公开(公告)号：US20160030574A1

公开(公告)日：2016-02-04

申请号：US14884343

申请日：2015-10-15

Applicant: AstraZeneca AB ,  Array BioPharma, Inc.

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

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

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.

公开(公告)号：US20150045391A1

公开(公告)日：2015-02-12

申请号：US14454626

申请日：2014-08-07

Applicant: Array BioPharma Inc.

Inventor： Deborah A. Anderson ,  Michael J. Humphries ,  Robert A. Rieger ,  Lance M. Williams

IPC: A61K31/454 ,  A61K31/433

CPC classification number: A61K31/454 ,  A61K31/433 ,  A61K2300/00

Abstract: A combination of filanesib and pomalidomide for treating patients is provided.

Abstract translation: 提供了用于治疗患者的西班珠菌素和派洛他米特的组合。

公开(公告)号：US20140349997A1

公开(公告)日：2014-11-27

申请号：US14458062

申请日：2014-08-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlacter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: C07D413/12 ,  C07D401/12 ,  C07D409/14 ,  C07D407/12 ,  C07D409/12 ,  C07D239/70 ,  C07D403/12

CPC classification number: A61K31/517 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。

公开(公告)号：US20140309226A1

公开(公告)日：2014-10-16

申请号：US14359036

申请日：2012-11-14

Applicant: Array BioPharma Inc.

Inventor： Jay Bradford Fell ,  John P. Fischer ,  Ronald J. Hinklin

IPC: C07D417/14 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X1, X2, R3, R4, R5, Rx, R7, R9, R10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

Abstract translation: 其中X1，X2，R3，R4，R5，Rx，R7，R9，R10和n具有本说明书中给出的含义的式I化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗 或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

公开(公告)号：US20140234376A1

公开(公告)日：2014-08-21

申请号：US14180939

申请日：2014-02-14

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

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

IPC: C07D223/16 ,  C07D405/04 ,  C07D401/04 ,  C07D405/10 ,  C07D401/12 ,  C07D403/10

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-verses-host disease.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，感染性疾病，炎性疾病，移植物排斥反应和移植物宿主病。

公开(公告)号：US20140228349A1

公开(公告)日：2014-08-14

申请号：US14351415

申请日：2012-10-09

Applicant: Array BioPharma Inc.

Inventor： Mark Laurence Boys ,  Laurence E. Burgess ,  C. Todd Eary ,  Robert Groneberg ,  Bruno P. Hache ,  Darren Harvey ,  Erik James Hicken ,  Christopher F. Kraser ,  Ellen Laird ,  David A. Moreno ,  Mark C. Munson ,  Li Ren ,  John E. Robinson ,  Stephen T. Schlachter

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract translation: R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂化物是一种或多种JAK激酶的抑制剂，并且是有用的 治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。

公开(公告)号：US08758830B2

公开(公告)日：2014-06-24

申请号：US13974895

申请日：2013-08-23

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: A61K31/4545 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/444 ,  A61K31/501 ,  A61K35/00 ,  A61K33/24

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：US20140100369A1

公开(公告)日：2014-04-10

申请号：US13974895

申请日：2013-08-23

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.

公开(公告)号：US20130252934A1

公开(公告)日：2013-09-26

申请号：US13782513

申请日：2013-03-01

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: A61K31/506 ,  C07D401/04 ,  A61K45/06 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  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.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体，前药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：US20040014643A1

公开(公告)日：2004-01-22

申请号：US10389012

申请日：2003-03-14

Applicant: Array BioPharma Inc.

Inventor： Barbara J. Brandhuber ,  Guy P.A. Vigers

IPC: A61K038/16 ,  G06F019/00 ,  G01N033/48 ,  G01N033/50 ,  C07K014/715

CPC classification number: A61K38/2006 ,  C07K14/7155 ,  C07K2299/00 ,  G01N33/6869 ,  G01N2333/715 ,  G06F19/16

Abstract: Crystals comprising a modified interleukin-1 type 1 receptor (IL-1R1) and one or more modulators of IL-1 activity are described. Methods of identifying potential inhibitors of IL-1 activity are also described. Compositions and methods for the treatment of IL-1 mediated diseases, such as rheumatoid arthritis, osteoarthritis, and other inflammatory conditions, are described.

Abstract translation: 描述了包含修饰的白细胞介素-1型受体（IL-1R1）和一种或多种IL-1活性调节剂的晶体。 还描述了识别IL-1活性的潜在抑制剂的方法。 描述了用于治疗IL-1介导的疾病如类风湿性关节炎，骨关节炎和其它炎性病症的组合物和方法。