公开(公告)号：US20190247398A1

公开(公告)日：2019-08-15

申请号：US16170976

申请日：2018-10-25

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

Inventor： Qian Zhao ,  Stacey Spencer ,  Yutong Jiang ,  Julia Haas ,  Charles Todd Eary

IPC: A61K31/519 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K9/0019 ,  A61K9/0095 ,  A61K31/404 ,  A61K31/496 ,  A61K47/02 ,  A61K47/36 ,  A61K47/38 ,  A61P35/00 ,  C07B2200/13 ,  C07C55/06 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15 ,  C07C59/08 ,  C07C59/245 ,  C07C59/255 ,  C07C59/265 ,  C07C59/285 ,  C07C63/06 ,  C07C229/24 ,  C07C233/83 ,  C07C301/00 ,  C07C309/04 ,  C07C309/05 ,  C07C309/08 ,  C07C309/29 ,  C07C309/30 ,  C07C309/35 ,  C07D471/22 ,  A61K2300/00

Abstract: The present application in some embodiments provides a pharmaceutical composition comprising: and a compounding agent. Further provided herein are methods of making and methods of using the pharmaceutical compositions, for example, in the treatment of cancer.

公开(公告)号：US10323022B2

公开(公告)日：2019-06-18

申请号：US15839706

申请日：2017-12-12

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 ,  A61K31/4162 ,  A61K31/4155 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  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 ,  C07D491/048

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：US20190161500A1

公开(公告)日：2019-05-30

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：US20190125749A1

公开(公告)日：2019-05-02

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

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：US20190076437A1

公开(公告)日：2019-03-14

申请号：US16199875

申请日：2018-11-26

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Julia Haas ,  Gabrielle R. Kolakowski

IPC: A61K31/529 ,  A61K31/675 ,  A61K31/4545 ,  A61K31/496 ,  A61P35/00

Abstract: Methods for inhibiting a ROS1 kinase with 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. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).

公开(公告)号：US20190076436A1

公开(公告)日：2019-03-14

申请号：US16199867

申请日：2018-11-26

Applicant: Array BioPharma Inc.

Inventor： Steven W. Andrews ,  James F. Blake ,  Julia Haas ,  Gabrielle R. Kolakowski

IPC: A61K31/529 ,  A61K31/675 ,  A61K31/4545 ,  A61P35/00

Abstract: Methods for inhibiting a ROS1 kinase with 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. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).

公开(公告)号：US10208024B2

公开(公告)日：2019-02-19

申请号：US15333148

申请日：2016-10-24

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 ,  C07D401/14 ,  C07D413/14 ,  A61K31/501 ,  A61K31/5377 ,  C12Q1/68 ,  A61K45/06 ,  C12Q1/6886 ,  G01N33/574

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：US10174027B2

公开(公告)日：2019-01-08

申请号：US15858658

申请日：2017-12-29

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：US20180297985A1

公开(公告)日：2018-10-18

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

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.

公开(公告)号：US20180258054A1

公开(公告)日：2018-09-13

申请号：US15782620

申请日：2017-10-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/42 ,  C07D403/04

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.