Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors
摘要:
A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists. (C) 2010 Elsevier Ltd. All rights reserved.
IMIDAZO[4,5-b]PYRIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
申请人:LES LABORATOIRES SERVIER
公开号:US20180273528A1
公开(公告)日:2018-09-27
Compounds of formula (I):
wherein R
1
, R
2
, R
3
, R
4
, and R
5
are as defined in the description.
Medicinal products containing the same which are useful in treating cancer, neurodegenerative disorders and metabolic disorders.
[EN] COMBINATIONS OF PERIPHERAL 5-HT2A RECEPTOR ANTAGONISTS AND CENTRAL 5-HT2A RECEPTOR AGONISTS<br/>[FR] COMBINAISONS D'ANTAGONISTES DU RÉCEPTEUR 5-HT2A PÉRIPHÉRIQUE ET D'AGONISTES DU RÉCEPTEUR 5-HT2A CENTRAL
申请人:[en]GILGAMESH PHARMACEUTICALS, INC.
公开号:WO2023028086A1
公开(公告)日:2023-03-02
Methods of treating mood disorders with compounds disclosed herein. Also provided are pharmaceutical compositions that include those compounds.