S-substituted n-1-¬(hetero)...

C - Chemistry – Metallurgy – 07 – C

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C07C 335/12 (2006.01) A61K 31/155 (2006.01) A61K 31/381 (2006.01) A61P 25/28 (2006.01) C07D 307/10 (2006.01) C07D 307/38 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2508783

The invention relates to s-substituted N-1-[(hetero)aryl]alkyl-N.prime.-1- [(hetero)aryl] alkylysothiocarbamides and the physiologically active salts and bases thereof, embodied in the form of racemic mixtures (or stereoisomer mixture) or individual optical isomers. The specific physiological activity of said compounds makes it possible to use them in the form of molecular tools . Said invention also relates to Pharmaceutical compositions, containing said compounds and to a method for preventing and curing various diseases including neurodegenerative diseases as, for example Alzheimer's disease (AD). The pharmacological effect of said compounds is based on the combined cognitive- stimulating and neuroprotective action thereof, which is produced by acting on chemo-controlled calcium channels of neurone membranes, in particular the neurones regulated by glutamate receptors of the central neural system (CNS).

La présente invention concerne des N-1-[(hétéro)aryl]alkyl-N.prime.-1-[(hétéro)aryl]alkylisothiocarbamides S-substitués ainsi que leurs sels et bases physiologiquement actifs qui se présentent sous la forme de mélanges racémiques (ou d'un mélange de stéréoisomères) ou sous la forme d'isomères optiques individuels. Cette invention porte également sur l'action physiologique spécifique de ces combinaisons, qui leur permet de servir "d'instruments moléculaires", sur des compositions pharmaceutiques contenant les combinaisons susmentionnées, ainsi que sur une méthode de traitement et de prévention du développement de divers troubles, parmi lesquels figurent les troubles neurodégénératifs tels que la maladie d'Alzheimer. L'effet pharmacologique de ces combinaisons repose sur leur fonction de stimulation cognitive complexe et de neuroprotection obtenue par leur action sur les canaux calciques chimiodirecteurs des membranes des cellules nerveuses, régulées en particulier par les récepteurs glutamiques du système nerveux central (SNC).

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