公开(公告)号：US10953005B1

公开(公告)日：2021-03-23

申请号：US16739846

申请日：2020-01-10

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 ,  A61K31/551 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00

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：US20210002287A1

公开(公告)日：2021-01-07

申请号：US17020461

申请日：2020-09-14

Applicant: Array BioPharma Inc.

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

IPC: C07D487/04 ,  C07D471/04 ,  A61P29/00 ,  C07D519/00 ,  A61K9/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

公开(公告)号：US10799505B2

公开(公告)日：2020-10-13

申请号：US14943014

申请日：2015-11-16

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04 ,  A61K31/519 ,  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：US10774085B2

公开(公告)日：2020-09-15

申请号：US16044653

申请日：2018-07-25

Applicant: Array BioPharma Inc.

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

IPC: C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  A61K9/00 ,  A61K31/5377 ,  A61K31/519 ,  A61K45/06 ,  A61P29/00

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

公开(公告)号：US10765678B2

公开(公告)日：2020-09-08

申请号：US16169937

申请日：2018-10-24

Applicant: Array BioPharma Inc.

Inventor： Donald T. Corson ,  Christopher M. Lindemann ,  Daniel J. Watson

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/517 ,  A61P35/00 ,  A61K45/06

Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.

公开(公告)号：US10758542B2

公开(公告)日：2020-09-01

申请号：US16377514

申请日：2019-04-08

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

IPC: A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  A61K31/5377

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20200216416A1

公开(公告)日：2020-07-09

申请号：US16732733

申请日：2020-01-02

Applicant: Array BioPharma Inc.

Inventor： Adam Cook ,  Ronald Jay Hinklin ,  Oren T. McNulty

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14

Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2, R3, R4, R5, R6 and R7 are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.

公开(公告)号：US10647730B2

公开(公告)日：2020-05-12

申请号：US15900019

申请日：2018-02-20

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  Hong-Woon Yang ,  Qian Zhao

IPC: C07D498/22 ,  C07D487/22 ,  C07D487/04 ,  C07D519/00 ,  C07D471/22 ,  A61K31/519

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US10590139B2

公开(公告)日：2020-03-17

申请号：US16025281

申请日：2018-07-02

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 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541

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.

公开(公告)号：US10576080B2

公开(公告)日：2020-03-03

申请号：US15818082

申请日：2017-11-20

Applicant: Array BioPharma, Inc.

Inventor： Shenlin Huang ,  Xianming Jin ,  Zuosheng Liu ,  Daniel Poon ,  John Tellew ,  Yongqin Wan ,  Xing Wang ,  Yongping Xie

IPC: A61K31/506 ,  A61K31/4184 ,  A61K9/00 ,  C07D405/14 ,  A61K45/06 ,  C07D403/04 ,  C07D401/14

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.