RP-66784(RP-66784) - 药物靶点：Kv7.2 x Potassium channel_在研适应症：心绞痛，高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Kv7.2 x Potassium channel

作用机制

Kv7.2激动剂(电压门控性钾通道蛋白亚型Kv7.2激动剂)、钾离子通道激动剂

治疗领域

神经系统疾病心血管疾病

在研适应症

心绞痛高血压

非在研适应症-

原研机构

Sanofi

在研机构

Rhone-Poulenc Rorer Ltd.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C21H27N3O2S2

InChIKeyGLFXCUUHWBFHSB-AURADERDSA-N

CAS号137392-34-8

关联

100 项与 RP-66784 相关的临床结果

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100 项与 RP-66784 相关的转化医学

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100 项与 RP-66784 相关的专利（医药）

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1

项与 RP-66784 相关的文献（医药）

1993-05-01·Journal of Medicinal Chemistry1区 · 医学

Syntheses and biological activities of potent potassium channel openers derived from (.+-.)-2-oxo-1-pyridin-3-yl-cyclohexanecarbothioic acid methylamide: new potassium channel openers

1区 · 医学

Article

作者: Walsh, Roger J. A. ; Brown, Thomas J. ; Mason, Jonathan S. ; Palfreyman, Malcolm N. ; Vicker, Nigel ; Chapman, Robert F.

The syntheses and biological activities of (+/-)-2-(cyanomethylene)-1-pyridin-3-ylcyclohexanecarbothioic++ + acid methylamide (6) and trans-(+/-)-2-(cyanomethyl)-1-pyridin-3-ylcyclohexanecarbothioic acid methylamide (14) derived from (+/-)-2-oxo-1-pyridin-3-ylcyclohexanecarbothioic acid methylamide (4) are reported. Compounds were tested for antagonism of potassium-induced contraction of de-endothelialized rat aorta. The effects of modification of 6 and 14 on in vitro K(+)-channel opening activity are presented. These new series of potassium channel openers so derived are best exemplified by (+/-)-2-[2-(phenylsulfanyl)ethylidene]-1-pyridin-3-ylcyclohexan ecarbothioic acid methylamide (13d, RP 66266) and trans-(+/-)-2-[2-[(phenylsulfonyl)amino]ethyl]-1-pyridin-3- ylcyclohexanecarbothioic acid methylamide (25a, RP 66784), which have IC90 values of 3 and 0.3 nM, respectively. The potency of the most active compounds indicates a possible interaction at an extra binding site. The compounds described herein are potential antihypertensive and antianginal agents.

100 项与 RP-66784 相关的药物交易

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