公开(公告)号：US08193231B2

公开(公告)日：2012-06-05

申请号：US12826158

申请日：2010-06-29

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-chloro-phenylamino)-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-氯 - 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 其中。 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。

公开(公告)号：US08193229B2

公开(公告)日：2012-06-05

申请号：US12824521

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 methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 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.

Abstract translation: 公开了治疗哺乳动物中过度增殖性疾病或与血管发生或血管发生相关的疾病的方法，包括向所述哺乳动物施用有效量的下式化合物或其药学上可接受的盐，其中A，R 1，R 2，R 7， R8和R9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。

公开(公告)号：US08178693B2

公开(公告)日：2012-05-15

申请号：US12824559

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 and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 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: 公开了式及其药学上可接受的盐和前药的化合物，其中A，R 1，R 2，R 7，R 8和R 9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：US20120108568A1

公开(公告)日：2012-05-03

申请号：US13382858

申请日：2010-07-09

Applicant: Shelley Allen ,  Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

Inventor： Shelley Allen ,  Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

IPC: A61K31/519 ,  A61K31/5377 ,  A61P33/02 ,  A61P35/00 ,  A61P29/00 ,  A61P25/28 ,  C07D487/04 ,  A61P25/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

Abstract: Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物及其盐是Trk激酶的抑制剂，可用于治疗可用 一种Trk激酶抑制剂，如疼痛，癌症，炎症，神经变性疾病和某些传染病。

公开(公告)号：US08138181B2

公开(公告)日：2012-03-20

申请号：US12593879

申请日：2008-03-27

Applicant: Shelley Allen ,  Julie Marie Greschuk ,  Nicholas C. Kallan ,  Fredrik P. Marmsäter ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  Qian Zhao ,  Joseph P. Lyssikatos

Inventor： Shelley Allen ,  Julie Marie Greschuk ,  Nicholas C. Kallan ,  Fredrik P. Marmsäter ,  Mark C. Munson ,  James P. Rizzi ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  Qian Zhao ,  Joseph P. Lyssikatos

IPC: A61K31/5386 ,  A61K31/437 ,  A61K31/506 ,  C07D471/02 ,  C07D401/14 ,  C07D498/08 ,  A61P35/04

CPC classification number: C07D471/04

Abstract: Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.

Abstract translation: 式I化合物：其中A，B，R 1，R 1a，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中给出的含义，是受体酪氨酸抑制剂，其可用于治疗由3类和 5类受体酪氨酸激酶。 本发明的具体化合物也被发现是Pim-1的抑制剂。

公开(公告)号：US08101639B2

公开(公告)日：2012-01-24

申请号：US12577312

申请日：2009-10-12

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

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

IPC: A61K31/44

CPC classification number: C07D213/78 ,  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 I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and 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和V的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：US08101611B2

公开(公告)日：2012-01-24

申请号：US13076267

申请日：2011-03-30

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

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

IPC: A61K31/50

CPC classification number: C07D213/78 ,  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 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和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：US20110319632A1

公开(公告)日：2011-12-29

申请号：US13229491

申请日：2011-09-09

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

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

Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供具有式VIIIa-1的化合物：其中Z，X5，R2，R2a和R10如本文所定义。 式VIIIa-1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：US20110275608A1

公开(公告)日：2011-11-10

申请号：US13143998

申请日：2010-01-07

Applicant: Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

Inventor： Martha E. Rodriguez ,  David A. Mareska ,  Jeremy J. Hans ,  Darren M. Harvey ,  Robert D. Groneberg ,  Michael O'Sullivan

IPC: A61K31/454 ,  C07D417/14 ,  C07D413/14 ,  C07D409/06 ,  C07D417/06 ,  C07D401/06 ,  A61K31/4535 ,  C07D409/14 ,  A61K31/4725 ,  C07D471/04 ,  A61K31/437 ,  C07D498/04 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/10 ,  C07D413/06

CPC classification number: C07D413/14 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04

Abstract: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.

Abstract translation: 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。

公开(公告)号：US08022223B2

公开(公告)日：2011-09-20

申请号：US12282600

申请日：2007-03-23

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

Inventor： Thomas D. 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 of formula I that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes meilitus. 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: 提供式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活性介导的疾病，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。