公开(公告)号：EP2074114A1

公开(公告)日：2009-07-01

申请号：EP08767429.7

申请日：2008-04-24

申请人： Exelixis, Inc.

发明人： KOLTUN, Elena S. ,  KEARNEY, Patrick ,  AAY, Naing ,  ARCALAS, Arlyn ,  CHAN, Wai Ki Vicky ,  CURTIS, Jeffry Kimo ,  DU, Hongwang ,  HUANG, Ping ,  KANE, Brian ,  KIM, Moon Hwan ,  PACK, Michael ,  TSUHAKO, Amy L. ,  XU, Wei ,  ZAHARIA, Cristiana A. ,  ZHOU, Peiwen

IPC分类号： C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/513 ,  A61P35/00

CPC分类号： C07D405/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

摘要： A compound having Formula I :or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Fomula I are inhibitors of Casein kinase II (CK2) pathways.

公开(公告)号：EP1948617B1

公开(公告)日：2011-07-27

申请号：EP06826578.4

申请日：2006-10-23

申请人： Exelixis, Inc.

发明人： RICE, Kenneth D. ,  ANAND, Neel Kumar ,  ARCALAS, Arlyn ,  BLAZEY, Charles M. ,  BUSSENIUS, Joerg ,  CHAN, Wai Ki Vicky ,  DU, Hongwang ,  EPSHTEYN, Sergey ,  IBRAHIM, Mohamed Abdulkader ,  KEARNEY, Patrick ,  KENNEDY, Abigail R. ,  KIM, Moon Hwan ,  MANALO, Jean-Claire Limun ,  PETO, Csaba J. ,  TSANG, Tsze H. ,  TSUHAKO, Amy Lew ,  ZHOU, Peiwen ,  KOLTUN, Elena, S.

IPC分类号： C07D237/36 ,  C07D239/46 ,  C07D401/04 ,  C07D403/04 ,  A61K31/505 ,  A61K31/506 ,  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.

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：EP2074114B1

公开(公告)日：2013-03-06

申请号：EP08767429.7

申请日：2008-04-24

申请人： Exelixis, Inc.

发明人： KOLTUN, Elena S. ,  KEARNEY, Patrick ,  AAY, Naing ,  ARCALAS, Arlyn ,  CHAN, Wai Ki Vicky ,  CURTIS, Jeffry Kimo ,  DU, Hongwang ,  HUANG, Ping ,  KANE, Brian ,  KIM, Moon Hwan ,  PACK, Michael ,  TSUHAKO, Amy L. ,  XU, Wei ,  ZAHARIA, Cristiana A. ,  ZHOU, Peiwen

IPC分类号： C07D403/04 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/513 ,  A61P35/00

CPC分类号： C07D405/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

公开(公告)号：EP2061768A2

公开(公告)日：2009-05-27

申请号：EP07839028.3

申请日：2007-09-28

申请人： Exelixis, Inc.

发明人： GALAN, Adam Antoni ,  CHEN, Jeff ,  DU, Hongwang ,  FORSYTH, Timothy ,  HUYNH, Tai Phat ,  JOHNSON, Henry William Beecroft ,  KEARNEY, Patrick ,  LEAHY, James W. ,  LEE, Matthew Sangyup ,  MANN, Grace ,  RIDGWAY, Brian Hugh ,  TAKEUCHI, Craig Stacy ,  ZHOU, Peiwen

IPC分类号： C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  A61K31/4178 ,  A61K31/4184 ,  A61P35/02 ,  A61P35/00

CPC分类号： C07D405/14 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.

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：EP1948617A2

公开(公告)日：2008-07-30

申请号：EP06826578.4

申请日：2006-10-23

申请人： Exelixis, Inc.

发明人： RICE, Kenneth D. ,  ANAND, Neel Kumar ,  ARCALAS, Arlyn ,  BLAZEY, Charles M. ,  BUSSENIUS, Joerg ,  CHAN, Wai Ki Vicky ,  DU, Hongwang ,  EPSHTEYN, Sergey ,  IBRAHIM, Mohamed Abdulkader ,  KEARNEY, Patrick ,  KENNEDY, Abigail R. ,  KIM, Moon Hwan ,  MANALO, Jean-Claire Limun ,  PETO, Csaba J. ,  TSANG, Tsze H. ,  TSUHAKO, Amy Lew ,  ZHOU, Peiwen ,  KOLTUN, Elena, S.

IPC分类号： C07D237/36 ,  C07D239/46 ,  C07D401/04 ,  C07D403/04 ,  A61K31/505 ,  A61K31/506 ,  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.