Delving into the Latest Updates on GSK-345931A with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

EP1

Mechanism

EP1 antagonists(Prostanoid EP1 receptor antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Inflammatory pain

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC22H20ClNO3

InChIKeyRVMVCPKCWWFOEL-UHFFFAOYSA-N

CAS Registry869534-13-4

Herein we describe the medicinal chemistry programme to identify a potential back-up compound to the EP(1) receptor antagonist GW848687X. This work started with the lipophilic 1,2-biaryl benzene derivative 4 which displayed molecular weight of 414.9g/mol and poor in vivo metabolic stability in the rat and resulted in the identification of compound 7i (GSK345931A) which demonstrated good metabolic stability in the rat and lower molecular weight (381.9g/mol). In addition, 7i (GSK345931A) showed measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.

100 Deals associated with GSK-345931A

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