公开(公告)号：EP2170887A2

公开(公告)日：2010-04-07

申请号：EP08768206.8

申请日：2008-06-05

申请人： Amgen Inc.

发明人： SMITH, Adrian L. ,  DOHERTY, Elizabeth M. ,  HUANG, Qi ,  LIU, Gang

IPC分类号： C07D473/00 ,  C07D487/04 ,  A61K31/519 ,  A61K31/52 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D473/00

摘要： The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1836174B1

公开(公告)日：2013-02-27

申请号：EP05818381.5

申请日：2005-10-03

申请人： AMGEN INC.

发明人： PATEL, Vinod F. ,  KIM, Joseph L. ,  GEUNS-MEYER, Stephanie D. ,  CHAFFEE, Stuart C. ,  CEE, Victor J. ,  HODOUS, Brian L. ,  BELLON, Steven ,  HARMANGE, Jean-christophe ,  OLIVIERI, Philip R. ,  THAMAN, Maya C. ,  DIMAURO, Erin F. ,  BUCHANAN, John L. ,  MCGOWAN, David C. ,  ALBRECHT, Brian K. ,  DEAK, Holly L. ,  BEMIS, Jean E. ,  WHITE, Ryan ,  MARTIN, Matthew W. ,  HABGOOD, Gregory J. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  TEMPEST, Paul A. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-giang ,  TOMLINSON, Susan Ann ,  PETTUS, Liping H. ,  SMITH, Adrian Leonard ,  PARAS, Nick A. ,  LIU, Gang ,  DEMORIN, Frenel F. ,  TASKER, Andrew ,  REED, Anthony

IPC分类号： C07D239/84

CPC分类号： C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A 1 , A 2 , A 3 , B, R 1 , R 2 , R 3 and R 4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1976836A2

公开(公告)日：2008-10-08

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1309589B1

公开(公告)日：2006-03-15

申请号：EP01964009.3

申请日：2001-08-15

申请人： AMGEN INC.

发明人： SANTORA, Vincent ,  ASKEW, Benny ,  GHOSE, Arup ,  HAGUE, Andrew ,  KIM, Tae, Seong ,  LABER, Ellen ,  LI, Aiwen ,  LIAN, Brian ,  LIU, Gang ,  NORMAN, Mark, Henry ,  SMITH, Leon ,  TASKER, Andrew ,  TEGLEY, Christopher ,  YANG, Kevin

IPC分类号： C07D417/14

CPC分类号： C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：EP1976836B1

公开(公告)日：2012-08-22

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/435 ,  A61K31/495 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D413/04

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1831207B1

公开(公告)日：2012-11-14

申请号：EP05854551.8

申请日：2005-12-16

申请人： Amgen Inc.

发明人： SMITH, Adrian, Leonard ,  BRENNAN, Paul, Edward ,  DEMORIN, Frenel, Fils ,  LIU, Gang ,  PARAS, Nick, A. ,  RETZ, Daniel, Martin ,  RAINBEAU, Elizabeth

IPC分类号： C07D409/14 ,  C07D417/14

CPC分类号： C07D417/14 ,  C07D409/14

公开(公告)号：EP1483263A1

公开(公告)日：2004-12-08

申请号：EP03711046.7

申请日：2003-02-13

申请人： Amgen Inc.

发明人： SANTORA, Vincent ,  ASKEW, Benny, C. ,  DE MORIN, Frenel, F. ,  HAGUE, Andrew ,  LABER, Ellen ,  LI, Aiwen ,  LIU, Gang ,  LOPEZ, Patricia ,  NOMAK, Rana ,  TEGLEY, Christopher ,  YANG, Kevin

IPC分类号： C07D417/14 ,  C07D471/04 ,  C07D453/02 ,  C07D417/04 ,  C07D491/10 ,  C07D277/48 ,  A61K31/47

CPC分类号： C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D453/06 ,  C07D471/04 ,  C07D491/10

摘要： Selected thiazolyl urea compounds of formula (VI) are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：EP1836174B2

公开(公告)日：2019-10-02

申请号：EP05818381.5

申请日：2005-10-03

申请人： AMGEN INC.

发明人： PATEL, Vinod F. ,  KIM, Joseph L. ,  GEUNS-MEYER, Stephanie D. ,  CHAFFEE, Stuart C. ,  CEE, Victor J. ,  HODOUS, Brian L. ,  BELLON, Steven ,  HARMANGE, Jean-christophe ,  OLIVIERI, Philip R. ,  THAMAN, Maya C. ,  DIMAURO, Erin F. ,  BUCHANAN, John L. ,  MCGOWAN, David C. ,  ALBRECHT, Brian K. ,  DEAK, Holly L. ,  BEMIS, Jean E. ,  WHITE, Ryan ,  MARTIN, Matthew W. ,  HABGOOD, Gregory J. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  TEMPEST, Paul A. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-giang ,  TOMLINSON, Susan Ann ,  PETTUS, Liping H. ,  SMITH, Adrian Leonard ,  PARAS, Nick A. ,  LIU, Gang ,  DEMORIN, Frenel F. ,  TASKER, Andrew ,  REED, Anthony

IPC分类号： C07D239/84

公开(公告)号：EP1976836B9

公开(公告)日：2013-02-06

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/435 ,  A61K31/495 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D413/04

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

公开(公告)号：EP1836174A2

公开(公告)日：2007-09-26

申请号：EP05818381.5

申请日：2005-10-03

申请人： AMGEN INC.

发明人： PATEL, Vinod F. ,  KIM, Joseph L. ,  GEUNS-MEYER, Stephanie D. ,  CHAFFEE, Stuart C. ,  CEE, Victor J. ,  HODOUS, Brian L. ,  BELLON, Steven ,  HARMANGE, Jean-christophe ,  OLIVIERI, Philip R. ,  THAMAN, Maya C. ,  DIMAURO, Erin F. ,  BUCHANAN, John L. ,  MCGOWAN, David C. ,  ALBRECHT, Brian K. ,  DEAK, Holly L. ,  BEMIS, Jean E. ,  WHITE, Ryan ,  MARTIN, Matthew W. ,  HABGOOD, Gregory J. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  TEMPEST, Paul A. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-giang ,  TOMLINSON, Susan Ann ,  PETTUS, Liping H. ,  SMITH, Adrian Leonard ,  PARAS, Nick A. ,  LIU, Gang ,  DEMORIN, Frenel F. ,  TASKER, Andrew ,  REED, Anthony

IPC分类号： C07D239/84

CPC分类号： C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I, wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.