-
11.发明申请Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 审中-公开苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法公开(公告)号：US20140066431A1
公开(公告)日：2014-03-06
申请号：US13885307
申请日：2011-11-15
申请人： Kenneth D. Rice , David Markby
发明人： Kenneth D. Rice , David Markby
IPC分类号： A61K31/553 , G01N33/574 , C12Q1/68 , A61K45/06
CPC分类号： A61K31/553 , A61K31/00 , A61K31/437 , A61K31/519 , A61K45/06 , C12Q1/6886 , G01N33/574 , A61K2300/00
摘要： The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.
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，以及使用该化合物的治疗方法，用于筛选抑制剂化合物的方法和鉴定治疗方案的方法。
-
12.发明授权Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture 失效苯并西泮作为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。
-
公开(公告)号：US20100130488A1
公开(公告)日：2010-05-27
申请号：US12083669
申请日：2006-10-23
申请人： Kenneth D. Rice , Joerg Bussenius , Simona Costanzo , Abigail R. Kennedy , Angie Inyoung Kim , Jean-Claire Limun Manalo , Csaba J. Peto
发明人： Kenneth D. Rice , Joerg Bussenius , Simona Costanzo , Abigail R. Kennedy , Angie Inyoung Kim , Jean-Claire Limun Manalo , Csaba J. Peto
IPC分类号： A61K31/519 , C07D487/04 , A61K31/5377 , A61K31/496 , A61P35/00
CPC分类号： C07D487/04
摘要： A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
摘要翻译： 根据式（I）的化合物或其药学上可接受的盐，其中R1，R2，R6，R7和Z如说明书中所定义; 其药物组合物; 及其使用方法。
-
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。
-
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。
-
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。
-
17.发明申请Benzoxazepines as Inhibitors of PI3K/M TOR and Methods of Their Use and Manufacture 审中-公开苯并西泮作为PI3K / M TOR的抑制剂及其使用和制造方法公开(公告)号：US20140005172A1
公开(公告)日：2014-01-02
申请号：US13989330
申请日：2011-11-23
申请人： Kenneth D. Rice
发明人： Kenneth D. Rice
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The invention is directed to inhibitors of PI3K and mTOR and pharmaceutically acceptable salts or solvates thereof as well as methods of using them, wherein the inhibitors are of structural Formula I and pharmaceutically acceptable salts thereof wherein the variables are as defined herein.
摘要翻译： 本发明涉及PI3K和mTOR及其药学上可接受的盐或溶剂合物的抑制剂以及其使用方法，其中所述抑制剂为结构式I及其药学上可接受的盐，其中变量如本文所定义。
-
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。
-
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。
-
20.发明申请Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 失效苯并西泮作为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。
-
-
-
-
-
-
-
-
-
搜索结果
37 条记录 (耗时 0.059 秒)
