MCHR1 inhibitors(Schering-Plough Research Institute)(MCHR1 inhibitors(Schering-Plough Research Institute))

概要

基本信息

药物类型

小分子化药

别名-

靶点

MCHR1

作用方式

抑制剂

作用机制

MCHR1抑制剂(黑色素浓缩激素受体-1抑制剂)

治疗领域

内分泌与代谢疾病

在研适应症-

非在研适应症

肥胖

原研机构

Schering-Plough Research Institute

在研机构-

非在研机构

Schering-Plough Research Institute

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 MCHR1 inhibitors(Schering-Plough Research Institute) 相关的临床结果

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100 项与 MCHR1 inhibitors(Schering-Plough Research Institute) 相关的转化医学

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100 项与 MCHR1 inhibitors(Schering-Plough Research Institute) 相关的专利（医药）

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1

项与 MCHR1 inhibitors(Schering-Plough Research Institute) 相关的文献（医药）

2005-07-01·Journal of medicinal chemistry1区 · 医学

Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

1区 · 医学

Article

作者: Farley, Constance ; Cook, John ; Clader, John W. ; McBriar, Mark D. ; Greenlee, William J. ; van Heek, Margaret ; Weig, Blair ; Graziano, Michael ; Shapiro, Sherry ; Spar, Brian ; Palani, Anandan ; Kowalski, Timothy J. ; O'Neill, Kim ; Hawes, Brian

Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound 1 exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.

100 项与 MCHR1 inhibitors(Schering-Plough Research Institute) 相关的药物交易

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