公开(公告)号：EP1940792B1

公开(公告)日：2014-06-04

申请号：EP06825696.5

申请日：2006-10-05

申请人： Exelixis, Inc.

发明人： KEARNEY, Patrick ,  BROWN, S. David ,  KOLTUN, Elena, S.

IPC分类号： C07D213/81 ,  C07D257/04 ,  C07D307/68 ,  C07D307/93 ,  C07D333/38

CPC分类号： C07D409/12 ,  C07C233/63 ,  C07C2601/08 ,  C07D213/81 ,  C07D257/04 ,  C07D307/68 ,  C07D307/93 ,  C07D333/38 ,  C07D333/70 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

公开(公告)号：EP1979329A2

公开(公告)日：2008-10-15

申请号：EP07717132.0

申请日：2007-01-30

申请人： Exelixis, Inc.

发明人： MANN, Grace ,  AAY, Naing ,  ARCALAS, Arlyn ,  BROWN, S. David ,  CHAN, Wai Ki Vicky ,  CHEN, Jeff ,  DU, Hongwang ,  EPSHTEYN, Sergey ,  FORSYTH, Timothy, Patrick ,  GALAN, Adam A. ,  HUYNH, Tai Phat ,  IBRAHIM, Mohamed Abdulkader ,  JOHNSON, Henry William Beecroft ,  KANE, Brian ,  KEARNEY, Patrick ,  KIM, Byung Gyu ,  KOLTUN, Elena ,  LEAHY, James W. ,  LEE, Matthew Sangyup ,  LEWIS, Gary L. ,  MEYR, Lisa E. ,  NOGUCHI, Robin Tammie ,  PACK, Michael ,  RIDGWAY, Brian Hugh ,  SHI, Xian ,  WOOLFREY, John ,  ZHOU, Peiwen

IPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04

摘要： This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：EP2074103A1

公开(公告)日：2009-07-01

申请号：EP08743264.7

申请日：2008-04-25

申请人： Exelixis, Inc. ,  Koltun, Elena S.

发明人： KOLTUN, Elena S. ,  TSUHAKO, Amy L. ,  AAY, Naing ,  BROWN, S. David ,  CHAN, Wai Ki Vicky ,  DU, Hongwang ,  HUANG, Ping ,  KANE, Brian ,  KEARNEY, Patrick ,  KIM, Moon Hwan ,  PACK, Michael ,  XU, Wei ,  ZHOU, Peiwen

IPC分类号： C07D239/36 ,  C07D403/12 ,  C07D413/04 ,  C07D409/04 ,  C07D407/12 ,  C07D409/12 ,  A61K31/513 ,  A61P35/00 ,  C07D213/64

CPC分类号： C07D213/64 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04

摘要： A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.

公开(公告)号：EP1940792A2

公开(公告)日：2008-07-09

申请号：EP06825696.5

申请日：2006-10-05

申请人： Exelixis, Inc.

发明人： KEARNEY, Patrick ,  BROWN, S. David ,  KOLTUN, Elena, S.

IPC分类号： C07D213/81 ,  C07D257/04 ,  C07D307/68 ,  C07D307/93 ,  C07D333/38

CPC分类号： C07D409/12 ,  C07C233/63 ,  C07C2601/08 ,  C07D213/81 ,  C07D257/04 ,  C07D307/68 ,  C07D307/93 ,  C07D333/38 ,  C07D333/70 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.

公开(公告)号：EP1608373A2

公开(公告)日：2005-12-28

申请号：EP04757665.7

申请日：2004-03-19

申请人： Exelixis Inc.

发明人： PARKS, Jason Jevious ,  BANNEN, Lynne Canne ,  BROWN, S. David ,  CHENG, Wei ,  CHEUNG, Atwood Kim ,  DALRYMPLE, Lisa Esther ,  EPSHTEYN, Sergey ,  IBRAHIM, Mohamed Abdulkader ,  JAMMALAMADAKA, Vasu ,  LEAHY, James William ,  LEWIS, Gary Lee ,  MAC, Morrison B. ,  MANN, Larry W. ,  NUSS, John M. ,  NOGUCHI, Robin Tammie ,  RIDGWAY, Brian Hugh ,  SANGALANG, Joan C. ,  SCHNEPP, Kevin Luke ,  SHI, Xian ,  WILLIAMS, Matthew A. ,  XU, Wei ,  KHOURY, Richard

IPC分类号： A61K31/496 ,  C07D417/04 ,  C07D417/14

CPC分类号： A61K31/496 ,  C07D213/75 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14

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. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.