公开(公告)号：US09676791B2

公开(公告)日：2017-06-13

申请号：US13607016

申请日：2012-09-07

Applicant: Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

Inventor： Eli Wallace ,  George Topalov ,  Joseph Lyssikatos ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D239/94 ,  C07D498/10 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  C04B35/632

CPC classification number: C07D498/10 ,  C04B35/632 ,  C07D239/94 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also 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：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：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。

公开(公告)号：US09562055B2

公开(公告)日：2017-02-07

申请号：US14117615

申请日：2012-05-09

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

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: C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D495/04 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  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

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.

Abstract translation: 其中R1，R2，Ra，Rb，Rc，Rd，X，Y，B和环C如本文所定义的式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物或前药，其中 Y-B部分和NH-C（= X）-NH部分是反式构型，是TrkA激酶的抑制剂，可用于治疗可用TrkA激酶抑制剂如疼痛，癌症治疗的疾病 ，炎症，神经变性疾病和某些传染病。

公开(公告)号：US20160368916A1

公开(公告)日：2016-12-22

申请号：US14988521

申请日：2016-01-05

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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：US20160355517A1

公开(公告)日：2016-12-08

申请号：US14442503

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Kevin Ronald Condroski ,  Lily Huang ,  Timothy Kercher ,  Shannon L. Winski

IPC: C07D487/04 ,  C07D519/00 ,  C07D403/12 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D231/56 ,  C07D403/12 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

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.

公开(公告)号：US20160318877A1

公开(公告)日：2016-11-03

申请号：US15204715

申请日：2016-07-07

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

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.

Abstract translation: 和其盐，其中R1如本文所定义，以及所述式的化合物和中间体。

公开(公告)号：US09370567B2

公开(公告)日：2016-06-21

申请号：US13885644

申请日：2011-11-16

Applicant: Kurtis D. Davies ,  Stefan Gross

Inventor： Kurtis D. Davies ,  Stefan Gross

IPC: A61K45/06 ,  A61K31/437 ,  A61K31/7068 ,  A61K31/495 ,  A61K31/551

CPC classification number: A61K31/4545 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/519 ,  A61K31/551 ,  A61K31/7068 ,  A61K45/06 ,  A61K2300/00

Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.

Abstract translation: 提供CHK1抑制剂和WEE1抑制剂的组合。

公开(公告)号：US09303040B2

公开(公告)日：2016-04-05

申请号：US12307526

申请日：2007-07-05

Applicant: Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

IPC: A61K31/496 ,  C07D409/02 ,  C07D495/04

CPC classification number: C07D495/04

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包括分解对映异构体，非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式：还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。