1-amino-alkylcyclohexane nmda receptor antagonists

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 211/17 (2006.01) A61K 31/137 (2006.01) A61K 31/40 (2006.01) C07C 211/35 (2006.01) C07D 295/135 (2006.01) C07C 211/00 (2006.01)

Patent

CA 2292558

Certain 1-amino-alkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti- Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method of treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-amino-alkylcyclohexane compounds involved.

Certains 1-aminoalkylcyclohexanes sont des antagonistes non compétitifs du récepteur de N-méthyl-D-aspartate (NMDA) présentant une activité systémique, une cinétique rapide de blocage et de déblocage et une forte dépendance à la tension électrique, ce qui les rend utiles pour soulager des états provenant de perturbations de la transmission glutamatergique et leur confère d'importantes possibilités de mise en application pour traiter des maladies du système nerveux central comportant ces perturbations, ainsi que des états n'impliquant pas NMDA, étant donné leurs activités et leurs potentialités immunomodulatrices, antipaludéennes, anti-virus de Borna et anti-hépatite C. Compositions pharmaceutiques à base de ces 1-aminoalkylcyclohexanes, procédé servant à traiter des états soulagés par l'utilisation d'un antagoniste du récepteur de NMDA, et, également, les états ci-dessus mentionnés indépendants de NMDA, ainsi que procédé servant à préparer ces composés actifs de 1-aminoalkylcyclohexane.

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