公开(公告)号：WO2010022076A1

公开(公告)日：2010-02-25

申请号：PCT/US2009/054193

申请日：2009-08-18

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  CELESTE, Laura L. ,  DAVIS, T. Gregg ,  DELISLE, Robert Kirk ,  GRESCHUK, Julie Marie ,  GROSS, Stefan, D. ,  HICKEN, Erik, James ,  JACKSON, Leila, J. ,  LYSSIKATOS, Joseph, P. ,  KALLAN, Nicholas C. ,  MARMSATER, Fredrik, P. ,  MUNSON, Mark, C. ,  PHENEGER, Jed ,  RAST, Bryson ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen T. ,  TOPALOV, George T. ,  WRIGHT, A. Dale ,  ZHAO, Qian

Inventor： ALLEN, Shelley ,  CELESTE, Laura L. ,  DAVIS, T. Gregg ,  DELISLE, Robert Kirk ,  GRESCHUK, Julie Marie ,  GROSS, Stefan, D. ,  HICKEN, Erik, James ,  JACKSON, Leila, J. ,  LYSSIKATOS, Joseph, P. ,  KALLAN, Nicholas C. ,  MARMSATER, Fredrik, P. ,  MUNSON, Mark, C. ,  PHENEGER, Jed ,  RAST, Bryson ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen T. ,  TOPALOV, George T. ,  WRIGHT, A. Dale ,  ZHAO, Qian

IPC: C07D471/04 ,  A61K31/47

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I), in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.

Abstract translation: 其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫细胞相关的受体酪氨酸抑制剂 疾病和病症，如炎性和自身免疫性疾病。

公开(公告)号：WO2011123674A1

公开(公告)日：2011-10-06

申请号：PCT/US2011/030769

申请日：2011-03-31

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  CLARK, Christopher, T. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin W. ,  KALLAN, Nicholas, C. ,  SIU, Michael ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

Inventor： CLARK, Christopher, T. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin W. ,  KALLAN, Nicholas, C. ,  SIU, Michael ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

IPC: C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D263/64 ,  A61K31/41 ,  A61P25/28

CPC classification number: C07D401/14 ,  C07D263/64 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10

Abstract: The invention provides novel spirotetrahydronaphthalene compounds of Formula α that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.

Abstract translation: 本发明提供新颖的抑制APP分泌​​酶切割的式（a）的四氢四氢化合物，可用作治疗神经变性疾病的治疗剂。

公开(公告)号：WO2009006569A1

公开(公告)日：2009-01-08

申请号：PCT/US2008/069147

申请日：2008-07-03

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  BENCSIK, Josef, R. ,  BLAKE, James, F. ,  KALLAN, Nicholas, C. ,  MITCHELL, Ian, S. ,  SPENCER, Keith, L. ,  XIAO, Dengming ,  XU, Rui ,  CHABOT, Christine ,  LIANG, Jun ,  SAFINA, Brian, S.

Inventor： BENCSIK, Josef, R. ,  BLAKE, James, F. ,  KALLAN, Nicholas, C. ,  MITCHELL, Ian, S. ,  SPENCER, Keith, L. ,  XIAO, Dengming ,  XU, Rui ,  CHABOT, Christine ,  LIANG, Jun ,  SAFINA, Brian, S.

IPC: C07D239/70 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

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: 本发明提供了式I化合物，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：WO2009089462A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/030617

申请日：2009-01-09

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  BANKA, Anna ,  BENCSIK, Josef R. ,  BLAKE, James F. ,  HENTEMANN, Martin F. ,  KALLAN, Nicholas C. ,  LIANG, Jun ,  MITCHELL, Ian S. ,  SCHLACHTER, Stephen T. ,  WALLACE, Eli M. ,  XU, Rui ,  TANG, Tony, P.

Inventor： BANKA, Anna ,  BENCSIK, Josef R. ,  BLAKE, James F. ,  HENTEMANN, Martin F. ,  KALLAN, Nicholas C. ,  LIANG, Jun ,  MITCHELL, Ian S. ,  SCHLACHTER, Stephen T. ,  WALLACE, Eli M. ,  XU, Rui ,  TANG, Tony, P.

IPC: C07D239/70 ,  A61K31/517 ,  A61P35/00 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D417/04 ,  C07D487/04

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula (I).

