公开(公告)号：WO2010104933A1

公开(公告)日：2010-09-16

申请号：PCT/US2010/026796

申请日：2010-03-10

Applicant: MERCK SHARP & DOHME CORP. ,  BANYU PHARMACEUTICAL CO., LTD. ,  FAN, Weiming ,  HAXELL, Thomas, F. N. ,  JENKS, Matthew, G. ,  KAWANISHI, Nobuhiko ,  LEE, Shuliang ,  LIU, Hao ,  MALASKA, Michael, J. ,  MOORE, Joseph, A., III ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  PANDI, Bharathi ,  PEEL, Michael, R. ,  SAKAMOTO, Toshihiro ,  SIU, Tony

Inventor： FAN, Weiming ,  HAXELL, Thomas, F. N. ,  JENKS, Matthew, G. ,  KAWANISHI, Nobuhiko ,  LEE, Shuliang ,  LIU, Hao ,  MALASKA, Michael, J. ,  MOORE, Joseph, A., III ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  PANDI, Bharathi ,  PEEL, Michael, R. ,  SAKAMOTO, Toshihiro ,  SIU, Tony

IPC: C07D403/00 ,  C07D413/00

CPC classification number: C07D471/14 ,  C07D487/14 ,  C07D519/00

Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Abstract translation: 本发明提供抑制Akt活性的取代的稠合萘啶衍生物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。