公开(公告)号：US08431574B2

公开(公告)日：2013-04-30

申请号：US12356441

申请日：2009-01-20

Applicant: James F. Blake ,  Joseph P. Lyssikatos ,  Hong-Woon Yang ,  Eli M. Wallace

Inventor： James F. Blake ,  Joseph P. Lyssikatos ,  Hong-Woon Yang ,  Eli M. Wallace

IPC: A01N43/58 ,  A61K31/50 ,  C07D237/00

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 Formulas III and IV and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and R10 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III和IV的化合物及其药学上可接受的盐和前药，其中R 1，R 2，R 7，R 8，R 9和R 10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性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US08362056B2

公开(公告)日：2013-01-29

申请号：US12739560

申请日：2008-11-04

Applicant: George A. Doherty

Inventor： George A. Doherty

IPC: A01N43/52 ,  A01N43/56 ,  A01N43/38 ,  A61K31/415 ,  A61K31/405 ,  C07D235/00 ,  C07D231/56 ,  C07D209/04

CPC classification number: C07D209/08 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08

Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中D1，D2，R1，R2，R7，R8和A具有本说明书中给出的含义的式I化合物是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US20120329808A1

公开(公告)日：2012-12-27

申请号：US12307526

申请日：2007-07-05

Applicant: Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

IPC: A61K31/519 ,  A61P29/00 ,  A61P15/02 ,  A61P9/00 ,  A61P25/28 ,  A61P17/00 ,  C07D495/04 ,  A61P35/00

CPC classification number: C07D495/04

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: 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: 本发明提供了包括分解对映异构体，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：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：US08299076B2

公开(公告)日：2012-10-30

申请号：US11914433

申请日：2006-05-17

Applicant: Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  Jim Blake ,  Richard Anthony Storey ,  Rebecca Jane Booth ,  John David Pittam ,  John Leonard ,  Mark Richard Fielding

Inventor： Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  Jim Blake ,  Richard Anthony Storey ,  Rebecca Jane Booth ,  John David Pittam ,  John Leonard ,  Mark Richard Fielding

IPC: A01N43/58 ,  A01N43/54 ,  A01N43/40 ,  C07D401/00 ,  C07D239/02 ,  C07D487/00 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D237/24 ,  C07D213/80 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85

Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide 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: 公开了可用于治疗过度增殖的2-（2-氟-4-碘苯基氨基）-N-（2-羟基乙氧基）-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺的结晶形式 疾病，如癌症和炎症，哺乳动物和炎症病症。 还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US20120263679A1

公开(公告)日：2012-10-18

申请号：US13484093

申请日：2012-05-30

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

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

IPC: A61K31/4412 ,  A61K31/7088 ,  A61K39/395 ,  A61K31/4704 ,  A61K38/17 ,  A61P35/00 ,  A61P31/04 ,  A61P9/00 ,  A61P5/28 ,  A61P37/00 ,  A61K38/21 ,  A61K48/00

CPC classification number: C07D213/80 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/46 ,  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 ,  A61K2300/00

Abstract: Disclosed are combinations comprising (a) a compound of the Formula: wherein R1, R2, R7, R8, R9 and W are as defined in the specification, and (b) at least one additional therapeutic agent. Such combinations are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such combinations in the treatment of hyperproliferative diseases and inflammatory conditions in mammals.

Abstract translation: 公开了包含（a）下式化合物的组合：其中R 1，R 2，R 7，R 8，R 9和W如说明书中所定义，和（b）至少一种另外的治疗剂。 这样的组合可用于治疗过度增生性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些组合来治疗哺乳动物中过度增殖性疾病和炎性病症的方法。

公开(公告)号：US08268852B2

公开(公告)日：2012-09-18

申请号：US12356415

申请日：2009-01-20

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

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

IPC: A01N43/40 ,  A61K31/435

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 I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, X and Y 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I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8，R9，W，X和Y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性疾病的方法和含有这些化合物的药物组合物。

公开(公告)号：US08236825B2

公开(公告)日：2012-08-07

申请号：US13093729

申请日：2011-04-25

Applicant: Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Joseph P. Lyssikatos ,  Thomas D. Aicher ,  Ellen R Laird ,  John Robinson ,  Shelley Allen

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Joseph P. Lyssikatos ,  Thomas D. Aicher ,  Ellen R Laird ,  John Robinson ,  Shelley Allen

IPC: A61K31/4439 ,  C07D417/04

CPC classification number: C07D285/12 ,  C07D271/107 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07F9/201 ,  C07F9/65392

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

公开(公告)号：US08212045B2

公开(公告)日：2012-07-03

申请号：US12678995

申请日：2008-09-15

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: A61K31/44 ,  C07D417/00

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：US20120157452A1

公开(公告)日：2012-06-21

申请号：US13393076

申请日：2010-08-27

Applicant: Stefan Gradl ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

Inventor： Stefan Gradl ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

IPC: A61K31/437 ,  A61P35/00 ,  A61P13/12 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/497 ,  A61K31/5377 ,  C07D471/04 ,  A61K31/444

CPC classification number: C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers 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. [FORMULA I]

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。 [公式I]

公开(公告)号：US08193230B2

公开(公告)日：2012-06-05

申请号：US12824547

申请日：2010-06-28

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

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 pharmaceutical compositions 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. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.

Abstract translation: 公开了包含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） - 酰胺或其药学上可接受的盐的药物组合物。 还公开了使用这种组合物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。