公开(公告)号：US20170107232A1

公开(公告)日：2017-04-20

申请号：US15350888

申请日：2016-11-14

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: C07D498/22 ,  C07D471/22

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 and R3a 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：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：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：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.

公开(公告)号：US20160280682A1

公开(公告)日：2016-09-29

申请号：US14442613

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

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

CPC classification number: C07D401/14 ,  A61P29/00 ,  A61P35/00 ,  C07D403/12 ,  C07D403/14

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, Ring B, and Ring C are as defined herein, and wherein Ring B 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

公开(公告)号：US20160137654A1

公开(公告)日：2016-05-19

申请号：US14943014

申请日：2015-11-16

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04

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.

Abstract translation: （S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基） - 吡唑并[1,5-a]嘧啶-3-基） - 3-羟基吡咯烷-1-甲酰胺，含有所述结晶形式的药物组合物和所述结晶形式用于治疗疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的用途。 在一些实施方案中，新的结晶形式包含（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基） - 吡唑并[1,5-a ]嘧啶-3-基）-3-羟基吡咯烷-1-甲酰胺硫酸氢盐。 本发明进一步涉及制备新型结晶形式的方法。

公开(公告)号：US20160122316A1

公开(公告)日：2016-05-05

申请号：US14993985

申请日：2016-01-12

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: C07D401/04 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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：US09328091B2

公开(公告)日：2016-05-03

申请号：US14523481

申请日：2014-10-24

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Anna Leivers ,  Josef R. Bencsik ,  James F. Blake ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

IPC: C07D239/70 ,  C07D401/10 ,  C07D401/04 ,  C07D409/04 ,  C07D417/04 ,  C07D487/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D417/10 ,  C07D211/08 ,  C07D211/46

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. 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.

Abstract translation: 式I化合物可用于抑制AKT蛋白激酶。 公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。