Abstract translation: 式I化合物可用于抑制AKT蛋白激酶。 公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。 式（I）。

公开(公告)号：WO2009089459A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/030610

申请日：2009-01-09

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  BENCSIK, Josef R. ,  BLAKE, James F. ,  KALLAN, Nicholas C. ,  MITCHELL, Ian S. ,  SPENCER, Keith Lee ,  XIAO, Dengming ,  XU, Rui ,  CHABOT, Christine ,  DO, Steven ,  LIANG, Jun ,  SAFINA, Brian ,  ZHANG, Birong

Inventor： BENCSIK, Josef R. ,  BLAKE, James F. ,  KALLAN, Nicholas C. ,  MITCHELL, Ian S. ,  SPENCER, Keith Lee ,  XIAO, Dengming ,  XU, Rui ,  CHABOT, Christine ,  DO, Steven ,  LIANG, Jun ,  SAFINA, Brian ,  ZHANG, Birong

IPC: C07D239/70 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/70

Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): 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: 本发明提供包含式（I）的化合物，包括其药学上可接受的盐：还提供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：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：WO2008124323A1

公开(公告)日：2008-10-16

申请号：PCT/US2008/058395

申请日：2008-03-27

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  GRESCHUK, Julie, Marie ,  KALLAN, Nicholas, C. ,  MARMSÄTER, Fredrik, P. ,  MUNSON, Mark, C. ,  RIZZI, James, P. ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen, T. ,  TOPALOV, George, T. ,  ZHAO, Qian ,  LYSSIKATOS, Joseph, P.

Inventor： ALLEN, Shelley ,  GRESCHUK, Julie, Marie ,  KALLAN, Nicholas, C. ,  MARMSÄTER, Fredrik, P. ,  MUNSON, Mark, C. ,  RIZZI, James, P. ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen, T. ,  TOPALOV, George, T. ,  ZHAO, Qian ,  LYSSIKATOS, Joseph, P.

IPC: C07D471/04 ,  A61K31/33 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula I: in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 R 6 , R 7 and R 8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

Abstract translation: 式I化合物：其中A，B，R 1，R 1a，R 2，R 3， R 4，R 5，R 6，R 7和R 8都具有 说明书中给出的含义是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。 本发明的具体化合物也被发现是Pim-1的抑制剂。

公开(公告)号：WO2008006040A1

公开(公告)日：2008-01-10

申请号：PCT/US2007/072885

申请日：2007-07-05

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  MITCHELL, Ian, S. ,  BLAKE, James, F. ,  XU, Rui ,  KALLAN, Nicholas, C. ,  XIAO, Dengming ,  SPENCER, Keith, Lee ,  BENCSIK, Josef, R. ,  LIANG, Jun ,  SAFINA, Brian ,  ZHANG, Birong ,  CHABOT, Christine ,  DO, Steven

Inventor： MITCHELL, Ian, S. ,  BLAKE, James, F. ,  XU, Rui ,  KALLAN, Nicholas, C. ,  XIAO, Dengming ,  SPENCER, Keith, Lee ,  BENCSIK, Josef, R. ,  LIANG, Jun ,  SAFINA, Brian ,  ZHANG, Birong ,  CHABOT, Christine ,  DO, Steven

IPC: C07D239/70 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/70 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I). 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: 本发明提供了包含式（I）的化合物，包括拆分的对映体，拆分的非对映异构体，溶剂化物和药学上可接受的盐。 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：WO2008006025A1

公开(公告)日：2008-01-10

申请号：PCT/US2007/072863

申请日：2007-07-05

Applicant: ARRAY BIOPHARMA INC. ,  MITCHELL, Ian, S. ,  BLAKE, James, F. ,  XU, Rui ,  KALLAN, Nicholas, C. ,  XIAO, Dengming ,  SPENCER, Keith, Lee ,  BENCSIK, Josef, R.

Inventor： MITCHELL, Ian, S. ,  BLAKE, James, F. ,  XU, Rui ,  KALLAN, Nicholas, C. ,  XIAO, Dengming ,  SPENCER, Keith, Lee ,  BENCSIK, Josef, R.

IPC: C07D493/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D493/04

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): 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: 本发明提供包含式（I）的分解的对映体，非对映异构体，溶剂化物和药学上可接受的盐的化合物：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 作为癌症。

公开(公告)号：WO2005051304A3

公开(公告)日：2005-06-09

申请号：PCT/US2004/039094

申请日：2004-11-19

Applicant: ARRAY BIOPHARMA INC. ,  MITCHELL, Ian, S. ,  SPENCER, Keith, L. ,  STENGEL, Peter ,  HAN, Yongxin ,  KALLAN, Nicholas, C. ,  MUNSON, Mark ,  VIGERS, Guy, P., A. ,  BLAKE, James ,  PISCOPIO, Anthony ,  JOSEY, John ,  MILLER, Scott ,  XIAO, Dengming ,  XU, Riu ,  RAO, Chang ,  WANG, Bin ,  BERNACKI, April, L.

Inventor： MITCHELL, Ian, S. ,  SPENCER, Keith, L. ,  STENGEL, Peter ,  HAN, Yongxin ,  KALLAN, Nicholas, C. ,  MUNSON, Mark ,  VIGERS, Guy, P., A. ,  BLAKE, James ,  PISCOPIO, Anthony ,  JOSEY, John ,  MILLER, Scott ,  XIAO, Dengming ,  XU, Riu ,  RAO, Chang ,  WANG, Bin ,  BERNACKI, April, L.

IPC: A61K31/53 ,  A61K31/519 ,  A61K31/496 ,  C07D257/12 ,  C07D253/00 ,  C07D401/00

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. 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.