公开(公告)号：US10138243B2

公开(公告)日：2018-11-27

申请号：US15860781

申请日：2018-01-03

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 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/499 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D519/00

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：US10112942B2

公开(公告)日：2018-10-30

申请号：US15858240

申请日：2017-12-29

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: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  C07D471/04 ,  A61P1/12 ,  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：US20180142306A1

公开(公告)日：2018-05-24

申请号：US15860789

申请日：2018-01-03

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

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

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

CPC classification number: C12Q1/6886 ,  A61K31/5025 ,  A61K31/519 ,  C12Q2600/106 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/57492 ,  G01N2800/50 ,  G01N2800/52

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 the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：US20180134703A1

公开(公告)日：2018-05-17

申请号：US15861244

申请日：2018-01-03

Applicant: Array BioPharma, Inc.

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

IPC: C07D471/04 ,  A61P35/02 ,  A61P1/12

CPC classification number: C07D471/04 ,  A61K31/4162 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/00 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02

Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m 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：US20180072723A1

公开(公告)日：2018-03-15

申请号：US15814279

申请日：2017-11-15

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： James F. Blake ,  Laurence E. Burgess ,  Mark Joseph Chicarelli ,  James Gail Christensen ,  Jay Bradford Fell ,  John P. Fischer ,  John J. Gaudino ,  Erik James Hicken ,  Ronald Jay Hinklin ,  Matthew Randolf Lee ,  Matthew Arnold Marx ,  Macedonio J. Mejia ,  Martha E. Rodriguez ,  Pavel Savechenkov ,  Tony P. Tang ,  Guy P.A. Vigers ,  Henry J. Zecca

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US09790210B2

公开(公告)日：2017-10-17

申请号：US14442604

申请日：2013-11-12

Applicant: Array BioPharma Inc.

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

IPC: C07D231/00 ,  C07D403/00 ,  C07D401/00 ,  C07D211/72 ,  C07D413/00 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D401/04 ,  C07D413/12 ,  C07D231/52 ,  C07D401/12 ,  C07D405/04 ,  A61K31/4155

CPC classification number: C07D405/12 ,  A61K31/4155 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12

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：US20170217936A1

公开(公告)日：2017-08-03

申请号：US15382028

申请日：2016-12-16

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

IPC: C07D403/12 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D495/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07D403/12 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  Y02A50/414

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, Y, B, and Ring C are as defined herein, and wherein the Y—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, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20170096425A1

公开(公告)日：2017-04-06

申请号：US15211702

申请日：2016-07-15

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 ,  A61K31/496 ,  C07D519/00 ,  A61K31/499 ,  A61K31/497 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/506 ,  A61K45/06 ,  A61K31/55

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

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：US20160368916A1

公开(公告)日：2016-12-22

申请号：US14988521

申请日：2016-01-05

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 ,  C07D519/00

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.

公开(公告)号：US20130065908A1

公开(公告)日：2013-03-14

申请号：US13672546

申请日：2012-11-08

Applicant: Array BioPharma Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

IPC: A61K31/519 ,  A61P29/00 ,  A61P17/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/00 ,  C07D491/048 ,  A61P35/00

CPC classification number: C07D491/048 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: 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.