公开(公告)号：EP1848719B1

公开(公告)日：2012-02-01

申请号：EP05855490.8

申请日：2005-12-27

申请人： Exelixis, Inc.

发明人： RICE, Kenneth, D. ,  CO, Erick, Wang ,  KIM, Moon, Hwan ,  BANNEN, Lynn, Canne ,  BUSSENIUS, Joerg ,  LE, Donna ,  TSUHAKO, Amy, Lew ,  NUSS, John ,  WANG, Yong ,  XU, Wei ,  KLEIN, Rhett, Ronald

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D487/04

摘要： The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

公开(公告)号：EP1750727A2

公开(公告)日：2007-02-14

申请号：EP05804792.9

申请日：2005-04-22

申请人： Exelixis, Inc.

发明人： ANAND, Neel, K. ,  BLAZEY, Charles, M. ,  BOWLES, Owen, Joseph ,  BUSSENIUS, Joerg ,  CANNE BANNEN, Lynne ,  CHAN, Diva Sze-Ming ,  CHEN, Baili ,  CO, Erick Wang ,  COSTANZO, Simona ,  DEFINA, Steven, Charles ,  DUBENKO, Larisa ,  FRANZINI, Maurizio ,  HUANG, Ping ,  JAMMALAMADAKA, Vasu ,  KHOURY, Richard George ,  KIM, Moon, Hwan ,  KLEIN, Rhett, Ronald ,  LE, Donna, Tra ,  MAC, Morrison, B. ,  PARKS, Jason, Jevious ,  RICE, Kenneth, D. ,  NUSS, John M. ,  TSANG, Tsze ,  TSUHAKO, Amy Lew ,  WANG, Yong ,  XU, Wei

IPC分类号： A61K31/7076

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.

公开(公告)号：EP1678168A2

公开(公告)日：2006-07-12

申请号：EP04796443.2

申请日：2004-10-22

申请人： Exelixis, Inc.

发明人： CHENG, Wei ,  CO, Erick, Wang ,  KIM, Moon, Hwan ,  KLEIN, Rhett, Ronald ,  LE, Donna, T. ,  LEW, Amy ,  NUSS, John, M. ,  XU, Wei

IPC分类号： C07D413/00 ,  C07D251/48 ,  C07D239/02 ,  C07D213/84 ,  A61K31/535 ,  A01N43/66 ,  A01N43/54 ,  A01N43/40

CPC分类号： C07D239/58 ,  C07D213/85 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04

摘要： The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

公开(公告)号：EP2097419B1

公开(公告)日：2011-05-25

申请号：EP08832770.5

申请日：2008-12-22

申请人： Exelixis, Inc.

发明人： BROWN, S., David ,  DU, Hongwang ,  FRANZINI, Maurizio ,  GALAN, Adam, Antoni ,  HUANG, Ping ,  KEARNEY, Patrick ,  KIM, Moon, Hwan ,  KOLTUN, Elena, S. ,  RICHARDS, Steven, James ,  TSUHAKO, Amy, L. ,  ZAHARIA, Cristiana, A.

IPC分类号： C07D491/04

CPC分类号： C07D491/04

摘要： A compound according to formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3a, R3b, R3c and R3d are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：EP2097419A1

公开(公告)日：2009-09-09

申请号：EP08832770.5

申请日：2008-12-22

申请人： Exelixis, Inc.

发明人： BROWN, S., David ,  DU, Hongwang ,  FRANZINI, Maurizio ,  GALAN, Adam, Antoni ,  HUANG, Ping ,  KEARNEY, Patrick ,  KIM, Moon, Hwan ,  KOLTUN, Elena, S. ,  RICHARDS, Steven, James ,  TSUHAKO, Amy, L. ,  ZAHARIA, Cristiana, A.

IPC分类号： C07D491/04

CPC分类号： C07D491/04

摘要： A compound according to formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3a, R3b, R3c and R3d are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：EP1848719A1

公开(公告)日：2007-10-31

申请号：EP05855490.8

申请日：2005-12-27

申请人： Exelixis, Inc.

