公开(公告)号：US20170056375A1

公开(公告)日：2017-03-02

申请号：US15348053

申请日：2016-11-10

Applicant: AstraZeneca AB ,  Array BioPharma, Inc.

Inventor： Nicola Frances BATEMAN ,  Paul Richard GELLERT ,  Kathryn Jane HILL

IPC: A61K31/4184 ,  A61K9/14 ,  A61K47/22 ,  A61K9/48 ,  A61K9/00 ,  A61K47/36

CPC classification number: A61K31/4184 ,  A61K9/0053 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/22 ,  A61K47/36 ,  C07D235/06

Abstract: The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.

Abstract translation: 本发明涉及含有6-（4-溴-2-氯 - 苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-羧酸（2-羟基 - 乙氧基） - 酰胺的硫酸氢盐的药物组合物 并使用所述组合物作为药物溶剂化其结晶形式和无定形形式; 以及制备所述组合物的方法。

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：US20160168104A1

公开(公告)日：2016-06-16

申请号：US15053441

申请日：2016-02-25

Applicant: Novartis Pharma 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: C07D235/08

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：US20160168102A1

公开(公告)日：2016-06-16

申请号：US14974588

申请日：2015-12-18

Applicant: Array BioPharma, Inc. ,  Novartis Pharma AG

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 ,  C30B29/54 ,  C30B7/08

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：US09278936B2

公开(公告)日：2016-03-08

申请号：US14382178

申请日：2013-02-27

Applicant: Array BioPharma Inc.

Inventor： Alisha B. Arrigo ,  Donald T. Corson ,  Coralee G. Mannila

IPC: C07D231/56 ,  A61K31/4155

CPC classification number: C07D231/56 ,  A61K31/4155 ,  Y02A50/411 ,  Y02A50/463

Abstract: Provided herein is a hydrogen chloride salt of 1-(3-/t?r/-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea, crystalline forms of 1-(3-½^butyl-1^-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride, processes for the preparation of said crystalline forms, pharmaceutical compositions containing a crystalline form of 1-(3-r

Abstract translation: 本文提供的是1-（3-叔丁基-1-叔丁基-1-对甲苯基-1H-吡唑-5-基）-3-（5-氟-2-（1-（2 - 羟基乙基）-1H-吲唑-5-基氧基）苄基）脲，1-（3 - 1/2丁基-1'-甲苯基-1H-吡唑-5-基）-3-（5-氟-2 - （1-（2-羟乙基）-1H-吲唑-5-基氧基）苄基）脲盐酸盐，制备所述结晶形式的方法，含有1-（3-r 丁基-1-对甲苯基-1H-吡唑-5-基）-3-（5-氟-2-（1-（2-羟乙基）-1H-吲唑-5-基氧基）苄基）脲盐酸盐形式B ，所述组合物的制备方法，通过所述方法制备的药物组合物，以及所述组合物在治疗各种疾病和病症中的用途。

公开(公告)号：US20160024018A1

公开(公告)日：2016-01-28

申请号：US14698151

申请日：2015-04-28

Applicant: Array BioPharma Inc. ,  ASTRAZENECA R&D ALDERLEY

Inventor： John DeMattei ,  Tsung-Hsun Chuang ,  Gorkhn Sharma-Singh ,  Paul Alfred Dickinson ,  Mohammed Pervez ,  Richard Anthony Storey ,  Christopher John Squire ,  James Gair Ford ,  Ronald John Roberts

IPC: C07D235/08

CPC classification number: C07D235/08 ,  C07D235/06

Abstract: The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.

Abstract translation: 本发明涉及化合物1硫酸氢盐和溶剂合物，其结晶形式和无定形形式，以及其制备方法。

公开(公告)号：US09242964B2

公开(公告)日：2016-01-26

申请号：US14016951

申请日：2013-09-03

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

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert M. Hershberg ,  Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61K31/55 ,  C07D223/16 ,  C07D403/14 ,  A61K31/4025 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D401/14

CPC classification number: C07D223/16 ,  A61K31/4025 ,  A61K31/55 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14

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-verses-host disease.

公开(公告)号：US09238627B2

公开(公告)日：2016-01-19

申请号：US14057498

申请日：2013-10-18

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 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20

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。