4-aminoethoxy indoles as dopamin d2 agonists and as 5ht1a...

Details 4-aminoethoxy indoles as dopamin d2 agonists and as 5ht1a... 4-aminoethoxy indoles as dopamin d2 agonists and as 5ht1a...

C - Chemistry, Metallurgy

07

D

C07D 209/08 (2006.01) A61K 31/40 (2006.01) C07D 209/12 (2006.01) C07D 209/30 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2264080

Compounds of the formula (I) in which R1 is hydrogen, alkyl, cycloalkylalkyl, arylalkyl, (haloaryl)alkyl, (alkoxy-aryl)alkyl, thienylmethyl, furanylmethyl, pyridinylmethyl, alkylphenyl, 4-fluoro-butyrophenome or 6-fluoro-1,2- benzisoxasol-yl-propyl; X is hydrogen, halogen, cyano, alkyl, acetyl, trifluoroacetyl, trifluoromethyl or formyl; Y is hydrogen, halogen, alkoxy or alkyl; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs and they also have affinity for the 5-HT1A receptors which characterizes them as useful in the treatment of diseases attending disturbances in the serotinergic systems, such as anxiety, stress, depression, sexual dysfunctions and sleep disturbances.

Cette invention se rapporte à des composés représentés par la formule (I) dans laquelle R¿1? est hydrogène, alkyle, cycloalkylalkyle, arylalkyle, (haloaryl)alkyle, (alcoxyaryl)alkyle, thiénylméthyle, furanylméthyle, pyridinylméthyle, alkylphényle, 4-fluoro-butyrophénone ou 6-fluoro-1,2-benzisoxazol-yl-propyle; X est hydrogène, halogène, cyano, alkyle, acétyle, trifluoroacétyle, trifluorométhyle ou formyle; Y est hydrogène, halogène, alcoxy ou alkyle. Ces composés ou leurs sels pharmaceutiquement acceptables sont des inhibiteurs de synthèse et de libération de la dopamine qui s'avèrent utiles dans le traitement de la schizophrénie, de la maladie de Parkinson, de la maladie de Gilles de La Tourette, de la toxicomanie alcoolique, de la cocaïnomanie et de la toxicomanie associée à des drogues analogues. Ces composés possèdent également une affinité pour les récepteurs 5-HT¿1A? qui en font des agents utiles dans le traitement des maladies associées à des troubles des systèmes sérotoninergiques, tels que l'anxiété, le stress, la dépression, les dysfonctionnements sexuels et les troubles du sommeil.

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