Delving into the Latest Updates on RP-66784 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

Kv7.2 x Potassium channel

Mechanism

Kv7.2 agonists(Voltage-gated potassium channel subunit Kv7.2 agonists), Potassium channel agonists

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Angina PectorisHypertension

Inactive Indication-

Originator Organization

Sanofi

Active Organization

Rhone-Poulenc Rorer Ltd.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC21H27N3O2S2

InChIKeyGLFXCUUHWBFHSB-AURADERDSA-N

CAS Registry137392-34-8

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 Deals associated with RP-66784

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