公开(公告)号：US11028093B2

公开(公告)日：2021-06-08

申请号：US16890663

申请日：2020-06-02

Applicant: Array BioPharma Inc. ,  Celgene Corporation

Inventor： Shelley Allen ,  Mark Laurence Boys ,  Mark J. Chicarelli ,  Jay Bradford Fell ,  John P. Fischer ,  John Gaudino ,  Erik James Hicken ,  Ronald Jay Hinklin ,  Christopher F. Kraser ,  Ellen Laird ,  John E. Robinson ,  Tony P. Tang ,  Laurence E. Burgess ,  Robert Andrew Rieger ,  Jed Pheneger ,  Yoshitaka Satoh ,  Katerina Leftheris ,  Raj K. Raheja ,  Brydon L. Bennett

IPC: A61K45/06 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/5377

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

公开(公告)号：US20210077463A1

公开(公告)日：2021-03-18

申请号：US16772306

申请日：2018-12-17

Applicant: PFIZER INC. ,  MERCK PATENT GMBH ,  ARRAY BIOPHARMA INC.

Inventor： Christoffel Hendrik Boshoff ,  Rossano Cesari ,  Cristian Massacesi ,  Nuzhat Pathan ,  Patrice A. Lee ,  Shannon L. Winski

IPC: A61K31/4184 ,  A61K39/395 ,  A61K31/5025 ,  A61P35/00 ,  A61K9/00

Abstract: This invention relates to a method of treating cancer by administering a combination therapy comprising a combination of a MEK inhibitor and a PD-1 axis binding antagonist, or a combination of a MEK inhibitor and a PARP inhibitor, or a combination of a MEK inhibitor and a PD-1 axis binding antagonist and a PARP inhibitor to a patient in need thereof.

公开(公告)号：US10907215B2

公开(公告)日：2021-02-02

申请号：US15860789

申请日：2018-01-03

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

公开(公告)号：US10813936B2

公开(公告)日：2020-10-27

申请号：US16366368

申请日：2019-03-27

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A61K31/519 ,  C07D487/04 ,  C12Q1/48

Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

公开(公告)号：US20200308194A1

公开(公告)日：2020-10-01

申请号：US16902424

申请日：2020-06-16

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

Inventor： Charles Todd EARY ,  Stacey SPENCER ,  Zack CRANE ,  Katelyn CHANDO ,  Sylvie ASSELIN ,  Weidong LIU ,  Mike WELCH ,  Adam COOK ,  Gabrielle R. KOLAKOWSKI ,  Andrew T. METCALF ,  David A. MORENO ,  Tony P. TANG

IPC: C07D519/00 ,  C07D471/04

Abstract: In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US10766881B2

公开(公告)日：2020-09-08

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：US10655186B2

公开(公告)日：2020-05-19

申请号：US15785218

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: 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：US10647715B2

公开(公告)日：2020-05-12

申请号：US16412091

申请日：2019-05-14

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

Inventor： Matthew Arnold Marx ,  Thomas P. Bobinski ,  Aaron Craig Burns ,  John Gaudino ,  Julia Haas ,  John Michael Ketcham ,  John David Lawson ,  Brad Newhouse ,  Spencer Pajk ,  Christopher Ronald Smith ,  Tony P. Tang

IPC: C07D471/04 ,  A61P35/00 ,  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：US10561654B2

公开(公告)日：2020-02-18

申请号：US15921306

申请日：2018-03-14

Applicant: Array BioPharma Inc.

Inventor： Daya Verma ,  Yogita Krishnamachari ,  Xiaohong Shen ,  Hanchen Lee ,  Ping Li ,  Rajinder Singh ,  LayChoo Tan

IPC: A61K31/506 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00 ,  A61K9/28

Abstract: This invention relates to solid oral pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate (COMPOUND A) and the use of these formulations for treating proliferative diseases, such as solid tumor diseases.

公开(公告)号：US20190270749A1

公开(公告)日：2019-09-05

申请号：US16415575

申请日：2019-05-17

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Julia Haas ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Allen A. Thomas ,  Shannon L. Winski

IPC: C07D491/048 ,  C07D409/14 ,  C07D401/14 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D453/02 ,  C07D413/12 ,  C07D405/12 ,  C07D403/14 ,  C07D403/04 ,  C07D403/02 ,  C07D401/12 ,  C07D231/54 ,  C07D231/40 ,  C07D405/14 ,  C07D471/08

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 and pelvic pain syndrome.