公开(公告)号：US20170165267A1

公开(公告)日：2017-06-15

申请号：US15399207

申请日：2017-01-05

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A61K31/519 ,  C12Q1/48

CPC classification number: A61K31/519 ,  C07D487/04 ,  C12Q1/485 ,  C12Y207/10001 ,  G01N2333/91205 ,  G01N2800/52

Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

公开(公告)号：US20170114067A1

公开(公告)日：2017-04-27

申请号：US15399389

申请日：2017-01-05

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04 ,  C07D519/00

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：US20170112849A1

公开(公告)日：2017-04-27

申请号：US15401969

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

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

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/5025

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：US20170112842A1

公开(公告)日：2017-04-27

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: A61K31/529

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：US20170087156A1

公开(公告)日：2017-03-30

申请号：US15311148

申请日：2015-05-14

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  Brian Baer ,  Zackary Crane ,  Weidong Liu ,  Daniel John Watson

IPC: A61K31/506 ,  A61K9/00 ,  C07D207/16 ,  C07D403/14 ,  A61K45/06

CPC classification number: A61K31/506 ,  A61K9/0053 ,  A61K45/06 ,  C07D207/16 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.

公开(公告)号：US09598376B2

公开(公告)日：2017-03-21

申请号：US15053441

申请日：2016-02-25

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

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：US09562017B2

公开(公告)日：2017-02-07

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 ,  C07D235/06

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。 化合物I

公开(公告)号：US09546156B2

公开(公告)日：2017-01-17

申请号：US14442584

申请日：2013-11-12

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  James F. Blake ,  Barbara J. Brandhuber ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Rui Xu ,  Shannon L. Winski

IPC: C07D231/40 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

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.

Abstract translation: 式（I）的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，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可以 用TrkA激酶抑制剂治疗，如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些传染病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征。

公开(公告)号：US20160375002A1

公开(公告)日：2016-12-29

申请号：US15169149

申请日：2016-05-31

Applicant: Array BioPharma Inc.

Inventor： Kurtis D. Davies ,  Stefan Gross

IPC: A61K31/4545 ,  A61K31/7068 ,  A61K31/4745 ,  A61K31/519

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.

公开(公告)号：US20160280690A1

公开(公告)日：2016-09-29

申请号：US14442495

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： Barbara J. Brandhuber ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D403/14 ,  C07D403/12 ,  C07D401/14

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D403/12

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.

Abstract translation: 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，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可治疗的疾病 具有TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征。