| abstract |
The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C 1 -C 4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C 1 -C 4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C 1 -C 4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C 1 -C 4 alkyl or C 1 -C 4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH═ and/or —CH 2 — groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C 1 -C 4 alkylene, C 2 -C 4 alkenylene, aminocarbonyl, —NH—, —N(alkyl)-, —CH 2 O—, —CH 2 S—, —CH(OH)—, —OCH 2 — group, wherein the meaning of alkyl is a C 1 -C 4 alkyl group—, when the dotted bonds ( ) represent simple C—C bonds then U is hydroxy group or hydrogen atom or when W is C 1 -C 4 alkylene or C 2 -C 4 alkenylene group, then one of the dotted bonds ( ) can represent a further double C—C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions. |