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：WO2004085425A1

公开(公告)日：2004-10-07

申请号：PCT/US2004/008809

申请日：2004-03-22

Applicant: AMGEN INC

Inventor： DIPIETRO, Lucian V. ,  HARMANGE, Jean-Christophe ,  ASKEW, JR., Benny C. ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  HABGOOD, Gregory J. ,  KIM, Joseph L. ,  PATEL, Vinod F. ,  POTASHMAN, Michele ,  VAN DER PLAS, Simon

IPC: C07D401/12

CPC classification number: C07D401/12 ,  C07D235/30 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.

Abstract translation: 本发明涉及式（I）至（III）的化合物，其中取代基如说明书中所定义。 这些化合物具有激酶抑制活性，例如VEGFR / KDR抑制活性。 因此，式（I）至（III）的化合物可用于预防和治疗血管发生相关疾病，眼科病症，增殖性疾病，炎性疾病和其他病理状况，如本说明书所述。