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公开(公告)号:US07704995B2
公开(公告)日:2010-04-27
申请号:US10513081
申请日:2003-05-02
申请人: Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller
发明人: Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller
IPC分类号: C07D279/16 , C07D279/12 , C07D417/12 , C07D265/36 , C07D413/12 , C07D403/12 , C07D401/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D419/12 , C07D241/18 , C07D241/20 , A61K31/55 , A61K31/497 , A61K31/5355 , A61K31/541 , C07D305/12 , C07D307/79 , A61K31/44 , A61P35/00
CPC分类号: C07D241/26 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12
摘要: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.
摘要翻译: 本发明涉及用于调节蛋白激酶酶活性以调节细胞活性如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物,以及含有这些化合物的药物组合物。 更具体地,本发明涉及抑制,调节和/或调节激酶,特别是检查点激酶,甚至更特别是检查点激酶1或Chk1的化合物。 治疗或预防性地使用化合物和组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面,并且包括通过以下方法治疗癌症以及与不期望的血管生成和/或细胞增殖相关的其它疾病状态, 施用有效量的这些化合物。
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公开(公告)号:US08012956B2
公开(公告)日:2011-09-06
申请号:US12290159
申请日:2008-10-27
申请人: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
发明人: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
IPC分类号: A61K31/46 , A61K31/5377 , A61K31/496 , A61K31/497 , C07D451/04
CPC分类号: C07D451/02
摘要: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译: 根据式I或II的化合物:其中R1,R1b,R2,L1和L2和L2b如说明书中所定义,其药物组合物及其使用方法。
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公开(公告)号:US20090163471A1
公开(公告)日:2009-06-25
申请号:US12290159
申请日:2008-10-27
申请人: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
发明人: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
IPC分类号: A61K31/46 , C07D451/04 , A61K31/5377 , A61K31/496 , A61K31/497
CPC分类号: C07D451/02
摘要: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译: 根据式I或II的化合物:其中R1,R1b,R2,L1和L2和L2b如说明书中所定义,其药物组合物及其使用方法。
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公开(公告)号:US20060211709A1
公开(公告)日:2006-09-21
申请号:US10513081
申请日:2003-05-02
申请人: Chris Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Co , Sergey Epshteyn , Abigail Kennedy , Baili Chen , Larisa Dubenko , Neel Anand , Tsze Tsang , John Nuss , Csabaj Peto , Kenneth Rice , Mohamed Ibrahim , Xian Shi , James Leahy , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Grace Mann , Larry Mann , Craig Takeuchi
发明人: Chris Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Co , Sergey Epshteyn , Abigail Kennedy , Baili Chen , Larisa Dubenko , Neel Anand , Tsze Tsang , John Nuss , Csabaj Peto , Kenneth Rice , Mohamed Ibrahim , Xian Shi , James Leahy , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Grace Mann , Larry Mann , Craig Takeuchi
IPC分类号: A61K31/497 , C07D403/02
CPC分类号: C07D241/26 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12
摘要: Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
摘要翻译: 公开了取代的芳基1,4-吡嗪衍生物及其在治疗焦虑症,抑郁症和应激相关疾病中的用途。
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5.Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture 失效
标题翻译: 苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法公开(公告)号:US08648066B2
公开(公告)日:2014-02-11
申请号:US12784254
申请日:2010-05-20
申请人: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
发明人: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
IPC分类号: A61P35/00 , A61K31/553 , C07D267/14
CPC分类号: C07D413/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/08 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物,以及制备和使用该化合物的方法。
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6.Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 失效
标题翻译: 苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法公开(公告)号:US20100298290A1
公开(公告)日:2010-11-25
申请号:US12784254
申请日:2010-05-20
申请人: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
发明人: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
IPC分类号: A61K31/553 , C07D413/14 , A61P35/00 , A61P35/04
CPC分类号: C07D413/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/08 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物,以及制备和使用该化合物的方法。
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公开(公告)号:US08710038B2
公开(公告)日:2014-04-29
申请号:US11575411
申请日:2005-09-15
申请人: Tae-Gon Baik , Chris A. Buhr , Sunghoon Ma , John M. Nuss , Zerom Tesfai , Longcheng Wang , Bryan K. S. Yeung
发明人: Tae-Gon Baik , Chris A. Buhr , Sunghoon Ma , John M. Nuss , Zerom Tesfai , Longcheng Wang , Bryan K. S. Yeung
IPC分类号: C07D403/00 , A01N43/00 , A61K31/33
CPC分类号: C07D403/04 , C07D231/12 , C07D401/04 , C07D405/04 , C07D409/04
摘要: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译: 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖,分化,程序性细胞死亡,迁移和化学侵蚀的化合物。 本发明的化合物抑制,调节和/或调节激酶。 使用化合物及其药物组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面。
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公开(公告)号:US20100305093A1
公开(公告)日:2010-12-02
申请号:US12756374
申请日:2010-04-08
申请人: Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Chris A. Buhr , Jonah Cannoy , Sergey Ephsteyn , Henry William Beecroft Johnson , Anagha Joshi , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Sunghoon Ma , Morrison B. Mac , John M. Nuss , Craig Stacy Takeuchi , Longcheng Wang , Yong Wang
发明人: Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Chris A. Buhr , Jonah Cannoy , Sergey Ephsteyn , Henry William Beecroft Johnson , Anagha Joshi , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Sunghoon Ma , Morrison B. Mac , John M. Nuss , Craig Stacy Takeuchi , Longcheng Wang , Yong Wang
IPC分类号: A61K31/553 , C07D405/10 , A61P35/00 , A61P37/00 , A61P35/02 , A61P27/00
CPC分类号: C07D267/14 , C07D413/04
摘要: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物,以及制备和使用该化合物的方法。
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公开(公告)号:US20110237608A1
公开(公告)日:2011-09-29
申请号:US13152045
申请日:2011-06-02
申请人: Tae-Gon Baik , Chris A. Buhr , Katherine Lara , Sunghoon Ma , Morrison Mac , John M. Nuss , Longcheng Wang , Yong Wang , Bryan K.S. Yeung
发明人: Tae-Gon Baik , Chris A. Buhr , Katherine Lara , Sunghoon Ma , Morrison Mac , John M. Nuss , Longcheng Wang , Yong Wang , Bryan K.S. Yeung
IPC分类号: A61K31/519 , C07D471/04 , A61P35/00 , A61P35/02
CPC分类号: C07D471/04 , A61K9/0095 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/2018 , A61K9/4858
摘要: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物,以及制备和使用该化合物的方法。
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10.Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha 有权
标题翻译: 取代的吡啶并[2,3-d]嘧啶-7(8H) - 酮磷酸肌醇3-激酶α抑制剂公开(公告)号:US08044062B2
公开(公告)日:2011-10-25
申请号:US11988848
申请日:2006-10-09
申请人: Tae-Gon Baik , Chris A. Buhr , Katherine Lara , Sunghoon Ma , Morrison Mac , John M. Nuss , Longcheng Wang , Yong Wang , Bryan K. S. Yeung
发明人: Tae-Gon Baik , Chris A. Buhr , Katherine Lara , Sunghoon Ma , Morrison Mac , John M. Nuss , Longcheng Wang , Yong Wang , Bryan K. S. Yeung
IPC分类号: C07D471/04 , A61K31/519 , A61P35/00
CPC分类号: C07D471/04 , A61K9/0095 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/2018 , A61K9/4858
摘要: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
摘要翻译: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物,以及制备和使用该化合物的方法。
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