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：EP2121621A1

公开(公告)日：2009-11-25

申请号：EP07865385.4

申请日：2007-12-07

申请人： Exelixis, Inc.

发明人： BOREN, Brant Clayton ,  BUSCH, Brett B. ,  GU, Xiao-hui ,  JAMMALAMADAKA, Vasu ,  LU, Shao-Po ,  MARTIN, Richard ,  MOHAN, Raju ,  SCHWEIGER, Edwin ,  STEVENS, William C. Jr. ,  WANG, Tie-lin ,  XIE, Yinong ,  XU, Wei

IPC分类号： C07D233/90 ,  C07D231/10 ,  A61K31/415 ,  A61K31/4164 ,  A61P3/10

CPC分类号： C07D233/90 ,  C07D231/10

摘要： Compounds of the invention are disclosed, such as compounds of formulae LX - LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

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：EP1678121A2

公开(公告)日：2006-07-12

申请号：EP04796442.4

申请日：2004-10-22

申请人： Exelixis, Inc.

发明人： BALY, Deborah, Lynn ,  GALAN, Adam, Antoni ,  IBRAHIM, Mohamed, Abdulkader ,  JAEGER, Christopher ,  KEARNEY, Patrick ,  LEAHY, James, William ,  LEWIS, Gary, Lee ,  MCMILLAN, Kirk ,  NOGUCHI, Robin, Tammie ,  NUSS, John, M. ,  PARKS, Jason, Jevious ,  SCHNEPP, Kevin, Luke ,  SHI, Xian ,  WILLIAMS, Matthew, Alan ,  XU, Wei ,  ZHANG, Wentao

IPC分类号： C07C233/64 ,  C07C275/06 ,  C07C275/28 ,  A61K31/16 ,  A61K31/17

CPC分类号： C07C237/22 ,  C07C275/16 ,  C07C275/34 ,  C07C2602/10 ,  C07D207/16 ,  C07D209/20 ,  C07D209/42 ,  C07D209/44 ,  C07D213/56 ,  C07D213/75 ,  C07D215/48 ,  C07D215/54 ,  C07D217/06 ,  C07D217/22 ,  C07D233/56 ,  C07D233/58 ,  C07D263/32 ,  C07D277/46 ,  C07D277/66 ,  C07D277/82 ,  C07D295/155 ,  C07D295/185 ,  C07D319/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The invention provides compounds and methods for inhibition of kinases, such as those of the TAO family, more specifically KIAA1361, TAO, and JIK kinases. The 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 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：EP4294804A1

公开(公告)日：2023-12-27

申请号：EP22707995.1

申请日：2022-02-18

申请人： Exelixis, Inc.

发明人： BANNEN, Lynne ,  XU, Wei ,  RAUB, Andrew ,  JIANG, Faming ,  JEONG, Joon Won ,  TSO, Kin ,  SALVANT, Justin

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/4375 ,  A61K31/519

公开(公告)号：EP3743068A1

公开(公告)日：2020-12-02

申请号：EP19704968.7

申请日：2019-01-25

申请人： Exelixis, Inc.

发明人： BANNEN, Lynne Canne ,  BUI, Minna ,  JIANG, Faming ,  WANG, Yong ,  XU, Wei

IPC分类号： A61K31/4375 ,  A61K31/517 ,  C07D239/88 ,  C07D471/04 ,  A61P35/00

公开(公告)号：EP3329918A2

公开(公告)日：2018-06-06

申请号：EP17190013.7

申请日：2004-09-24

申请人： Exelixis, Inc.

发明人： BANNEN, Lynne Canne ,  CHAN, Diva Sze-Ming ,  CHEN, Jeff ,  DALRYMPLE, Lisa Esther ,  FORSYTH, Timothy Patrick ,  HUYNH, Tai Phat ,  JAMMALAMADAKA, Vasu ,  KHOURY, Richard George ,  LEAHY, James William ,  MAC, Morrison B. ,  MANN, Grace ,  MANN, Larry W. ,  NUSS, John M. ,  PARKS, Jason Jevious ,  TAKEUCHI, Craig Stacy ,  WANG, Yong ,  XU, Wei

IPC分类号： A61K31/47 ,  A61P35/00 ,  C07D215/22 ,  A61K31/4709 ,  A61K31/517

CPC分类号： C07D215/233 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  C07D215/22 ,  C07D215/36 ,  C07D215/38 ,  C07D215/46 ,  C07D239/88 ,  C07D239/94 ,  C07D295/15 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C12Q1/485 ,  G01N2500/04 ,  Y02A50/393

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 quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, 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. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：EP3174854A1

公开(公告)日：2017-06-07

申请号：EP15762798.5

申请日：2015-07-31

申请人： Exelixis, Inc.

发明人： XU, Wei ,  DONNELLY, David J. ,  CHOW, Patrick L. ,  HENLEY, Benjamin J.

IPC分类号： C07D215/22

CPC分类号： C07D215/233 ,  C07D215/22

摘要： The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.

摘要翻译： 本发明涉及制备卡博替的方法（环丙烷-1,1-二羧酸[4-（6,7-二甲氧基 - 喹啉-4-基氧基）-phenylo]酰胺（4-氟 - 苯基）酰胺）和18F 标记卡博替。

公开(公告)号：EP2970126A1

公开(公告)日：2016-01-20

申请号：EP14721149.4

申请日：2014-03-17

申请人： Exelixis, Inc.

发明人： AFTAB, Dana, T. ,  NAGANATHAN, Sriram ,  XU, Wei ,  LACY, Steven ,  NGUYEN, Linh

IPC分类号： C07D215/22 ,  C07C305/24 ,  C07C233/60 ,  A61K31/47 ,  A61P35/00

CPC分类号： C07D215/22 ,  C07C233/60 ,  C07C305/24 ,  C07C2601/02 ,  C07D215/60 ,  G01N33/487 ,  G01N2570/00

摘要： The invention relates to metabolites of cabozantinib (I) as well as uses thereof.

摘要翻译： 本发明涉及卡泊沙坦（I）的代谢物及其用途。