G. Monovich , Christoph Gaul
IPC分类号: A61K31/397 , A61K31/551 , A61K31/499 , A61K31/496 , A61K31/4375 , A61K31/4725 , C07D471/04 , C07D401/14 , C07D217/12 , C07D205/04 , A61P37/00 , A61P29/00
CPC分类号: C07D471/04
摘要: The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.
摘要翻译: 本发明涉及包含萘啶的新型有机化合物,其可以是属于AGC激酶家族的激酶的选择性子集的介体,例如PKC,PKD,PKN-1,CDK-9,MRCK-beat, PASK,PRKX,ROCK-I / II或其他激酶的介质,其选择性取决于其结构变化。
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公开(公告)号:US20120142685A1
公开(公告)日:2012-06-07
申请号:US12594728
申请日:2008-04-04
申请人: Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
发明人: Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
IPC分类号: A61K31/5377 , C07D471/10 , A61K31/444 , A61P7/10 , A61P9/04 , A61P35/00 , A61P3/04 , A61P3/10 , C07D471/04 , A61K31/496
CPC分类号: C07D471/04
摘要: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译: 本发明提供式I化合物:(式I)所述化合物是属于AGC或钙调蛋白激酶家族的激酶选择性亚型的抑制剂,例如MARK1 / 2/3,PKD-1/2/3,PKN -1/2,CDK-9,CaMKII,ROCK-I / II,组蛋白脱乙酰酶(HDAC)磷酸化抑制剂或其他激酶抑制剂。 最后,本发明还提供药物组合物。
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3.2,4- Di(hetero)-arylamino-pyrimidine Derivatives as ZAP-70 and/or SYK inhibitors 失效
标题翻译: 2,4-二(杂) - 芳基氨基 - 嘧啶衍生物,为ZAP-70和/或SYK抑制剂公开(公告)号:US20100152182A1
公开(公告)日:2010-06-17
申请号:US12686863
申请日:2010-01-13
申请人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
发明人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
IPC分类号: A61K31/5377 , C07D239/69 , A61K31/506 , A61P35/00 , A61P37/00 , A61P7/00 , C07D413/14
CPC分类号: C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.
摘要翻译: 公开了下式的嘧啶衍生物其中R 0,R 1,R 3至R 9和Z具有如权利要求1所示的含义,其具有有趣的药物性质。
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4.2,4 Di (hetero) -arylamino-pyrimidine derivatives as ZAP-70 and/or syk inhibitors 失效
标题翻译: 2,4-二(杂) - 芳基氨基 - 嘧啶衍生物,如ZAP-70和/或syk抑制剂公开(公告)号:US07671063B2
公开(公告)日:2010-03-02
申请号:US11377716
申请日:2006-03-16
申请人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
发明人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
IPC分类号: C07D405/12 , C07D239/48 , C07D413/14 , A61K31/506
CPC分类号: C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.
摘要翻译: 公开了下式的嘧啶衍生物其中R 0,R 1,R 3至R 9和Z具有如权利要求1所示的含义,其具有有趣的药物性质。
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5.2,4- Di(hetero)-arylamino-pyrimidine derivatives as ZAP-70 and/or SYK inhibitors 失效
标题翻译: 2,4-二(杂) - 芳基氨基 - 嘧啶衍生物,为ZAP-70和/或SYK抑制剂公开(公告)号:US08283356B2
公开(公告)日:2012-10-09
申请号:US12686863
申请日:2010-01-13
申请人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
发明人: Rolf Baenteli , Marie Claude Bernhard , Peter Buehlmayer , Nigel Graham Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
IPC分类号: C07D405/12 , C07D239/48 , C07D413/14 , A61K31/506
CPC分类号: C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.
摘要翻译: 公开了下式的嘧啶衍生物其中R 0,R 1,R 3至R 9和Z具有如权利要求1所示的含义,其具有有趣的药物性质。
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6.2,4 Di (hetero) -arylamino-pyrimidine derivatives as ZAP-70 and/or syk inhibitors 失效
标题翻译: 2,4-二(杂) - 芳基氨基 - 嘧啶衍生物,如ZAP-70和/或syk抑制剂公开(公告)号:US20060247262A1
公开(公告)日:2006-11-02
申请号:US11377716
申请日:2006-03-16
申请人: Rolf Baenteli , Marie Bernhard , Peter Buehlmayer , Nigel Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
发明人: Rolf Baenteli , Marie Bernhard , Peter Buehlmayer , Nigel Cooke , Rudolf Duthaler , Klaus Hinterding , Gebhard Thoma , Maurice Van Eis , Anette Von Matt , Louis Walliser , Gerhard Zenke
IPC分类号: A61K31/506 , C07D403/02
CPC分类号: C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.
