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：US20190177328A1

公开(公告)日：2019-06-13

申请号：US16212493

申请日：2018-12-06

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: C07D487/04 ,  A61K45/06 ,  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：US10189845B2

公开(公告)日：2019-01-29

申请号：US15532937

申请日：2015-12-04

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：US10172851B2

公开(公告)日：2019-01-08

申请号：US15860808

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: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  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：US10172845B2

公开(公告)日：2019-01-08

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: A61K31/437 ,  A61K31/4353 ,  A61K31/4545 ,  A61K31/4162 ,  C07D471/04 ,  A61P1/00 ,  A61P35/00 ,  A61P35/02 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/12

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：US10154995B2

公开(公告)日：2018-12-18

申请号：US15684733

申请日：2017-08-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: A61K31/506 ,  C07D417/14 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt 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：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：US20180334441A1

公开(公告)日：2018-11-22

申请号：US16009030

申请日：2018-06-14

Applicant: Array Biopharma Inc.

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Joseph P. Lyssikatos ,  Thomas D. Aicher ,  Ellen Laird ,  John Robinson ,  Shelley Allen

IPC: C07D285/12 ,  C07F9/6539 ,  C07F9/201 ,  C07D417/12 ,  C07D417/06 ,  C07D271/107 ,  C07D413/12 ,  C07D413/06 ,  C07D413/04 ,  C07D401/12 ,  C07D417/04

CPC classification number: C07D285/12 ,  C07D271/107 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07F9/201 ,  C07F9/65392

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors.

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：US10011604B2

公开(公告)日：2018-07-03

申请号：US14984353

申请日：2015-12-30

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

IPC: C07D487/04 ,  C07D471/04 ,  C07C51/41 ,  C07C53/18 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00 ,  Y02A50/414

Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.