公开(公告)号：US09750744B2

公开(公告)日：2017-09-05

申请号：US15401952

申请日：2017-01-09

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: A61K31/519

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, 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：US20170231963A1

公开(公告)日：2017-08-17

申请号：US15445393

申请日：2017-02-28

Applicant: Array BioPharma, Inc.

Inventor： Christoph Max Krell ,  Marian Misun ,  Daniel Andreas Niederer ,  Werner Heinz Pachinger ,  Marie-Christine Wolf ,  Daniel Zimmermann ,  Weidong Liu ,  Peter J. Stengel ,  Paul Nichols

IPC: A61K31/4184 ,  A61K9/00 ,  A61K9/20 ,  A61K45/06

CPC classification number: A61K31/4184 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  C07B2200/13 ,  C07D235/06 ,  C07D235/08 ,  C30B7/08 ,  C30B29/54

Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.

公开(公告)号：US20170217936A1

公开(公告)日：2017-08-03

申请号：US15382028

申请日：2016-12-16

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

IPC: C07D403/12 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D495/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07D403/12 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  Y02A50/414

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(═X)—NH moiety are in the trans configuration, 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, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US09676783B2

公开(公告)日：2017-06-13

申请号：US14846166

申请日：2015-09-04

Applicant: Array BioPharma, Inc.

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

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

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

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：US20170136022A1

公开(公告)日：2017-05-18

申请号：US15275163

申请日：2016-09-23

Applicant: Array BioPharma Inc.

Inventor： David Shank Fry ,  Christopher M. Lindemann ,  Michael Preigh ,  Corey Jay Bloom ,  Christopher Donovan Craig ,  Devon Brevard Dubose ,  Jeff Gautschi ,  Dan Smithey

IPC: A61K31/517 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20

CPC classification number: A61K31/517 ,  A61K9/0053 ,  A61K9/10 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2077 ,  A61K47/32 ,  A61K47/38

Abstract: A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.

公开(公告)号：US20170119770A1

公开(公告)日：2017-05-04

申请号：US15401913

申请日：2017-01-09

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 ,  A61K31/5377

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

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：US20170114069A1

公开(公告)日：2017-04-27

申请号：US15401895

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

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：US20170114068A1

公开(公告)日：2017-04-27

申请号：US15401792

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04 ,  C07D519/00

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

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：US20170096425A1

公开(公告)日：2017-04-06

申请号：US15211702

申请日：2016-07-15

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 ,  A61K31/496 ,  C07D519/00 ,  A61K31/499 ,  A61K31/497 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/506 ,  A61K45/06 ,  A61K31/55

CPC classification number: 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：US09593100B2

公开(公告)日：2017-03-14

申请号：US14994827

申请日：2016-01-13

Applicant: Array BioPharma, Inc.

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

IPC: A61K31/535 ,  C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  A61K9/00 ,  A61K31/4184

CPC classification number: C07D403/04 ,  A61K9/0053 ,  A61K31/4184 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  A61K2300/00

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.

Abstract translation: 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及B-Raf异常激活的疾病或病症。