2-OXO-1-OXA-8-AZASPIRO/4,5/DECANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING THE SAME

摘要

NOVEL 2-OXO-1-OXA-3-AZASPIRO¢4,5!DECANE DERIVATIVE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME The invention relates to novel 2-oxo-1-oxa-8-aza-spiro¢4,5!decane derivatives of the formula (I), (I) wherein X means oxygen or an ?NR group, wherein R stands for hydrogen; a C1-12alkyl; C3-6cycloalkyl; carbocyclic C6-10aryl or carbocyclic C6-10aryl- -C1-4alkyl group, the two latter ones being optionally substituted on their aromatic part by one or more, same or different halogen(s), one or more C1-4alkyl, C1-4alkoxy or trihalomethyl group(s); or a tosyl group; R1 and R2 together represent a methylene group or, when X stands for an ?NR group wherein R is as defined above, one of R1 and R2 may represent a hydroxyl goup and the other one is a methyl group; and R3 means hydrogen, benzyl, (C1-4alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-l-yl-carbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin- -l-ylcarbonyl, 4-(2-hydroxyethyl)piperazin-1-ylcar-bonyl, 2-chloro-3-nicotinoylcarbamoyl or C1-6alkyl-carbamoyl group, as well as their acid addition and quaternary ammonium salts. The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of formula (I) possess anticonvulsive, antiallergic and lipid level lowering effects. Thus, they are useful for the treatment of epileptic and allergic diseases and increased lipid levels.