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1. (WO2017220799) COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS

Pub. No.:    WO/2017/220799    International Application No.:    PCT/EP2017/065585
Publication Date: Fri Dec 29 00:59:59 CET 2017 International Filing Date: Sat Jun 24 01:59:59 CEST 2017
IPC: C07D 401/12
C07D 405/12
C07D 211/38
A61K 31/44
A61K 31/4427
A61P 25/00
Applicants: NEUROLIXIS
UNIVERSITE JAGELLONNE
Inventors: SNIECIKOWSKA, Joanna
BUCKI, Adam
NEWMAN-TANCREDI, Adrian
VARNEY, Mark Andrew
Title: COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS
Abstract:
The invention concerns compounds that possess a high affinity at 5-HT 1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.