Derivatives of perhydro-aza-heterocycles

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Fungus – except allergen – or component thereof or substance...

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26032633, 26032647, 2603265C, 2603265M, C07D20712, A61K 3140

Patent

active

043201377

ABSTRACT:
The present invention provides new derivatives of perhydro-aza-heterocycles of the formula ##STR1## in which X is the oxo radical or hydrogen and the radical OR.sub.1, in which R.sub.1 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, a substituted or unsubstituted araliphatic hydrocarbon radical or a substituted or unsubstituted aromatic hydrocarbon radical or an acyl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, Y is oxygen or sulphur, n.sub.1 and n.sub.2 each are values of 1 to 3, n.sub.1 +n.sub.2 being at most four, and Ar is a substituted or unsubstituted aromatic hydrocarbon radical, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions. Specific embodiments are trans- and cis-3-hydroxy-4-(3,4-dimethyl-phenoxy)-piperidine, trans- und cis-3-hydroxy-4-(2,3-dimethyl-phenoxy)-piperidine, their 1-methyl derivatives and the pharmaceutically acceptable salts of these substances.

REFERENCES:
patent: 3381013 (1968-04-01), Minor
patent: 3446897 (1969-05-01), Koppanyi
patent: 3577432 (1971-05-01), Helsley
patent: 3627766 (1971-12-01), Eichenberger et al.
patent: 3823151 (1974-07-01), Eichenberger et al.
patent: 3961959 (1976-06-01), Fujiwhara et al.
patent: 4160837 (1979-07-01), Paioni
patent: 4246269 (1981-01-01), Paioni
patent: 4251541 (1981-02-01), Walsh
Chemical Abstracts 88:P152446e, Paioni, (1978).

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