Delving into the Latest Updates on RP-69698 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

LTB4R

Mechanism

LTB4R antagonists(Leukotriene B4 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Inflammation

Originator Organization

Rhone-Poulenc SA

Active Organization-

Inactive Organization

Rhone-Poulenc SA

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

A series of omega-[(4,6-diphenyl-2-pyridyl)oxy]alkanoic acid derivatives was prepared which inhibited the binding of leukotriene B4 to its receptors on guinea pig spleen membranes and on human polymorphonuclear leukocytes (PMNs) and selectively antagonized the LTB4-induced elastase release in human PMNs. On the basis of these three screens, a structure-activity relationship was investigated. alpha-Substitution on the carboxylic acid side chain led to only small changes in the binding affinities but greatly enhanced the LTB4 antagonist activity. Substitution on the phenyl rings was also evaluated. The terminal carboxylic acid function can be replaced by a tetrazole ring without loss in activity. The best in vitro LTB4 antagonists of this series were investigated in vivo in the inhibition of LTB4-induced leukopenia in rabbits. Compound 9b (RP69698) displayed potent LTB4 antagonist activity, after oral administration, with an ED50 value of 6.7 mg/kg.

100 Deals associated with RP-69698

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