发明人： RICE, Kenneth, D. ,  CO, Erick, Wang ,  KIM, Moon, Hwan ,  BANNEN, Lynn, Canne ,  BUSSENIUS, Joerg ,  LE, Donna ,  TSUHAKO, Amy, Lew ,  NUSS, John ,  WANG, Yong ,  XU, Wei ,  KLEIN, Rhett, Ronald

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D487/04

摘要： The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

公开(公告)号：EP2320895A2

公开(公告)日：2011-05-18

申请号：EP09774582.2

申请日：2009-07-02

申请人： Exelixis, Inc.

发明人： BAHCECI, Suleyman ,  CHAN, Bryan ,  CHAN, Diva, Sze-ming ,  CHEN, Jeff ,  FORSYTH, Timothy, Patrick ,  FRANZINI, Maurizio ,  JAMMALAMADAKA, Vasu ,  JEONG, Joon, Won ,  JONES, Lisa, Renee ,  KELLEY, Ryan, Michael ,  KIM, Moon, Hwan ,  LEAHY, James, W. ,  MAC, Morrison, B. ,  NOGUCHI, Robin, Tammie ,  RAO, Pallavi ,  RIDGWAY, Brian, Hugh ,  XU, Wei ,  WANG, Yong

IPC分类号： A61K31/437 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04 ,  C07D498/14 ,  C07D491/107 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： A compound according to Formula I : or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：EP1581309A2

公开(公告)日：2005-10-05

申请号：EP03812437.6

申请日：2003-11-14

申请人： Exelixis, Inc.

发明人： BANNEN, Lynne, Canne ,  BROWN, S., David ,  CHENG, Wei ,  CO, Erick, Wang ,  NUSS, John, M. ,  KIM, Moon, Hwan ,  KLEIN, Rhett Ronald ,  LE, Donna, T. ,  LEW, Amy ,  MAC, Morrison, B. ,  PARKS, Jason Jevious ,  WEN,, Zhaoyang ,  XU, Wei

IPC分类号： A61P35/00 ,  A61K31/445 ,  A61K31/44 ,  A61K31/52 ,  A61K31/415 ,  A61K31/535 ,  C07D235/00 ,  C07D401/00 ,  C07D413/00 ,  C07D471/00 ,  C07D487/00

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D413/14 ,  C07D451/04

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. More specifically, the invention provides oxindole derivatives which inhibit, regulate and/or modulate kinase receptor, particularly VEGF receptor 2 (Flk-1/KDR), FGFR1, and PDGFR (alpha and beta), signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

公开(公告)号：EP1663204B1

公开(公告)日：2014-05-07

申请号：EP04782473.5

申请日：2004-08-27

申请人： Exelixis, Inc.

发明人： CHENG, Wei ,  CO, Erick, Wang ,  KIM, Moon, Hwan ,  KLEIN, Rhett, Ronald ,  LE, Donna, T. ,  LEW, Amy ,  NUSS, John, M. ,  XU, Wei ,  BAJJALIEH, William

IPC分类号： C07D257/04 ,  C07D403/04 ,  C07D215/14 ,  C07D401/12 ,  C07D403/12 ,  C07D239/26 ,  C07D405/12 ,  C07D409/12 ,  C07D241/12 ,  C07D417/12 ,  C07D249/06 ,  C07D471/04 ,  C07D261/08 ,  C07D207/333 ,  C07D209/12 ,  C07D213/30 ,  C07D307/42 ,  C07D307/91 ,  C07D207/404 ,  A61K31/41 ,  A61K31/495

CPC分类号： A61K31/41 ,  A61K31/495 ,  C07D207/333 ,  C07D207/404 ,  C07D209/12 ,  C07D213/30 ,  C07D215/14 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D257/04 ,  C07D261/08 ,  C07D307/42 ,  C07D307/91 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

公开(公告)号：EP1678168B1

公开(公告)日：2012-07-11

申请号：EP04796443.2

申请日：2004-10-22

申请人： Exelixis, Inc.

发明人： CHENG, Wei ,  CO, Erick, Wang ,  KIM, Moon, Hwan ,  KLEIN, Rhett, Ronald ,  LE, Donna, T. ,  LEW, Amy ,  NUSS, John, M. ,  XU, Wei

IPC分类号： C07D413/00 ,  C07D251/48 ,  C07D239/02 ,  C07D213/84 ,  A61K31/535 ,  A01N43/66 ,  A01N43/54 ,  A01N43/40

CPC分类号： C07D239/58 ,  C07D213/85 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04

摘要： The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.