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：WO2013055645A1

公开(公告)日：2013-04-18

申请号：PCT/US2012/059282

申请日：2012-10-09

Applicant: ARRAY BIOPHARMA INC. ,  BOYS, Mark Laurence ,  BURGESS, Laurence E. ,  EARY, C. Todd ,  GRONEBERG, Robert ,  HACHE, Bruno P. ,  HARVEY, Darren ,  HICKEN, Erik James ,  KRASER, Christopher F. ,  LAIRD, Ellen ,  MORENO, David A. ,  MUNSON, Mark C. ,  REN, Li ,  ROBINSON, John E. ,  SCHLACHTER, Stephen T.

Inventor： BOYS, Mark Laurence ,  BURGESS, Laurence E. ,  EARY, C. Todd ,  GRONEBERG, Robert ,  HACHE, Bruno P. ,  HARVEY, Darren ,  HICKEN, Erik James ,  KRASER, Christopher F. ,  LAIRD, Ellen ,  MORENO, David A. ,  MUNSON, Mark C. ,  REN, Li ,  ROBINSON, John E. ,  SCHLACHTER, Stephen T.

IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X 1 and X 2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract translation: R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂合物是一种或多种JAK激酶的抑制剂，并且是有用的 治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。

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：EP2250155B1

公开(公告)日：2013-07-03

申请号：EP09701043.3

申请日：2009-01-09

Applicant: Array Biopharma, Inc. ,  Genentech, Inc.

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

公开(公告)号：EP2250155A1

公开(公告)日：2010-11-17

申请号：EP09701043.3

申请日：2009-01-09

Applicant: Array Biopharma, Inc. ,  Genentech, Inc.

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).

公开(公告)号：EP2766368A1

公开(公告)日：2014-08-20

申请号：EP12775905.8

申请日：2012-10-09

Applicant: Array Biopharma Inc.

Inventor： BOYS, Mark Laurence ,  BURGESS, Laurence E. ,  EARY, C. Todd ,  GRONEBERG, Robert ,  HACHE, Bruno P. ,  HARVEY, Darren ,  HICKEN, Erik James ,  KRASER, Christopher F. ,  LAIRD, Ellen ,  MORENO, David A. ,  MUNSON, Mark C. ,  REN, Li ,  ROBINSON, John E. ,  SCHLACHTER, Stephen T.

IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , X
1 and X
2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract translation: 其中R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有说明书中给出的含义的式I化合物及其立体异构体和药学上可接受的盐和溶剂合物是 一种或多种JAK激酶，并且可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞的排斥，以及血液病和恶性肿瘤及其并发症。

公开(公告)号：EP2334677B1

公开(公告)日：2013-10-09

申请号：EP09791625.8

申请日：2009-08-18

Applicant: Array Biopharma, Inc.

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

公开(公告)号：EP2334677A1

公开(公告)日：2011-06-22

申请号：EP09791625.8

申请日：2009-08-18

Applicant: Array Biopharma, Inc.

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，R 1，R 1a，R 2，R 3，R 4，R 5，R 6和R 7具有说明书中给出的含义的式（I）化合物是有用的受体酪氨酸抑制剂 用于治疗免疫细胞相关疾病和病症，例如炎性和自身免疫性疾病。