2-oxo-1-oxa-8-azaspiro/4,5/decane derivatives,...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/113 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 498/10 (2006.01)

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CA 2023027

NOVEL 2-OXO-1-OXA-3-AZASPIRO[4,5]DECANE DERIVATIVE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME Abstract The invention relates to novel 2-oxo-1-oxa-8-aza- spiro[4,5]decane derivatives of the formula (I), Image (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, phenoxy- carbonyl, 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 composi- tions containing these compounds and a process for their pre- paration. 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.

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