公开(公告)号：WO2007076092A3

公开(公告)日：2007-07-05

申请号：PCT/US2006/049187

申请日：2006-12-22

Applicant: AMGEN INC. ,  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

Inventor： 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: C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/435

Abstract: 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 R 1 is Formula (II), (III) or (IV) and A 1 , A 2 , A 3 , A 4 , X, Z, Z', R 1 , R 2 , R 3 , R 4 , R 5 and R 6 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：WO2003070727A1

公开(公告)日：2003-08-28

申请号：PCT/US2003/004537

申请日：2003-02-13

Applicant: AMGEN INC.

Inventor： 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: C07D417/14

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

Abstract: 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.

Abstract translation: 式（VI）的选择的噻唑基脲化合物对于预防和治疗诸如细胞增殖或细胞凋亡介导的疾病的疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及stoke，癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：WO2006039718A3

公开(公告)日：2006-04-13

申请号：PCT/US2005/035873

申请日：2005-10-03

Applicant: AMGEN INC

Inventor： 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. ,  TEMPEST, Paul A. ,  MASSE, Craig E. ,  BUCKNER, William H. ,  HERBERICH, Bradley J. ,  GRACEFFA, Russell ,  ZHANG, Dawei ,  XU, Shimin ,  SHAM, Kelvin ,  RZASA, Robert M. ,  FALSEY, James Richard ,  CHAKRABARTI, Partha P. ,  CAO, Guo-qiang ,  TOMLINSON, Susan Ann ,  PETTUS, Liping H. ,  SMITH, Adrian Leonard ,  PARAS, Nick A. ,  LIU, Gang ,  DEMORIN, Frenel F. ,  TASKER, Andrew ,  REED, Anthony

IPC: C07D239/84 ,  C07D239/95 ,  C07D401/12 ,  C07D409/04 ,  C07D405/12 ,  C07D409/14 ,  C07D405/04 ,  C07D403/10 ,  C07D401/04 ,  C07D471/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D409/12 ,  C07D215/12

Abstract: 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.

公开(公告)号：WO2006066172A1

公开(公告)日：2006-06-22

申请号：PCT/US2005/045863

申请日：2005-12-16

Applicant: AMGEN, INC. ,  SMITH, Adrian, Leonard ,  BRENNAN, Paul, Edward ,  DEMORIN, Frenel, Fils ,  LIU, Gang ,  PARAS, Nick, A. ,  RETZ, Daniel, Martin

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

IPC: C07D409/14 ,  A61K31/381 ,  C07D333/16

CPC classification number: C07D417/14 ,  C07D409/14

Abstract: The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

Abstract translation: 本发明涉及可用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。 本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

公开(公告)号：WO2008153947A3

公开(公告)日：2008-12-18

申请号：PCT/US2008/007132

申请日：2008-06-05

Applicant: AMGEN INC. ,  SMITH, Adrian L. ,  DOHERTY, Elizabeth M. ,  HUANG, Qi ,  LIU, Gang

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

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

Abstract: 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 A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , A 9 , bond B, X, rings Z 1 and Z 2 , R 1 and R 3 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.