公开(公告)号：US20130195971A1

公开(公告)日：2013-08-01

申请号：US13747853

申请日：2013-01-23

Applicant: AstraZeneca AB ,  Array BioPharma, Inc.

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

IPC: 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.

公开(公告)号：US08394795B2

公开(公告)日：2013-03-12

申请号：US12920050

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven Mark Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven Mark Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K31/535 ,  A61K31/44 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和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：US08372842B2

公开(公告)日：2013-02-12

申请号：US12812448

申请日：2009-01-08

Applicant: James F. Blake ,  Indrani W. Gunawardana ,  Yvan Le Huerou ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang

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

IPC: A61K31/496 ,  C07D471/04

CPC classification number: C07D471/04

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：US08354540B2

公开(公告)日：2013-01-15

申请号：US13191994

申请日：2011-07-27

Applicant: Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

Inventor： Thomas Daniel Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Ronald Jay Hinklin ,  Ajay Singh

IPC: C07D417/00 ,  C07D401/00

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

公开(公告)号：US08338452B2

公开(公告)日：2012-12-25

申请号：US12920045

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs 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Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和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：US20120277277A1

公开(公告)日：2012-11-01

申请号：US13463487

申请日：2012-05-03

Applicant: Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

Inventor： Eli M. Wallace ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  T. Brian Hurley

IPC: A61K31/4184 ,  A61P17/00 ,  A61P35/00

CPC classification number: C07D235/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

Abstract: Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy.

Abstract translation: 公开了抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法，包括向哺乳动物施用包含6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑的药物组合物 -5-羧酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐与有效量的抗肿瘤剂组合或与放射治疗组合。

公开(公告)号：US20120277242A1

公开(公告)日：2012-11-01

申请号：US13493616

申请日：2012-06-11

Applicant: Thomas Daniel AICHER ,  Steven Armen BOYD ,  Mark Joseph CHICARELLI ,  Kevin Ronald CONDROSKI ,  Jay Bradford FELL ,  John P. FISCHER ,  Indrani W. GUNAWARDANA ,  Ronald Jay HINKLIN ,  Ajay SINGH ,  Timothy M. TURNER ,  Eli M. WALLACE

Inventor： Thomas Daniel AICHER ,  Steven Armen BOYD ,  Mark Joseph CHICARELLI ,  Kevin Ronald CONDROSKI ,  Jay Bradford FELL ,  John P. FISCHER ,  Indrani W. GUNAWARDANA ,  Ronald Jay HINKLIN ,  Ajay SINGH ,  Timothy M. TURNER ,  Eli M. WALLACE

IPC: A61K31/444 ,  C07D417/12 ,  A61P3/10 ,  A61K31/4709 ,  A61K31/501 ,  C07D417/14 ,  A61K31/4439

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract translation: 提供式（I）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可以 通过激活葡糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损））以及其它疾病和病症如本文讨论的疾病和病症。

公开(公告)号：US20120232055A1

公开(公告)日：2012-09-13

申请号：US13272079

申请日：2011-10-12

Applicant: Ian S. MITCHELL ,  James F. BLAKE ,  Rui XU ,  Nicholas C. KALLAN ,  Dengming XIAO ,  Keith Lee SPENCER ,  Josef R. BENCSIK ,  Eli M. WALLACE ,  Stephen T. SCHLACHTER ,  Anna L. BANKA ,  Jun LIANG ,  Brian SAFINA ,  Birong ZHANG ,  Christine CHABOT ,  Steven DO

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. SCHLACHTER ,  Anna L. BANKA ,  Jun LIANG ,  Brian SAFINA ,  Birong ZHANG ,  Christine CHABOT ,  Steven DO

IPC: A61K31/517 ,  A61K31/5377 ,  A61K31/553 ,  A61P17/00 ,  A61P35/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/02 ,  A61K31/541 ,  A61P29/00

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：US08211921B2

公开(公告)日：2012-07-03

申请号：US12356428

申请日：2009-01-20

Applicant: James F. Blake ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  Jeongbeob Seo ,  Eli M. Wallace ,  Hong-Woon Yang

Inventor： James F. Blake ,  Joseph P. Lyssikatos ,  Allison L. Marlow ,  Jeongbeob Seo ,  Eli M. Wallace ,  Hong-Woon Yang

IPC: A61K31/4412 ,  C07D213/80 ,  C07D213/82 ,  A61K31/4965 ,  C07D241/28

CPC classification number: C07D209/46 ,  C07D213/80 ,  C07D213/82 ,  C07D215/48 ,  C07D231/56 ,  C07D237/24 ,  C07D237/28 ,  C07D237/32 ,  C07D239/74 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract translation: 公开了式及其药学上可接受的盐和前药的化合物，其中R1，R2，R7，R8，R9，W和X如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。 还公开了使用这些化合物治疗哺乳动物中过度增殖疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US20120157439A1

公开(公告)日：2012-06-21

申请号：US13393163

申请日：2010-08-27

Applicant: Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Rebecca Pulk ,  Joachim Rudolph ,  Zhaoyang Wen ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

Inventor： Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Rebecca Pulk ,  Joachim Rudolph ,  Zhaoyang Wen ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

IPC: A61K31/519 ,  C07D495/04 ,  A61P35/00 ,  A61K31/5377 ,  A61K31/53 ,  C07D487/04 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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Raf激酶。 公开了使用式I化合物和其立体异构体，互变异构体，前药和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。