摘要翻译: 公开了下式的嘧啶衍生物其中R 0,R 1,R 3至R 9,Z具有 如权利要求1所述的含义,其具有有趣的药物性质。
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公开(公告)号:US08653092B2
公开(公告)日:2014-02-18
申请号:US13175050
申请日:2011-07-01
申请人: Nigel Graham Cooke , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Christina Hebach , Klemens Högenauer , Gregory Hollingworth , Alexander Baxter Smith , Nicolas Soldermann , Frank Stowasser , Ross Strang , Nicola Tufilli , Anette Von Matt , Romain Wolf , Frédéric Zecri
发明人: Nigel Graham Cooke , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Christina Hebach , Klemens Högenauer , Gregory Hollingworth , Alexander Baxter Smith , Nicolas Soldermann , Frank Stowasser , Ross Strang , Nicola Tufilli , Anette Von Matt , Romain Wolf , Frédéric Zecri
IPC分类号: C07D471/04 , A61K31/519 , A61P37/08 , A61P25/28 , A61P35/00 , A61P37/06
CPC分类号: C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译: 本发明涉及式(I)的取代的四氢 - 吡啶并 - 嘧啶衍生物,其中Y,R 1,R 2和m如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。
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公开(公告)号:US09499536B2
公开(公告)日:2016-11-22
申请号:US14151796
申请日:2014-01-09
申请人: Nigel Graham Cooke , Frédèric Zecri , Nicolas Soldermann , Romain Wolf , Christina Hebach , Klemens Hoegenauer , Gregory John Hollingworth , Anette Von Matt , Ross Sinclair Strang , Alexander Baxter Smith , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Frank Stowasser , Nicola Tufilli
发明人: Nigel Graham Cooke , Frédèric Zecri , Nicolas Soldermann , Romain Wolf , Christina Hebach , Klemens Hoegenauer , Gregory John Hollingworth , Anette Von Matt , Ross Sinclair Strang , Alexander Baxter Smith , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Frank Stowasser , Nicola Tufilli
IPC分类号: A61K31/519 , A61P35/02 , A61P19/02 , C07D471/04
CPC分类号: C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译: 本发明涉及式(I)的取代的四氢 - 吡啶并 - 嘧啶衍生物,其中Y,R 1,R 2和m如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。
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公开(公告)号:US20110172231A1
公开(公告)日:2011-07-14
申请号:US13069816
申请日:2011-03-23
申请人: Rolf BAENTELI , Gerhard Zenke , Nigel Graham Cooke , Rudolf Duthaler , Gebhard Thoma , Anette Von Matt , Toshiyuki Honda , Naoko Matsuura , Kazuhiko Nonomura , Osamu Ohmori , Ichiro Umemura , Klaus Hinterding , Christos Papageorgiou
发明人: Rolf BAENTELI , Gerhard Zenke , Nigel Graham Cooke , Rudolf Duthaler , Gebhard Thoma , Anette Von Matt , Toshiyuki Honda , Naoko Matsuura , Kazuhiko Nonomura , Osamu Ohmori , Ichiro Umemura , Klaus Hinterding , Christos Papageorgiou
IPC分类号: A61K31/5377 , C07D403/12 , A61K31/506 , A61P29/00 , A61P35/00 , A61P35/02 , C07D239/48 , C07D413/12 , A61K31/496
CPC分类号: C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
摘要: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
摘要翻译: 提供式I化合物,其中X,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8和R 9如权利要求1所述,其可用于ZAP-70和/或Syk抑制起作用或 由与FAK连接的信号级联故障引起的。
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公开(公告)号:US07943627B2
公开(公告)日:2011-05-17
申请号:US10507060
申请日:2003-03-14
申请人: Rolf Baenteli , Gerhard Zenke , Nigel Graham Cooke , Rudolf Duthaler , Gebhard Thoma , Anette Von Matt , Toshiyuki Honda , Naoko Matsuura , Kazuhiko Nonomura , Osamu Ohmori , Ichiro Umemura , Klaus Hinterding , Christos Papageorgiou
发明人: Rolf Baenteli , Gerhard Zenke , Nigel Graham Cooke , Rudolf Duthaler , Gebhard Thoma , Anette Von Matt , Toshiyuki Honda , Naoko Matsuura , Kazuhiko Nonomura , Osamu Ohmori , Ichiro Umemura , Klaus Hinterding , Christos Papageorgiou
IPC分类号: C07D239/48 , A61K31/505
CPC分类号: C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
摘要: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
摘要翻译: 提供式I化合物,其中X,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8和R 9如权利要求1所述,其可用于ZAP-70和/或Syk抑制起作用或 由与FAK连接的信号级联故障引起的。
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