公开(公告)号：WO2021250521A1

公开(公告)日：2021-12-16

申请号：PCT/IB2021/054919

申请日：2021-06-04

Applicant: ARRAY BIOPHARMA INC.

Inventor： BETTENDORF, Tanna Marie ,  DOERNER BARBOUR, Patrick Michael ,  KAHN, Dean Russell ,  KELLUM, Alex Andrew ,  LAIRD, Ellen Ruth ,  MORENO, David Austin ,  REN, Li

IPC: C07D239/90 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61P35/00 ,  A61K31/517

Abstract: Provided herein is a compound of the Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7 and L are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors.

公开(公告)号：WO2020261156A1

公开(公告)日：2020-12-30

申请号：PCT/IB2020/055992

申请日：2020-06-24

Applicant: ARRAY BIOPHARMA INC.

Inventor： BARBOUR, Patrick Michael ,  BROWN, Katie Keaton ,  COOK, Adam Wade ,  HICKEN, Erik James ,  KAHN, Dean Russell ,  LAIRD, Ellen Ruth ,  METCALF, Andrew Terrance ,  MORENO, David Austin ,  NEWHOUSE, Bradley Jon ,  PAJK, Spencer Phillip ,  PRIGARO, Brett Joseph ,  REN, Li ,  TARLTON, Eugene

IPC: C07D239/90 ,  A61P35/00 ,  C07D239/91 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07C271/28 ,  A61K31/517

Abstract: Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

公开(公告)号：WO2015103133A1

公开(公告)日：2015-07-09

申请号：PCT/US2014/072547

申请日：2014-12-29

Applicant: GENENTECH, INC. ,  ARRAY BIOPHARMA INC.

Inventor： BLAKE, James, F. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin, W. ,  LYON, Michael ,  METCALF, Andrew, T. ,  MOHR, Peter, J. ,  MORENO, David, A. ,  NEWHOUSE, Brad ,  REN, Li ,  TANG, Tony, P. ,  THOMAS, Allen, A. ,  SCHWARZ, Jacob ,  SCHMIDT, Jane ,  GAZZARD, Lewis ,  CHEN, Huifen

IPC: A61P35/00 ,  A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt 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.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，其可用于治疗过度增殖，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体或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。

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：WO2011025940A1

公开(公告)日：2011-03-03

申请号：PCT/US2010/046955

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  MATHIEU, Simon ,  PULK, Rebecca ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

Inventor： ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  MATHIEU, Simon ,  PULK, Rebecca ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

IPC: C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/38 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和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。

公开(公告)号：WO2009111280A1

公开(公告)日：2009-09-11

申请号：PCT/US2009/035383

申请日：2009-02-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  NEWHOUSE, Brad ,  REN, Li ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B. ,  MORENO, David, A.

Inventor： AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  NEWHOUSE, Brad ,  REN, Li ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B. ,  MORENO, David, A.

IPC: C07C311/08 ,  C07D213/75 ,  A61K31/44 ,  A61P35/00

CPC classification number: C07D213/75 ,  C07C311/48 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D417/04

Abstract: Compounds of Formula (I) are useful for inhibition of Raf 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.

Abstract translation: 式（I）的化合物可用于抑制Raf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。

公开(公告)号：WO2020055672A1

公开(公告)日：2020-03-19

申请号：PCT/US2019/049859

申请日：2019-09-06

Applicant: ARRAY BIOPHARMA INC.

Inventor： BLAKE, James F. ,  DAI, Donghua ,  HAAS, Julia ,  JIANG, Yutong ,  KAHN, Dean ,  KOLAKOWSKI, Gabrielle R. ,  MCFADDIN, Elizabeth A. ,  MCKENNEY, Megan L. ,  METCALF, Andrew T. ,  MORENO, David A. ,  PRIGARO, Brett ,  RAMANN, Ginelle A. ,  REN, Li ,  WALLS, Shane M. ,  ZHANG, Hailong

IPC: C07D487/14 ,  C07D487/22 ,  C07D498/14 ,  C07D498/22 ,  A61P35/00 ,  A61K31/551

Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R x , R y , W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：WO2019143994A1

公开(公告)日：2019-07-25

申请号：PCT/US2019/014277

申请日：2019-01-18

Applicant: ARRAY BIOPHARMA INC.

Inventor： WALLS, Shane M. ,  REN, Li ,  RAMANN, Ginelle A. ,  MORENO, David A. ,  METCALF, Andrew T. ,  MCFADDIN, Elizabeth A. ,  KOLAKOWSKI, Gabrielle R. ,  BLAKE, James F. ,  DAI, Donghua ,  HAAS, Julia ,  JIANG, Yutong ,  KAHN, Dean

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/437

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 and R 3 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：WO2012118850A1

公开(公告)日：2012-09-07

申请号：PCT/US2012/027009

申请日：2012-02-28

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  BLAKE, James F. ,  CHEN, Huifen ,  CHICARELLI, Mark Joseph ,  DEMEESE, Jason ,  GARREY, Rustam ,  GAUDINO, John J. ,  KAUS, Robert J. ,  KOLAKOWSKI, Gabrielle R. ,  MARLOW, Allison L. ,  MOHR, Peter J. ,  REN, Li ,  SCHWARZ, Jacob ,  SIEDEM, Christopher S. ,  THOMAS, Allen A. ,  WALLACE, Eli ,  WENGLOWSKY, Steven Mark

Inventor： BLAKE, James F. ,  CHEN, Huifen ,  CHICARELLI, Mark Joseph ,  DEMEESE, Jason ,  GARREY, Rustam ,  GAUDINO, John J. ,  KAUS, Robert J. ,  KOLAKOWSKI, Gabrielle R. ,  MARLOW, Allison L. ,  MOHR, Peter J. ,  REN, Li ,  SCHWARZ, Jacob ,  SIEDEM, Christopher S. ,  THOMAS, Allen A. ,  WALLACE, Eli ,  WENGLOWSKY, Steven Mark

IPC: C07D471/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K45/06 ,  C07D491/052

Abstract: Compounds having the formula I wherein Z, Z 1 Z 2 Z 3 , R 3a , R 3b and R b and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中Z，Z 1 Z 2 Z 3，R 3a，R 3b和R b如本文所定义是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：WO2011025968A1

公开(公告)日：2011-03-03

申请号：PCT/US2010/047013

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  GRADL, Stefan ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

Inventor： GRADL, Stefan ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

IPC: C07D471/04 ,  A61K31/437 ,  A61P13/12 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers 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Raf激酶。 公开了使用式I化合物和其立体异构体，互变异构体和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。 [公式I]