公开(公告)号：US20100324041A1

公开(公告)日：2010-12-23

申请号：US12812447

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: A61K31/5377 ,  C07D487/04 ,  A61K31/496 ,  A61P35/00

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. Formula, (I).

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。 公式，（一）。

公开(公告)号：US20100099697A1

公开(公告)日：2010-04-22

申请号：US12581072

申请日：2009-10-16

Applicant: Brian J. Tunquist ,  Duncan H. Walker ,  Richard D. Woessner

Inventor： Brian J. Tunquist ,  Duncan H. Walker ,  Richard D. Woessner

IPC: A61K31/437 ,  A61P35/00

CPC classification number: A61K31/433 ,  A61K31/00

Abstract: Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose.

Abstract translation: 治疗由细胞分裂引起的疾病或通过在允许回收或减少副作用的给药循环中的生物学有效剂量和最大耐受剂量之间施用两剂有丝分裂抑制剂来治疗由细胞分裂引起的疾病或通过抑制有丝分裂来治疗疾病的方法，其中 在第一剂后24至48小时施用第二剂量。

公开(公告)号：US20100056530A1

公开(公告)日：2010-03-04

申请号：US12092233

申请日：2006-10-24

Applicant: Thomas D. Aicher ,  Wai-man Lee ,  Ronald Jay Hinklin ,  Mark Joseph Chicarelli ,  Steven Armen Boyd ,  Kevin Ronald Condroski

Inventor： Thomas D. Aicher ,  Wai-man Lee ,  Ronald Jay Hinklin ,  Mark Joseph Chicarelli ,  Steven Armen Boyd ,  Kevin Ronald Condroski

IPC: A61K31/498 ,  C07D417/12 ,  C07D401/14 ,  C07D241/36 ,  A61K31/4439 ,  A61K31/444 ,  A61P3/10

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds of Formula I wherein R1, R2, Y, Z and G are as defined herein, 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.

Abstract translation: 本发明提供了其中R 1，R 2，Y，Z和G如本文所定义的式I化合物，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的糖蛋白水平介导的疾病，例如糖尿病。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：US20090247526A1

公开(公告)日：2009-10-01

申请号：US12161366

申请日：2007-01-24

Applicant: Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

Inventor： Thomas D. Aicher ,  Steven Armen Boyd ,  Mark Joseph Chicarelli ,  Kevin Ronald Condroski ,  Rustam Ferdinand Garrey ,  Ronald Jay Hinklin ,  Ajay Singh ,  Timothy M. Turner

IPC: A61K31/5377 ,  C07D417/12 ,  C07D413/14 ,  C07D409/14 ,  A61P3/10 ,  A61K31/497 ,  C07D417/02 ,  A61K31/4439

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

Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that 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化合物，其中R 2，L，Z，Y，G和R 1如本文所定义，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，或可由 激活葡萄糖激酶，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）），以及其他疾病和病症如本文讨论的疾病和病症。

公开(公告)号：US07576072B2

公开(公告)日：2009-08-18

申请号：US10992479

申请日：2004-11-18

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

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

IPC: A61K31/655 ,  C07D471/02

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 and R9, W, X, Y and Z are as defined in the specification. Such compounds are MEK inhibitors and are 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和R9，W，X，Y和Z如说明书中所定义。 这些化合物是MEK抑制剂，并且可用于治疗哺乳动物和炎性病症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和含有这些化合物的药物组合物。

公开(公告)号：US07566716B2

公开(公告)日：2009-07-28

申请号：US11436353

申请日：2006-05-18

Applicant: Ellen Laird ,  George Topalov ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse

Inventor： Ellen Laird ,  George Topalov ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse

IPC: A61K31/497

CPC classification number: C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates 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激酶和用于治疗由此介导的病症。 公开了使用式I化合物及其立体异构体，互变异构体，溶剂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：US20090143422A1

公开(公告)日：2009-06-04

申请号：US12364330

申请日：2009-02-02

Applicant: Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Groneberg ,  James Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

Inventor： Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Groneberg ,  James Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

IPC: A61K31/4375 ,  C07D231/54 ,  A61K31/416 ,  C07D261/20 ,  A61K31/42 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D231/56 ,  C07D261/20 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.

Abstract translation: 本发明涉及p38的抑制剂和利用该抑制剂及其药物组合物治疗和预防由p38介导的各种疾病的方法。

公开(公告)号：US20090143389A1

公开(公告)日：2009-06-04

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: A61K31/5025 ,  C07D487/04 ,  A61P35/00

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：US20080306050A1

公开(公告)日：2008-12-11

申请号：US12064196

申请日：2006-08-17

Applicant: George A. Doherty ,  Zachary Jones

Inventor： George A. Doherty ,  Zachary Jones

IPC: A61K31/5513 ,  C07D243/14 ,  A61P37/02

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：US20080177082A1

公开(公告)日：2008-07-24

申请号：US12050847

申请日：2008-03-18

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: 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.