Bicyclolactam compounds, use of the same and intermediate in...

Details Bicyclolactam compounds, use of the same and intermediate in... Bicyclolactam compounds, use of the same and intermediate in...

C - Chemistry, Metallurgy

07

D

C07D 221/04 (2006.01) A61K 31/40 (2006.01) A61K 31/435 (2006.01) A61K 31/55 (2006.01) C07D 205/12 (2006.01) C07D 209/52 (2006.01) C07D 215/20 (2006.01) C07D 215/227 (2006.01) C07D 217/24 (2006.01) C07D 221/16 (2006.01) C07D 223/14 (2006.01)

Patent

CA 2197178

Bicyclolactam compounds represented by general formula (1) (see formula I) wherein: R is oxo or -OR1, where R1 is a hydrogen atom or an aliphatic acyl group having 2 to 6 carbon atoms, benzoyl, toluyl, methoxybenzoyl, dimethoxybenzoyl, or naphthylcarbonyl; A is a group of (2) or (3) (see formula II and III) wherein R2 is a benzoyl group or a benzoyl group substituted by a halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group, hydroxyl group or amino group; Q is a hydrogen atom or lower alkyl group; 1 is 1 or 2; m is 0 or 1 and n is 0, 1 or 2 (provided the case where both of m and n represent 0 simultaneously is excluded); are useful as the active ingredient of medicines having an excellent anxiolytic effect with little side effects such as hypnotic effect, a muscle relaxing effect and a sedative effect.

Les composés de bicyclolactame représentés par la formule générale (1) sont utiles comme ingrédient actif de médicaments ayant un excellent effet anxiolytique et une sécurité élevée avec peu d'effets secondaires tels qu'un effet hypnotique, de relaxation musculaire, sédatif, etc. Dans cette formule, R représente oxo ou -OR<1> (R<1> représente hydrogène ou acyle); A représente l'un des groupes suivants (2) et (3); Q représente hydrogène ou un alkyle inférieur; l vaut 1 ou 2, m vaut 0 ou 1, et n vaut 0, 1 ou 2 mais m et n ne valent pas 0 en même temps; R<2> est du benzoyle éventuellement substitué.

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