SB-568849(SB-568849) - 药物靶点：MCHR1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

SB 568849

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

内分泌与代谢疾病其他疾病

在研适应症-

非在研适应症

焦虑症肥胖

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

权益机构-

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 SB-568849 相关的临床结果

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100 项与 SB-568849 相关的转化医学

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100 项与 SB-568849 相关的专利（医药）

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2

项与 SB-568849 相关的文献（医药）

2006-09-01·Bioorganic & medicinal chemistry letters4区 · 医学

SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849

4区 · 医学

Article

作者: Muir, Alison I. ; Witty, David R. ; O'Hanlon, Peter J. ; Stemp, Geoffrey ; Jeffrey, Phillip ; Stevens, Alex J. ; Hervieu, Guillaume J. ; Thewlis, Kevin M. ; Johnson, Christopher N. ; Winborn, Kim Y. ; Wilson, Shelagh ; Bateson, John H.

We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were utilised to allow rapid exploration of the structure-activity relationship around this template, leading to compound SB-568849 which possessed good receptor affinity and selectivity. This compound proved to be an antagonist with stability in vivo, an acceptable brain-blood ratio and oral bioavailability.

2006-09-01·Bioorganic & medicinal chemistry letters4区 · 医学

Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

4区 · 医学

Article

作者: Jeffrey, Phillip ; O'Hanlon, Peter J. ; Muir, Alison I. ; Stemp, Geoffrey ; Johnson, Christopher N. ; Winborn, Kim Y. ; Al-Barazanji, Kamal ; Stevens, Alex J. ; Witty, David R. ; Thewlis, Kevin ; Haynes, Andrea ; Hervieu, Guillaume J. ; Hamprecht, Dieter ; Bateson, John

A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.

100 项与 SB-568849 相关的药物交易

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