公开(公告)号：US20170260168A1

公开(公告)日：2017-09-14

申请号：US15333148

申请日：2016-10-24

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Andrew T. Metcalf ,  David Moreno ,  Li Ren ,  Tony P. Tang

IPC: C07D403/14 ,  A61K31/501 ,  G01N33/574 ,  A61K31/5377 ,  C07D401/14 ,  C12Q1/68 ,  A61K45/06 ,  C07D413/14

CPC classification number: C07D403/14 ,  A61K31/501 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C12Q1/6886 ,  G01N33/574

Abstract: Provided herein are compounds of the general Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which X, R1, R2, R3, Ring A and z have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, including diseases or disorders mediated by FGFR1, FGFR2, FGFR3 and/or FGFR4.

公开(公告)号：US09670208B2

公开(公告)日：2017-06-06

申请号：US15197445

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  John Gaudino ,  Indrani W. Gunawardana ,  Erik James Hicken ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Lewis Gazzard ,  Jane Schmidt ,  Steve Do

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/444 ,  C07D487/04 ,  C07D519/00 ,  A61K31/55

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of 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 diseases, or associated pathological conditions are disclosed.

公开(公告)号：US20160297758A1

公开(公告)日：2016-10-13

申请号：US14442514

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Yutong Jiang ,  Timothy Kercher ,  Shannon L. Winski

IPC: C07D207/50 ,  C07D487/04 ,  C07D513/04 ,  C07D471/04 ,  C07C53/18 ,  C07D403/12

CPC classification number: C07D207/50 ,  C07C53/18 ,  C07D207/14 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

公开(公告)号：US20160280681A1

公开(公告)日：2016-09-29

申请号：US14442584

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  James F. Blake ,  Barbara J. Brandhuber ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Rui Xu ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D231/56 ,  C07D231/52 ,  C07D403/04 ,  C07D401/12 ,  C07D401/04 ,  C07D231/40

CPC classification number: C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

Abstract: Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

公开(公告)号：US09346805B2

公开(公告)日：2016-05-24

申请号：US13676963

申请日：2012-11-14

Applicant: Array BioPharma Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Ian S. Mitchell ,  Douglas McCord Sammond ,  Tony P. Tang ,  Eli M. Wallace ,  Rui Xu ,  James Graham

IPC: C07D471/10 ,  C07D487/10

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved 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 Akt-mediated diseases, for example, 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，拆分的非对映体，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Akt介导的疾病例如过度增殖性疾病如癌症的方法。

公开(公告)号：US08981085B2

公开(公告)日：2015-03-17

申请号：US14271129

申请日：2014-05-06

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. 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CHK1和/或CHK2。 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：US20140357644A1

公开(公告)日：2014-12-04

申请号：US14457582

申请日：2014-08-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith Lee Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Steven Do ,  Jun Liang ,  Brian Safina ,  Birong Zhang

IPC: C07D239/70

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：US20140249127A1

公开(公告)日：2014-09-04

申请号：US14181418

申请日：2014-02-14

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: C07D417/14 ,  C07D409/14 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/04

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug 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, prodrug 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，前药或其药学上可接受的盐，其可用于治疗过度增生，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，前药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：US08697715B2

公开(公告)日：2014-04-15

申请号：US13782513

申请日：2013-03-01

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug 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, prodrug 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，前药或其药学上可接受的盐，其可用于治疗过度增生，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，前药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：US12180207B2

公开(公告)日：2024-12-31

申请号：US17416117

申请日：2019-12-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： James F. Blake ,  David A. Moreno ,  Li Ren ,  Tony P. Tang ,  Shane M. Walls

IPC: C07D471/04 ,  A61P35/00 ,  C07D519/00

Abstract: Provided herein are compounds of the general Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which Ring A, Ring B, Ring C, R1, R2, L, Y, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, including diseases or disorders mediated by FGFR1, FGFR2, FGFR3 and/or FGFR4.