公开(公告)号：US20180133200A1

公开(公告)日：2018-05-17

申请号：US15860852

申请日：2018-01-03

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang ,  Li Ren

IPC: A61K31/444 ,  A61K31/496 ,  A61P35/00 ,  A61P35/02 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/551

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D519/00

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E 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：US09896435B2

公开(公告)日：2018-02-20

申请号：US14442613

申请日：2013-11-12

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D401/14 ,  A61P29/00 ,  A61P35/00 ,  C07D403/12 ,  C07D403/14

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 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 or pelvic pain syndrome.

公开(公告)号：US20170107232A1

公开(公告)日：2017-04-20

申请号：US15350888

申请日：2016-11-14

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  Hong-Woon Yang ,  Qian Zhao

IPC: C07D498/22 ,  C07D471/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a R3 and R3a are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US09493476B2

公开(公告)日：2016-11-15

申请号：US14575663

申请日：2014-12-18

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  Hong-Woon Yang ,  Qian Zhao

IPC: C07D487/22 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  C07D471/22 ,  C07D498/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20160280682A1

公开(公告)日：2016-09-29

申请号：US14442613

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D401/14 ,  A61P29/00 ,  A61P35/00 ,  C07D403/12 ,  C07D403/14

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 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 or pelvic pain syndrome.

公开(公告)号：US20210164055A1

公开(公告)日：2021-06-03

申请号：US17163930

申请日：2021-02-01

Applicant: Loxo Oncology, Inc. ,  Array BioPharma, Inc.

Inventor： Nisha Nanda ,  Joshua H. Bilenker ,  James F. Blake ,  Gabrielle R. Kolakowski ,  Barbara J. Brandhuber ,  Steven W. Andrews

IPC: C12Q1/6886 ,  A61K31/5025 ,  A61K31/519 ,  G01N33/574

Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：US10378068B2

公开(公告)日：2019-08-13

申请号：US15785228

申请日：2017-10-16

Applicant: Loxo Oncology, Inc. ,  Array BioPharma, Inc.

Inventor： Nisha Nanda ,  Joshua H. Bilenker ,  James F. Blake ,  Gabrielle R. Kolakowski ,  Barbara J. Brandhuber ,  Steven W. Andrews

IPC: A61K31/519 ,  C12Q1/6886 ,  A61K31/5025 ,  G01N33/574

Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：US20190127375A1

公开(公告)日：2019-05-02

申请号：US16245004

申请日：2019-01-10

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Mark J. Chicarelli ,  Adam Golos ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/506 ,  C07D519/00 ,  A61K31/497 ,  A61K31/55 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/499 ,  A61K45/06 ,  A61K31/496

Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 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 diseases or disorders mediated by a RET kinase.

公开(公告)号：US20190127374A1

公开(公告)日：2019-05-02

申请号：US16241839

申请日：2019-01-07

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Mark J. Chicarelli ,  Adam Golos ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski

IPC: C07D471/04 ,  A61K31/55 ,  A61K45/06 ,  A61K31/499 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/497 ,  C07D519/00 ,  A61K31/506 ,  A61K31/4545

Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 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 diseases or disorders mediated by a RET kinase.

公开(公告)号：US20190127373A1

公开(公告)日：2019-05-02

申请号：US16241837

申请日：2019-01-07

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Mark J. Chicarelli ,  Adam Golos ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski

IPC: C07D471/04 ,  A61K31/55 ,  A61K45/06 ,  A61K31/499 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/497 ,  C07D519/00 ,  A61K31/506 ,  A61K31/4545

Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 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 diseases or disorders mediated by a RET kinase.