| abstract |
The invention relates to amide derivatives of carboxylic acids that are highly effective and selective NMDA receptor antagonists, most of which are selective NR2B antagonists of the NMDA receptor. They have the formula wherein - (CHR 1) m - and - (CHR 2) n - are -CH 2 -CH 2 - groups; the adjacent V and U groups together with one or more identical or different additional heteroatoms and -CH = and / or -CH2- groups form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholino, pyrrole, pyrrolidine, oxo - or a thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxoimidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, oxo- or thioxo- oxazolidine or 3-oxo- 1,4- oxazine ring ; X is -CO-group; W is -CO-, -CH2- or -CH (-alkyl) -group, the alkyl moiety being a C1-C4-alkyl group; Y is an oxygen atom, and also a C 1 -C 4 alkylene group, a C 2 -C 4 alkylene group, a cycloalkylene group, an aminocarbonyl group, -NH-, -N (alkyl) -, -CH 2 O-, CH (OH) OCH 2 - group, the alkyl moiety being a C 1 -C 4 -alkyl group; Z is a hydrogen or halogen atom, a nitro group, an amino group, a C1-C4 alkyl group, a C1-C4 alkoxy group, a cyano group, a trifluoromethyl group, a hydroxyl group or a carboxyl group. The invention also relates to their optical antipodes or racemates and / or pharmaceutically acceptable salts thereof formed by reaction with acids or bases and to pharmaceutical compositions containing amide compounds |