公开(公告)号：EP1773768A2

公开(公告)日：2007-04-18

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hu ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/325 ,  A61K31/40

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

公开(公告)号：EP1773768B8

公开(公告)日：2018-12-26

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hui ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61P3/00 ,  A61P15/08 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

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：EP2370438A1

公开(公告)日：2011-10-05

申请号：EP09768463.3

申请日：2009-12-03

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHAN, Diva Sze-ming ,  GU, Xiao-hui ,  MAC, Morrison, B. ,  NG, Stephanie ,  WANG, Tie-lin ,  WANG, Yong ,  XU, Wei

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P37/00

CPC分类号： C07D471/04

摘要： The invention is directed to Compounds of Formula (I) as well as methods of making and using the compounds.

公开(公告)号：EP1461313B1

公开(公告)日：2009-08-05

申请号：EP02784794.6

申请日：2002-12-13

申请人： Exelixis, Inc.

发明人： BROWN, S., David ,  CANNE, Lynne ,  CO, Erick, W. ,  JAMMALAMADAKA, Vasu ,  KHOURY, Richard, G. ,  KIM, Moon Hwan ,  LE, Donna, T. ,  LEW, Amy ,  MAC, Morrison, B. ,  MAMO, Shumeye ,  NUSS, John, M. ,  PRISBYLLA, Michael, P. ,  XU, Wei

IPC分类号： C07C311/19 ,  C07C311/29 ,  C07C259/06 ,  C07C259/08 ,  C07D213/32 ,  C07D213/68 ,  A61K31/16 ,  A61K31/44 ,  A61P19/02 ,  A61P35/00

CPC分类号： C07D409/04 ,  C07C311/29 ,  C07C2601/14 ,  C07D207/09 ,  C07D211/34 ,  C07D213/56 ,  C07D213/65 ,  C07D213/70 ,  C07D233/48 ,  C07D233/64 ,  C07D295/13 ,  C07D295/15 ,  C07D295/185 ,  C07D295/215 ,  C07D311/70

摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chorides and ADAM-10 modulators therefrom.

摘要翻译： 本发明提供了可用于抑制ADAM-10蛋白质的化合物。 这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。 本发明还包括药物组合物，其包含根据本发明的一种或多种ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症，关节炎和与血管生成有关的疾病。 相应地，本发明还包括治疗癌症形式，关节炎和与血管生成相关的疾病的方法，其中ADAM-10起关键作用。 本发明还提供从其制备双芳基醚磺酰氯和ADAM-10调节剂的方法。

公开(公告)号：EP1874759A1

公开(公告)日：2008-01-09

申请号：EP06749361.9

申请日：2006-04-06

申请人： Exelixis, Inc.

发明人： FORSYTH, Timothy, Patrick ,  MAC, Morrison, B. ,  LEAHY, James, William ,  NUSS, John, M. ,  XU, Wei

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/47 ,  A61K31/517

CPC分类号： C07D215/233

摘要： The present invention provides compounds, which have activity for modulating protein kinase enzymatic activity and are potentially useful for modulating cellular activities such as, e.g., proliferation, differentiation, programmed cell death, migration and chemoinvasion. The present invention also provides compositions containing such compounds, and methods for producing and using such compounds and compositions.

公开(公告)号：EP1773768B1

公开(公告)日：2018-08-22

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hui ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61P3/00 ,  A61P15/08 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

公开(公告)号：EP1931645B1

公开(公告)日：2014-07-16

申请号：EP06836252.4

申请日：2006-10-09

申请人： Exelixis, Inc.

发明人： BAJJALIEH, William ,  CANNE BANNEN, Lynne ,  BROWN, S., David ,  KEARNEY, Patrick ,  MAC, Morrison, B. ,  MARLOWE, Charles, K. ,  NUSS, John, M. ,  TESFAI, Zerom ,  WANG, Yong ,  XU, Wei

IPC分类号： C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/498 ,  A61K31/4985 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D241/44 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  Y02P20/55

公开(公告)号：EP1511488A2

公开(公告)日：2005-03-09

申请号：EP03736979.0

申请日：2003-06-11

申请人： Exelixis, Inc.

发明人： BANNEN, Lynne, Canne ,  CO, Erick, W. ,  JAMMALAMADAKA, Vasu ,  NUSS, John, M. ,  KIM, Moon, Hwan ,  LE, Donna, Tra ,  LEW, Amy ,  MAC, Morrison, B. ,  MAMO, Shumeye ,  WEN, Zhaoyang ,  XU, Wei ,  KHOURY, Richard George

IPC分类号： A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12

CPC分类号： C07D241/04 ,  C07C309/87 ,  C07D213/70 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D413/06

摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.

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.