Delving into the Latest Updates on RGH-560 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CHRNA7

Mechanism

α7 receptor modulators(Neuronal acetylcholine receptor protein alpha-7 subunit modulators)

Therapeutic Areas

Nervous System Diseases

Active Indication

Amnesia

Inactive Indication-

Originator Organization

Gedeon Richter Romania SA

Active Organization

Gedeon Richter Romania SA

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC22H20FN3O3

InChIKeyLXOXUGXUUINWLS-UHFFFAOYSA-N

CAS Registry2408799-43-7

Author: Balázs, Ottilia ; Makó, Attila ; Némethy, Zsolt ; Greiner, István ; Vastag, Mónika ; Laszy, Judit ; Éles, János ; Fodor, László ; Vágó, István ; Thán, Márta ; Tapolcsányi, Pál ; Kolok, Sándor ; Ledneczki, István ; Visegrády, András ; Ilkei, Viktor ; Molnár, Katalin Dudásné ; Szigetvári, Áron ; Bata, Imre ; Lendvai, Balázs ; Krámos, Balázs ; Lévay, György

During optimization of a previously identified lead compound, attempts were made to optimize the reactive indole structural element, the suboptimal metabolic stability, as well as the low kinetic solubility. It was concluded that the indole was important for in vitro activity. With the aim of further improvements, more thorough modifications were also carried out. As a result, a new chemotype (the azetidinespirochromone family) was identified, which proved to be 1 order of magnitude less lipophilic retaining the same high level of in vitro potency as the lead series itself, however, with improved metabolic stability and kinetic solubility. Compound 53 showed the most balanced physicochemical and pharmacological profile with significant in vivo efficacy in the scopolamine-induced amnesia test. Based on these promising results, cognitive enhancement through the positive modulation of α7 nAChRs appears to be a viable approach. Compound 53 was selected to be a preclinical development candidate (as RGH-560).

100 Deals associated with RGH-560

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