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：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：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：EP1841760B1

公开(公告)日：2011-08-10

申请号：EP05855893.3

申请日：2005-12-28

申请人： Exelixis, Inc.

发明人： CHEN, Jeff ,  DALRYMPLE MEYR, Lisa, Esther ,  EPSHTEYN, Sergey ,  FORSYTH, Timothy, Patrick ,  HUYNH, Tai, Phat ,  IBRAHIM, Mohamed, Abdulkader ,  LEAHY, James, W. ,  LEWIS, Gary, Lee ,  MANN, Grace ,  MANN, Larry, W. ,  NOGUCHI, Robin, Tammie ,  RIDGWAY, Brian, Hugh ,  SANGALANG, Joan, Cruz ,  SCHNEPP, Kevin, Luke ,  SHI, Xian ,  TAKEUCHI, Craig, Stacy ,  WILLIAMS, Matthew, Alan ,  NUSS, John ,  CHEUNG, Atwood, K.

IPC分类号： C07D403/14 ,  C07D401/12 ,  C07D413/14 ,  A61K31/495 ,  A61K31/42 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D413/14 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14 ,  C07D487/04

摘要： The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wild­type Abl. 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. A compound of formula (I), or a farmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O-R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O-C1-C6 alkyl, or N(R13)-C(O)-C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6 alkyl-NR,15R16, NRI5R,6, C1-C6 alkoxy, -N(R13)-(CH2)n-­NR15R16, -C(O)O-C1-C6 alkyl, -O-(CH2)n-NR15R16, -C(O)-C1-C6 alkyl, -C0-C6-alkyl-R21, -O-R21, -C(O)-R21, -O-(CH2)n-R21, -C(O)-NR13R14, -C(O)-N(R13)-aryl, -C(O)-N(R13)­(CH2)n-NR15R16, -C(O)-N(R13)-(CH2)n-aryl -C(O)-N(R13)-(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, -S-R2a, or -0-R2a

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：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：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：EP1841760A2

公开(公告)日：2007-10-10

申请号：EP05855893.3

申请日：2005-12-28

申请人： Exelixis, Inc.

发明人： CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  EPSHTEYN, Sergey ,  FORSYTH, Timothy, Patrick ,  HUYNH, Tai, Phat ,  IBRAHIM, Mohamed, Abdulkader ,  LEAHY, James, W. ,  LEWIS, Gary, Lee ,  MANN, Grace ,  MANN, Lary, W. ,  NOGUCHI, Robin, Tammie ,  RIDGWAY, Brian, Hugh ,  SANGALANG, Joan, Cruz ,  SCHNEPP, Kevin, Luke ,  SHI, Xian ,  TAKEUCHI, Craig, Stacy ,  WILLIAMS, Matthew, Alan ,  NUSS, John ,  CHEUNG, Atwood, K.

IPC分类号： C07D403/14 ,  C07D401/12 ,  C07D413/14 ,  A61K31/495 ,  A61K31/42 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D413/14 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14 ,  C07D487/04

摘要： The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wild­type Abl. 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. A compound of formula (I), or a farmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O-R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O-C1-C6 alkyl, or N(R13)-C(O)-C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6 alkyl-NR,15R16, NRI5R,6, C1-C6 alkoxy, -N(R13)-(CH2)n-­NR15R16, -C(O)O-C1-C6 alkyl, -O-(CH2)n-NR15R16, -C(O)-C1-C6 alkyl, -C0-C6-alkyl-R21, -O-R21, -C(O)-R21, -O-(CH2)n-R21, -C(O)-NR13R14, -C(O)-N(R13)-aryl, -C(O)-N(R13)­(CH2)n-NR15R16, -C(O)-N(R13)-(CH2)n-aryl -C(O)-N(R13)-(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, -S-R2a, or -0-R2a