公开(公告)号：US11932633B2

公开(公告)日：2024-03-19

申请号：US17053273

申请日：2019-05-06

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

Inventor： Matthew Arnold Marx ,  Matthew Randolph Lee ,  James F. Blake ,  Mark Joseph Chicarelli ,  Jay Bradford Fell ,  John P. Fischer ,  Erik James Hicken ,  Pavel Savechenkov ,  Tony Tang ,  Guy P. A. Vigers ,  Henry J. Zecca

IPC: C07D413/06 ,  A61P35/00 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D413/14 ,  A61P35/00 ,  C07D413/06

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：US20240066029A1

公开(公告)日：2024-02-29

申请号：US18342314

申请日：2023-06-27

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

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

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：US20220226326A1

公开(公告)日：2022-07-21

申请号：US17409644

申请日：2021-08-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Leivers ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: A61K31/517 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D239/70 ,  C07D413/12 ,  C07D407/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and 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.

公开(公告)号：US20210380570A1

公开(公告)日：2021-12-09

申请号：US17053273

申请日：2019-05-06

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

Inventor： Matthew Arnold Marx ,  Matthew Randolph Lee ,  James F. Blake ,  Mark Joseph Chicarelli ,  Jay Bradford Fell ,  John P. Fischer ,  Erik James Hicken ,  Pavel Savechenkov ,  Tony Tang ,  Guy P.A. Vigers ,  Henry J. Zecca

IPC: C07D413/14 ,  C07D413/06 ,  A61P35/00

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：US20210230170A1

公开(公告)日：2021-07-29

申请号：US17272276

申请日：2019-08-29

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

Inventor： Matthew Arnold Marx ,  James F. Blake ,  Jay Bradford Fell ,  John P. Fischer ,  Macedonio J. Mejia

IPC: C07D487/04 ,  A61P35/00

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：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：US20190300511A1

公开(公告)日：2019-10-03

申请号：US16276326

申请日：2019-02-14

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 ,  C07D413/14 ,  C07D401/14 ,  G01N33/574 ,  A61K31/501 ,  A61K45/06 ,  A61K31/5377 ,  C12Q1/6886

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：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.