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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：US20110071145A1
公开(公告)日：2011-03-24
申请号：US12903031
申请日：2010-10-12
申请人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
发明人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
IPC分类号： A61K31/4184 , A61P35/00 , A61P19/02 , A61P9/10 , A61P1/00 , A61P9/00 , A61K31/538 , A61K31/498 , A61K31/416 , A61K31/4439 , A61K31/5377 , A61K31/454 , A61K31/496
CPC分类号： C07D413/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式I化合物，其中G，A，X 1，X 2，X 3，Z，E，Y和X如本文所定义。 该化合物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，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是Raf。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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公开(公告)号：US08697737B2
公开(公告)日：2014-04-15
申请号：US12903031
申请日：2010-10-12
申请人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
发明人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
IPC分类号： A01N43/56 , A61K31/415 , C07D231/56
CPC分类号： C07D413/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式I化合物，其中G，A，X 1，X 2，X 3，Z，E，Y和X如本文所定义。 该化合物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，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是Raf。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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公开(公告)号：US07846959B2
公开(公告)日：2010-12-07
申请号：US11568789
申请日：2005-03-25
申请人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
发明人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
IPC分类号： C07D231/02
CPC分类号： C07D413/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式I化合物，其中G，A，X 1，X 2，X 3，Z，E，Y和X如本文所定义。 该化合物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，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是Raf。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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公开(公告)号：US07872014B2
公开(公告)日：2011-01-18
申请号：US10565657
申请日：2004-07-23
申请人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Richard G. Khoury , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
发明人： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Richard G. Khoury , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04 , C07D491/147 , C07D519/00
摘要： The present invention comprises compounds and pharmaceutical compositions comprising the compounds that are inhibitors of ALK. The invention also comprises methods of using the compounds and compositions to treat diseases mediated by ALK, including diseases such as cancer, immunological disorders, cardiovascular diseases, and other degenerative disorders.
摘要翻译： 本发明包括包含作为ALK抑制剂的化合物的化合物和药物组合物。 本发明还包括使用化合物和组合物来治疗由ALK介导的疾病，包括诸如癌症，免疫学障碍，心血管疾病和其它退行性疾病的疾病的方法。
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公开(公告)号：US20090215803A1
公开(公告)日：2009-08-27
申请号：US12083749
申请日：2006-10-23
申请人： Kenneth D. Rice , Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Joerg Bussenius , Wai Ki Vickey Chan , Hongwang Du , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , Patrick Kearney , Abigail R. Kennedy , Moon Hwan Kim , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Amy Lew Tsuhako , Peiwen Zhou , Elena S. Koltun
发明人： Kenneth D. Rice , Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Joerg Bussenius , Wai Ki Vickey Chan , Hongwang Du , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , Patrick Kearney , Abigail R. Kennedy , Moon Hwan Kim , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Amy Lew Tsuhako , Peiwen Zhou , Elena S. Koltun
IPC分类号： A61K31/513 , C07D403/02 , C12N9/99 , A61P35/00
CPC分类号： C07D487/04
摘要： A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
摘要翻译： 具有式（I）的化合物或其药学上可接受的盐，其中X，R 1和R 2在说明书中定义; 其药物组合物; 及其使用方法。
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公开(公告)号：US08101625B2
公开(公告)日：2012-01-24
申请号：US12083749
申请日：2006-10-23
申请人： Kenneth D. Rice , Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Joerg Bussenius , Wai Ki Vicky Chan , Hongwang Du , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , Patrick Kearney , Abigail R. Kennedy , Moon Hwan Kim , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Amy Lew Tsuhako , Peiwen Zhou , Elena S. Koltun
发明人： Kenneth D. Rice , Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Joerg Bussenius , Wai Ki Vicky Chan , Hongwang Du , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , Patrick Kearney , Abigail R. Kennedy , Moon Hwan Kim , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Amy Lew Tsuhako , Peiwen Zhou , Elena S. Koltun
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D487/04
摘要： A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
摘要翻译： 具有式（I）的化合物或其药学上可接受的盐，其中X，R 1和R 2在说明书中定义; 其药物组合物; 及其使用方法。
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公开(公告)号：US20080076774A1
公开(公告)日：2008-03-27
申请号：US11568173
申请日：2005-04-22
申请人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
发明人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
IPC分类号： A61K31/497 , A61K31/501 , A61P43/00 , C07D403/14 , C07D473/00 , C12N5/06 , C12Q1/48
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式（I）和（II）的化合物，其中R 1，R 21，R 25，R 33，m ，n，X 21 -X 23和Q 1在本文中定义。 该化合物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，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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公开(公告)号：US08076338B2
公开(公告)日：2011-12-13
申请号：US11568173
申请日：2005-04-22
申请人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
发明人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
IPC分类号： A61K31/501 , A61K31/497 , C07D473/16 , C07D401/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式（I）和（II）的化合物，其中R，R 21，R 25 -R 33，m，n，X 21-X 23和Q 1在本文中定义。 该化合物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，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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