摘要 |
<p>The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independentlyare hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4alkylsulfonamido optionally substituted with a halogen atom or halogen atoms,C1-C4 alkanoylamido optionally substituted with a halogenatom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionallysubstituted with halogen atom or C1-C4 alkyl or C1-C4alkoxycarbonyl group, or the neighboring X and Y groups optionally form togetherwith one or more identical or different additional hetero atom and -CH= and/or-CH2- groups an optionally substituted 4-7 membered homo- or heterocyclicring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine,pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazoleor imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine,or 3-oxo-l,4-oxazine ring, V and Z independently are hydrogen or halogen atom,cyano, C1-C4 alkyl, C1-C4 alkoxy,trifluoromethyl , hydroxy or optionally esterized carboxyl group, W is oxygenatom, as well as C1-C4 alkylene, C2-C4alkenylene, aminocarbonyl, -NH-, -N(alkyl)-, -CH2O-, -CH2S-,-CH(OH)-, -OCH2- group, wherein the meaning of alkyl is a C1-C4alkyl group -, when the dotted bonds ( --- ) represent simple C-C bondsthen U is hydroxy group or hydrogen atom or when W is C1-C4alkylene or C2-C4 alkenylene group, then one of the dottedbonds ( --- ) can represent a further double C-C bond and in this case U meansan electron pair, which participate in the double bond and optical antipodes,racemates and the salts thereof are highly effective and selective antagonistsof NMDA receptor, and moreover most of the compounds are selective antagonistof NR2B subtype of NMDA receptor. Furthermore objects of the present inventionare the pharmaceutical compositions containing new benzoyl urea derivativesof formula (I) or optical antipodes or racemates or the salts thereof as activeingredients and processes for producing these c ompounds and pharmaceuticalcompositions.</p> |