SULPHONAMIDE DERIVATIVES OF ALICYCLIC AMINES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES
申请人:Kolaczkowski Marcin
公开号:US20140135310A1
公开(公告)日:2014-05-15
Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3;
and enancjomers, pharmaceutically acceptable salts and solvates thereof.
The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
[EN] SULPHONAMIDE DERIVATIVES OF ALICYCLIC AMINES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES<br/>[FR] DÉRIVÉS SULPHONAMIDE D'AMINES ALICYCLIQUES UTILISÉS DANS LE TRAITEMENT DE MALADIES DU SYSTÈME NERVEUX CENTRAL
申请人:ADAMED SP ZOO
公开号:WO2013001505A2
公开(公告)日:2013-01-03
Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with -or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; r represents 0 or 1; x, z independently represent 1 or 2; n represents 3 and p represents 0, or n represents 2 and p represents 1;and enantiomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders (Formula I).
Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties
properties of 5-HT7 receptorantagonists have been widely demonstrated in a large set of animal models. Considering the potential therapeutic advantages in targeting both α2-adrenoceptors and 5-HT7 receptors, we designed a small series of arylsulfonamide derivatives of (dihydrobenzofuranoxy)ethyl piperidines as dually active ligands. Following green chemistry principles, the designed compounds were synthesized