公开(公告)号：US20170260202A1

公开(公告)日：2017-09-14

申请号：US15606928

申请日：2017-05-26

Applicant: ARRAY BIOPHARMA INC.

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

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

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

Abstract: This invention provides compounds of Formula 11:

公开(公告)号：US09718796B2

公开(公告)日：2017-08-01

申请号：US13979632

申请日：2012-01-12

Applicant: James Jeffry Howbert ,  Robert Hershberg ,  Laurence E. Burgess ,  Hong Woon Yang

Inventor： James Jeffry Howbert ,  Robert Hershberg ,  Laurence E. Burgess ,  Hong Woon Yang

IPC: A61K31/55 ,  C07D223/16 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D413/10 ,  C07D295/192 ,  C07D487/04

CPC classification number: C07D295/192 ,  A61K31/55 ,  C07D223/16 ,  C07D401/04 ,  C07D403/10 ,  C07D413/10 ,  C07D487/04

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.

公开(公告)号：US09655904B2

公开(公告)日：2017-05-23

申请号：US14817291

申请日：2015-08-04

Applicant: VentiRx Pharmaceuticals, Inc. ,  Array BioPharma, Inc.

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong-Woon Yang

IPC: A01N43/00 ,  A61K31/55 ,  C07D223/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D223/16 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10

CPC classification number: A61K31/55 ,  C07D223/14 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-versus-host disease.

公开(公告)号：US09562016B2

公开(公告)日：2017-02-07

申请号：US14974655

申请日：2015-12-18

Applicant: Novartis AG ,  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: C07D235/06 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20 ,  C30B7/08 ,  C30B29/54 ,  C07D235/08

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.

Abstract translation: 本发明涉及制备6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺的方法， （4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺，以及有用的中间体。 本文还提供包含该结晶化合物的药物组合物。

公开(公告)号：US09561214B2

公开(公告)日：2017-02-07

申请号：US12581072

申请日：2009-10-16

Applicant: Brian J. Tunquist ,  Duncan H. Walker ,  Richard D. Woessner

Inventor： Brian J. Tunquist ,  Duncan H. Walker ,  Richard D. Woessner

IPC: A61K31/433 ,  A61K31/00

CPC classification number: A61K31/433 ,  A61K31/00

Abstract: Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose.

Abstract translation: 治疗由细胞分裂引起的疾病或通过在允许回收或减少副作用的给药循环中的生物学有效剂量和最大耐受剂量之间施用两剂有丝分裂抑制剂来治疗由细胞分裂引起的疾病或通过抑制有丝分裂来治疗疾病的方法，其中 在第一剂后24至48小时施用第二剂量。

公开(公告)号：US09556139B2

公开(公告)日：2017-01-31

申请号：US14702947

申请日：2015-05-04

Applicant: Array BioPharma Inc.

Inventor： Laurence E. Burgess ,  Christopher T. Clark ,  Adam Cook ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  George A. Doherty ,  Kevin W. Hunt ,  Todd T. Romoff ,  Ganghyeok Kim

IPC: A61K31/352 ,  C07D311/58 ,  C07D405/12 ,  C07D407/12

CPC classification number: C07D311/58 ,  C07D311/04 ,  C07D405/12 ,  C07D407/12

Abstract: Provided herein are compounds of Formula I: in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 式（Ⅳ，Ⅵ）化合物：其中A1，A2，P2，P3，R7a，R7b，R8，R9，R10和Z2具有说明书中给出的含义，是可用于制备DP2受体调节剂的化合物 免疫疾病的治疗。

公开(公告)号：US09527865B2

公开(公告)日：2016-12-27

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

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：US09493476B2

公开(公告)日：2016-11-15

申请号：US14575663

申请日：2014-12-18

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

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：US20160304519A1

公开(公告)日：2016-10-20

申请号：US15197445

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  John Gaudino ,  Indrani W. Gunawardana ,  Erik James Hicken ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Lewis Gazzard ,  Jane Schmidt ,  Steve Do

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/444 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of 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 diseases, or associated pathological conditions are disclosed.

Abstract translation: 提供式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，其可用于治疗疾病。 公开了使用式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在体外，原位和体内诊断，预防或治疗这些疾病或相关病理状况的方法。

公开(公告)号：US20160280692A1

公开(公告)日：2016-09-29

申请号：US14442604

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Shannon L. Winski

IPC: C07D405/12 ,  C07D231/40 ,  C07D231/52 ,  C07D405/04 ,  C07D401/12 ,  C07D401/14 ,  C07D401/04

CPC classification number: C07D405/12 ,  A61K31/4155 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12

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 or pelvic pain syndrome.