公开(公告)号：WO2013078254A1

公开(公告)日：2013-05-30

申请号：PCT/US2012/066153

申请日：2012-11-20

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  SKELTON, Nicholas ,  GRADL, Stefan ,  BLAKE, James F. ,  GRAHAM, James M. ,  GUNAWARDANA, Indrani W. ,  HENTEMANN, Martin ,  MARLOW, Allison L. ,  TANG, Tony P.

Inventor： SKELTON, Nicholas ,  GRADL, Stefan ,  BLAKE, James F. ,  GRAHAM, James M. ,  GUNAWARDANA, Indrani W. ,  HENTEMANN, Martin ,  MARLOW, Allison L. ,  TANG, Tony P.

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4188 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula 1: wherein Het, X, R 1 and R 2 are as defined herein.

Abstract translation: 本发明提供包括拆分的对映异构体，分解的非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式1：其中Het，X，R 1和R 2如本文所定义。

公开(公告)号：WO2012154274A1

公开(公告)日：2012-11-15

申请号：PCT/US2012/026572

申请日：2012-02-24

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James, F ,  DELISLE, Robert, Kirk ,  DE MEESE, Lisa, A. ,  GRAHAM, James, M. ,  LE HUEROU, Yvan ,  LYON, Michael ,  ROBINSON, John, E. ,  WALLACE, Eli, M. ,  WANG, Bin ,  XU, Rui

Inventor： BLAKE, James, F ,  DELISLE, Robert, Kirk ,  DE MEESE, Lisa, A. ,  GRAHAM, James, M. ,  LE HUEROU, Yvan ,  LYON, Michael ,  ROBINSON, John, E. ,  WALLACE, Eli, M. ,  WANG, Bin ,  XU, Rui

IPC: C07D401/06 ,  C07D471/04 ,  C07D519/00 ,  A61K31/4709 ,  A61P29/00

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D519/00

Abstract: Compounds of Formula I: in which R 1 , R 2 , R 3 , R 4 and R 10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.

Abstract translation: R 1，R 2，R 3，R 4和R 10具有本说明书中给出的含义的式I化合物是可用于治疗由PIM-1和/或PIM-2和/或PIM-2介导的疾病的受体酪氨酸抑制剂， 3激酶。

公开(公告)号：WO2009006567A3

公开(公告)日：2009-03-19

申请号：PCT/US2008069144

申请日：2008-07-03

Applicant: ARRAY BIOPHARMA INC ,  GENENTECH INC ,  BENCSIK JOSEF ,  BLAKE JAMES F ,  GRAHAM JAMES M ,  HENTEMANN MARTIN F ,  KALLAN NICHOLAS C ,  MITCHELL IAN S ,  SCHLACTER STEPHEN T ,  SPENCER KEITH L ,  XIAO DENGMING ,  XU RUI ,  WELCH MIKE ,  LIANG JUN ,  SAFINA BRIAN S

Inventor： BENCSIK JOSEF ,  BLAKE JAMES F ,  GRAHAM JAMES M ,  HENTEMANN MARTIN F ,  KALLAN NICHOLAS C ,  MITCHELL IAN S ,  SCHLACTER STEPHEN T ,  SPENCER KEITH L ,  XIAO DENGMING ,  XU RUI ,  WELCH MIKE ,  LIANG JUN ,  SAFINA BRIAN S

IPC: C07D401/12 ,  A61K31/517 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00 ,  C07D403/12

CPC classification number: C07D403/12 ,  C07D401/12

Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式（I）化合物，其包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：WO2009006567A2

公开(公告)日：2009-01-08

申请号：PCT/US2008/069144

申请日：2008-07-03

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  BENCSIK, Josef ,  BLAKE, James, F. ,  GRAHAM, James, M. ,  HENTEMANN, Martin, F. ,  KALLAN, Nicholas, C. ,  MITCHELL, Ian, S. ,  SCHLACTER, Stephen, T. ,  SPENCER, Keith, L. ,  XIAO, Dengming ,  XU, Rui ,  WELCH, Mike ,  LIANG, Jun ,  SAFINA, Brian, S.

Inventor： BENCSIK, Josef ,  BLAKE, James, F. ,  GRAHAM, James, M. ,  HENTEMANN, Martin, F. ,  KALLAN, Nicholas, C. ,  MITCHELL, Ian, S. ,  SCHLACTER, Stephen, T. ,  SPENCER, Keith, L. ,  XIAO, Dengming ,  XU, Rui ,  WELCH, Mike ,  LIANG, Jun ,  SAFINA, Brian, S.

IPC: C07D401/12 ,  C07D403/12

CPC classification number: C07D403/12 ,  C07D401/12

Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式（I）的化合物，包括其互变异构体，拆分的对映异构体，非对映异构体，溶剂化物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂并用于治疗过度增殖性疾病如癌症的方法。