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：US20220119396A1

公开(公告)日：2022-04-21

申请号：US17514684

申请日：2021-10-29

Applicant: Array BioPharma Inc.

Inventor： Steven W. ANDREWS ,  James F. BLAKE ,  Julia HAAS ,  Yutong JIANG ,  Gabrielle R. KOLAKOWSKI ,  David A. MORENO ,  Li REN ,  Shane M. WALLS

IPC: C07D487/04

Abstract: Provided herein are compounds of the 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：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：US11168090B2

公开(公告)日：2021-11-09

申请号：US16478071

申请日：2018-01-18

Applicant: Array BioPharma Inc.

Inventor： Steven W Andrews ,  James F Blake ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R Kolakowski ,  David A Moreno ,  Li Ren ,  Shane M Walls

IPC: A61K31/4985 ,  C07D487/04

Abstract: Provided herein are compounds of the 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：US20210284656A9

公开(公告)日：2021-09-16

申请号：US16264194

申请日：2019-01-31

Applicant: Array BioPharma Inc.

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D498/10 ,  C07D401/12 ,  C07D417/14 ,  C07D413/14 ,  C07D239/94 ,  C07D413/12 ,  C04B35/632 ,  C07D498/04

Abstract: The invention includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US20210269432A1

公开(公告)日：2021-09-02

申请号：US16099398

申请日：2017-05-17

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： John P. FISCHER ,  Jay Bradford FELL ,  James F. BLAKE ,  Ronald Jay HINKLIN ,  Macedonio J. MEJIA ,  Erik James HICKEN ,  Mark Joseph CHICARELLI ,  John J. GAUDINO ,  Guy P.A. VIGERS ,  Laurence E. BURGESS ,  Matthew Arnold MARX ,  James Gail CHRISTENSEN ,  Matthew Randolf LEE ,  Pavel SAVECHENKOV ,  Henry J. ZECCA ,  Tony P. TANG

IPC: C07D471/04 ,  C07D519/00 ,  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：US11007194B2

公开(公告)日：2021-05-18

申请号：US14355903

申请日：2012-11-09

Applicant: Array BioPharma Inc.

Inventor： Darrin Stuart ,  Meghna Das Thakur

IPC: A61K31/506

Abstract: The present invention relates to a method of treating a patient with a serine/threonine kinase inhibitor wherein resistance to the treatment with a serine/threonine kinase inhibitor is suppressed by administering the serine/threonine kinase inhibitor on an intermittent dosing schedule.

公开(公告)号：US10548894B2

公开(公告)日：2020-02-04

申请号：US15875031

申请日：2018-01-19

Applicant: Array BioPharma Inc.

Inventor： Giordano Caponigro ,  Darrin Stuart ,  Laure De Parseval

IPC: A61K31/506 ,  A61K45/06 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C12Q1/6886

Abstract: Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3 EGFR, MAP2K1, MAP2K2, NRAS, KRAS HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.