公开(公告)号：US08865726B2

公开(公告)日：2014-10-21

申请号：US13393767

申请日：2010-09-03

Applicant: Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Lisa A. De Meese ,  Jay Bradford Fell ,  John P. Fischer ,  John A. Josey ,  Kevin Koch ,  Yvan Le Huerou ,  Gregory F. Miknis ,  Martha E. Rodriguez ,  George T. Topalov ,  Eli M. Wallace ,  Rui Xu

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.

Abstract translation: 式I化合物及其盐，其中R 1，R 2，R 2a，R 3，n，X和环B具有本说明书中给出的含义，是mTOR的抑制剂，可用于治疗对抑制作用敏感的疾病 mTOR，如癌症。

公开(公告)号：US08865698B2

公开(公告)日：2014-10-21

申请号：US13943590

申请日：2013-07-16

Applicant: Array BioPharma Inc.

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

IPC: A61K31/55 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof 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.

Abstract translation: 本文提供了用于治疗哺乳动物的疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的方法，其包括向有需要的所述哺乳动物施用治疗有效量的式I化合物：其中R1，R2，R3， R4，X，Y和n具有说​​明书中给出的含义。

公开(公告)号：US08853216B2

公开(公告)日：2014-10-07

申请号：US12811983

申请日：2009-01-09

Applicant: Josef Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Steven Do ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  James Graham

Inventor： Josef Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Steven Do ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  James Graham

IPC: C07D239/70 ,  A61K31/517 ,  A61P35/00 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P15/02 ,  A61P17/00

CPC classification number: C07D239/70

Abstract: The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包含式I的化合物及其药学上可接受的盐。还提供了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。

公开(公告)号：US20140243520A1

公开(公告)日：2014-08-28

申请号：US14271129

申请日：2014-05-06

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

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.

Abstract translation: 式I的化合物可用于抑制CHK1和/或CHK2。 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。

公开(公告)号：US08809538B2

公开(公告)日：2014-08-19

申请号：US13143998

申请日：2010-01-07

Applicant: Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

Inventor： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

IPC: C07D403/00 ,  C07D403/14 ,  A61K31/454 ,  A61K31/4545

CPC classification number: C07D413/14 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04

Abstract: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.

Abstract translation: 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。

公开(公告)号：US20140221443A1

公开(公告)日：2014-08-07

申请号：US14152766

申请日：2014-01-10

Applicant: Astrazeneca AB ,  Array BioPharma Inc.

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：US20140221370A1

公开(公告)日：2014-08-07

申请号：US14248836

申请日：2014-04-09

Applicant: Array BioPharma Inc.

Inventor： James F. Blake ,  Indrani W. Gunawardana ,  Yvan LeHuerou ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

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.

Abstract translation: 式（I）的化合物可用于抑制CHK1和/或CHK2。 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。

公开(公告)号：US08791123B2

公开(公告)日：2014-07-29

申请号：US13382858

申请日：2010-07-09

Applicant: Shelley Allen ,  Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

Inventor： Shelley Allen ,  Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

Abstract: Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物及其盐是Trk激酶的抑制剂，可用于治疗可用 一种Trk激酶抑制剂，如疼痛，癌症，炎症，神经变性疾病和某些传染病。

公开(公告)号：US20140194403A1

公开(公告)日：2014-07-10

申请号：US13943590

申请日：2013-07-16

Applicant: Array BioPharma Inc.

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

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof 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.

Abstract translation: 本文提供了用于治疗哺乳动物的疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的方法，其包括向有需要的所述哺乳动物施用治疗有效量的式I化合物：其中R1，R2，R3， R4，X，Y和n具有说​​明书中给出的含义。

公开(公告)号：US20140128442A1

公开(公告)日：2014-05-08

申请号：US14057498

申请日：2013-10-18

Applicant: Array BioPharma, Inc. ,  Novartis 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 ,  A61K47/38 ,  A61K47/26

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。