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公开(公告)号：US20110086841A1
公开(公告)日：2011-04-14
申请号：US12943284
申请日：2010-11-10
IPC分类号： A61K31/5377 , C07D473/40 , A61P35/00 , A61P35/02
CPC分类号： A61K31/52 , A61K31/5377 , C07D473/34
摘要： The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
摘要翻译： 本发明涉及式I化合物：其中R1，R2，R3，A1，A2，A3，A4和D具有本文所述的含义。 本发明还涉及包含这些化合物的药物组合物及其治疗用途。
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公开(公告)号：US08288381B2
公开(公告)日：2012-10-16
申请号：US12943284
申请日：2010-11-10
IPC分类号： A61K31/52 , A61P35/00 , C07D473/34 , C07D473/40
CPC分类号： A61K31/52 , A61K31/5377 , C07D473/34
摘要： The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
摘要翻译： 本发明涉及式I化合物：其中R1，R2，R3，A1，A2，A3，A4和D具有本文所述的含义。 本发明还涉及包含这些化合物的药物组合物及其治疗用途。
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3.发明申请N-7 SUBSTITUTED PURINE AND PYRAZOLOPYRIMINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权N-7取代的嘌呤和吡唑啉酮化合物，组合物和使用方法公开(公告)号：US20110086840A1
公开(公告)日：2011-04-14
申请号：US12943225
申请日：2010-11-10
申请人： Zhonghua Pei , Joseph P. Lyssikatos , Wendy Lee , Kirk D. Robarge
发明人： Zhonghua Pei , Joseph P. Lyssikatos , Wendy Lee , Kirk D. Robarge
IPC分类号： A61K31/397 , C07D413/14 , A61K31/5377 , A61K31/5386 , A61K31/553 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04 , C07D519/00
摘要： The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
摘要翻译： 本发明涉及式I化合物：其中R1，R2，R3，A1，A2，A3，A4，Y1和Y2和D具有本文所述的含义。 本发明还涉及包含这些化合物的药物组合物及其治疗用途。
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4.发明授权N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use 有权N-7取代的嘌呤和吡唑并嘧啶化合物，组合物和使用方法公开(公告)号：US08828990B2
公开(公告)日：2014-09-09
申请号：US12943225
申请日：2010-11-10
申请人： Zhonghua Pei , Joseph P. Lyssikatos , Wendy Lee , Kirk D. Robarge
发明人： Zhonghua Pei , Joseph P. Lyssikatos , Wendy Lee , Kirk D. Robarge
IPC分类号： C07D473/04 , A61K31/52 , C07D473/34 , C07D519/00 , C07D487/04 , A61K31/519
CPC分类号： C07D473/34 , C07D487/04 , C07D519/00
摘要： The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
摘要翻译： 本发明涉及式I化合物：其中R1，R2，R3，A1，A2，A3，A4，Y1和Y2和D具有本文所述的含义。 本发明还涉及包含这些化合物的药物组合物及其治疗用途。
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5.发明申请OXO-HETEROCYCLE FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开氧化杂环化合物吡嗪化合物，组合物和使用方法公开(公告)号：US20100331305A1
公开(公告)日：2010-12-30
申请号：US12821998
申请日：2010-06-23
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Cuong Ly , Joseph P. Lyssikatos , Zhonghua Pei , Wendy Lee , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Cuong Ly , Joseph P. Lyssikatos , Zhonghua Pei , Wendy Lee , Xianrui Zhao
IPC分类号： A61K31/5377 , C07D491/052 , A61P35/00 , A61P35/04 , A61K31/519 , C07D491/10 , C07D498/08 , A61K31/5386
CPC分类号： C07D491/052 , C07D491/048 , C07D491/18 , C07D519/00
摘要： Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I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，其可用于调节PIKK相关激酶信号传导，例如mTOR，以及用于治疗疾病（例如癌症）， 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US08163763B2
公开(公告)日：2012-04-24
申请号：US12533935
申请日：2009-07-31
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I化合物，其包括立体异构体，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，其可用于调节PIKK相关激酶信号传导，例如mTOR和用于治疗疾病（例如癌症）， 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US20100069357A1
公开(公告)日：2010-03-18
申请号：US12533935
申请日：2009-07-31
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/5377 , C07D487/04 , C07D471/04 , A61K31/55 , A61K31/553 , A61K31/519 , A61P35/00
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I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，其可用于调节PIKK相关激酶信号传导，例如mTOR，以及用于治疗疾病（例如癌症） 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US20120165313A1
公开(公告)日：2012-06-28
申请号：US13410246
申请日：2012-03-01
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Coung Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Coung Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/553 , A61K31/5377 , C07D491/048 , A61K31/519 , C07D471/04 , A61P35/02 , A61K31/55 , C07D471/14 , C07D491/08 , C07D471/18 , A61P35/00 , C07D487/04 , A61K31/5386
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I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，其可用于调节PIKK相关激酶信号传导，例如mTOR，以及用于治疗疾病（例如癌症） 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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9.发明授权公开(公告)号：US08623889B2
公开(公告)日：2014-01-07
申请号：US13325751
申请日：2011-12-14
IPC分类号： A01N43/42 , A61K31/44 , A61K31/47 , C07D221/02 , C07D471/02 , C07D217/00
CPC分类号： C07D471/04 , A61K31/47 , A61K31/4725 , C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/04
摘要： The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
摘要翻译： 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。
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公开(公告)号：US20130109656A1
公开(公告)日：2013-05-02
申请号：US13586355
申请日：2012-08-15
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
IPC分类号： C07F9/6539 , C07D419/04 , C07D513/04 , C07D417/04
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
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