Compounds used to treat alcoholism

Details Compounds used to treat alcoholism Compounds used to treat alcoholism

C - Chemistry, Metallurgy

07

C

C07C 211/36 (2006.01) A61K 31/132 (2006.01) A61P 25/32 (2006.01) C07C 233/08 (2006.01)

Patent

CA 2451983

The invention relates to a novel compound, N,N'-bis (3-aminopropyl) cyclohexane-1,4-diamine, having formula (I) which is prepared by hydrogenation using a Raney nickel catalyst of N,N'-bis (2-cyanoethyl)-cyclohexane-1,4- diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration of the tetramethanesulphonate monohydrate of (I) to genetically alcoholic mice (from the UChB strain from the University of Chili) causes a significant reduction in the consumption of alcohol. The activity of said compound continues for a certain amount of time following the treatment period. Moreover, there is practically zero disulfiram- type adverse effect, which is advantageous given the disagreeable aspect of using some antialcoholic agents, such as calcium cyanamide and said disulfiram. In this way, the inventive compounds can be used to prepare medicaments for the therapeutic and/or prophylactic treatment of alcoholism in mammals, including humans.

L'invention concerne un nouveau composé, la N,N'-bis(3-aminopropyl)cyclohexane-1,4-diamine représentée par la formule (I), qui est préparée par hydrogénation au moyen d'un catalyseur nickel Raney de N,N-bis(2-cyanoéthyl)-cyclohexane-1,4-diamine, lequel est lui-même préparé par réaction de 1,4-cyclohexanodiamine et d'acrylonitrile. L'administration orale du monohydrate du tétraméthanosulfonate de (I) à des souris génétiquement alcooliques (provenant de la souche UChB de l'Université du Chili) entraîne une réduction significative de la consommation d'alcool. L'activité de ce composé se prolonge pendant un certain temps après la période de traitement. Par ailleurs, l'effet inverse du type disulfirame est pratiquement nul, ce qui constitue un avantage par rapport à l'aspect désagréable de l'utilisation de certains agents antialcooliques, tels que la cyanamide calcique et ledit disulfirame. Par conséquent, les composés selon l'invention sont utiles pour la préparation de médicaments destinés au traitement thérapeutique et/ou prophylactique de l'alcoolisme chez les mammifères, y compris les êtres humains.

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