公开(公告)号：US08183385B2

公开(公告)日：2012-05-22

申请号：US11917998

申请日：2006-06-21

Applicant: John DeMattei ,  Sagar Shakya ,  Paul J. Nichols ,  Bradley R. Barnett ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  John Leonard

Inventor： John DeMattei ,  Sagar Shakya ,  Paul J. Nichols ,  Bradley R. Barnett ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  John Leonard

IPC: C07C235/08

CPC classification number: C07D235/08 ,  C07D235/06

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X1, X2, X5, R1, R2 and R4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ia-2的苯并咪唑羧酸核心结构及其合成中间体：其中X 1，X 2，X 5，R 1，R 2和R 4如本文所定义。 式Ia-2及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：US08163738B2

公开(公告)日：2012-04-24

申请号：US12064196

申请日：2006-08-17

Applicant: George A. Doherty ,  Zachary Jones

Inventor： George A. Doherty ,  Zachary Jones

IPC: A61P37/02 ,  A61K31/5513 ,  C07D243/20

CPC classification number: C07D243/20

Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US08044083B2

公开(公告)日：2011-10-25

申请号：US12161412

申请日：2007-01-26

Applicant: Robert Groneberg ,  Laurence E. Burgess ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

Inventor： Robert Groneberg ,  Laurence E. Burgess ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

IPC: A61K31/416 ,  C07D231/56

CPC classification number: C07D231/40 ,  C07D231/56

Abstract: The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.

Abstract translation: 式（I）化合物及其药学上可接受的盐和前药可用于治疗和预防由激酶介导的各种疾病。

公开(公告)号：US08039639B2

公开(公告)日：2011-10-18

申请号：US13020578

申请日：2011-02-03

Applicant: Robert Groneberg ,  Laurence E. Burges ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

Inventor： Robert Groneberg ,  Laurence E. Burges ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

IPC: C07D231/56

CPC classification number: C07D231/40 ,  C07D231/56

Abstract: A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof.

Abstract translation: 式II化合物及其盐可用于制备式I化合物及其药学上可接受的盐和前药。

公开(公告)号：US08039637B2

公开(公告)日：2011-10-18

申请号：US11993745

申请日：2006-06-21

Applicant: John DeMattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

Inventor： John DeMattei ,  Sagar Shakya ,  Anthony D. Piscopio ,  Bruno P. Hache ,  Matthew Charles Evans ,  James Gair Ford ,  Simon Mark Pointon ,  Koen Peeters ,  Timothy John Lilley ,  John Leonard

IPC: C07D235/06 ,  C07D235/08 ,  C07D403/04 ,  C07D403/06

CPC classification number: C07D235/06 ,  C07C201/08 ,  C07C205/58 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18 ,  C07C229/60

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X1，X2，X5，R2和R10如本文所定义。 式Ia-1及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：US08026233B2

公开(公告)日：2011-09-27

申请号：US12294550

申请日：2007-03-27

Applicant: Mark C. Munson ,  Kevin W. Hunt ,  Christopher T. Clark ,  Ganghyeok Kim ,  Laurence E. Burgess ,  James P. Rizzi

Inventor： Mark C. Munson ,  Kevin W. Hunt ,  Christopher T. Clark ,  Ganghyeok Kim ,  Laurence E. Burgess ,  James P. Rizzi

IPC: C07D403/12 ,  C07D401/12 ,  A61K31/416

CPC classification number: C07D403/12 ,  C07D401/12

Abstract: Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.

Abstract translation: 式（I）化合物：其中A，B，X，Ar 1，R 8和R 4具有本说明书中给出的任何含义，是可用于治疗和预防由p38介导的各种疾病的p38的抑制剂。

公开(公告)号：US08003662B2

公开(公告)日：2011-08-23

申请号：US11699830

申请日：2007-01-30

Applicant: James F. Blake ,  Steven Boyd ,  Jason De Meese ,  John J. Gaudino ,  Allison L. Marlow ,  Jeongbeob Seo ,  Allen A. Thomas ,  Hongqi Tian

Inventor： James F. Blake ,  Steven Boyd ,  Jason De Meese ,  John J. Gaudino ,  Allison L. Marlow ,  Jeongbeob Seo ,  Allen A. Thomas ,  Hongqi Tian

IPC: A61K31/4365

CPC classification number: C07D495/04 ,  C07D519/00

Abstract: Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I 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化合物及其药学上可接受的盐可用于抑制受体酪氨酸激酶和用于治疗由此介导的病症。 公开了使用式I化合物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：US07973170B2

公开(公告)日：2011-07-05

申请号：US12824497

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 ,  C07D235/06

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 compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, 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. Also disclosed is a method 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W，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中的过度增生性疾病，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，以及含有这些化合物的药物组合物。

公开(公告)号：US20110124878A1

公开(公告)日：2011-05-26

申请号：US13020578

申请日：2011-02-03

Applicant: Robert Groneberg ,  Laurence E. Burges ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

Inventor： Robert Groneberg ,  Laurence E. Burges ,  Darren Harvey ,  Ellen Laird ,  Mark C. Munson ,  James P. Rizzi ,  Martha Rodriguez ,  Charles Todd Eary ,  Daniel John Watson

IPC: C07D231/56

CPC classification number: C07D231/40 ,  C07D231/56

Abstract: A compound of Formula II and salts thereof are useful in the preparation of a compound of Formula I and pharmaceutically acceptable salts and prodrugs thereof.

Abstract translation: 式II化合物及其盐可用于制备式I化合物及其药学上可接受的盐和前药。

公开(公告)号：US20110003809A1

公开(公告)日：2011-01-06

申请号：US12919981

申请日：2009-02-27

Applicant: Kateri A. Ahrendt

Inventor： Kateri A. Ahrendt

IPC: A61K31/5377 ,  C07D471/02 ,  A61K31/437 ,  C07C63/06 ,  C07D413/14 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07C311/48

Abstract: Compounds of Formula I are useful for inhibition of Raf 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Raf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。