Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...
Patent
1977-09-12
1979-03-27
Jiles, Henry R.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Parasitic organism or component thereof or substance...
546188, 546205, 546208, C07D21152, A61K 31455
Patent
active
041466292
ABSTRACT:
The present invention is concerned with novel 4-aryl-3/4-amino/hydroxy-piperidine derivatives of the general formula I: ##STR1## wherein R.sub.1 represents hydrogen; lower alkyl; lower aralkyl; lower acyl; aminoalkyl, wherein the alkyl moiety contains 2 to 6 carbon atoms and the amino moiety may be mono- or dialkyl substituted --(CH.sub.2).sub.n --COOH; --(CH.sub.2).sub.n --OH; ##STR2## wherein X is hydrogen or halogen and n is 1, 2, 3 or 4; one of R.sub.2 and R.sub.3 represents a cyano, or a free amino group or a derivative thereof and the other represents a free or protected hydroxyl group; or R.sub.2 represents an azido group when R.sub.3 represents a free or protected hydroxyl group, or R .sub.2 and R.sub.3 together with their associated ring carbons represent an oxazepine ring, and Ar represents an aryl group which may be substituted by lower alkyl, lower alkoxy, halogen or CF.sub.3 , as well as addition salts thereof with organic or inorganic acids.
Compounds of formula I generally have useful biological properties and in particular, some such compounds had been found to exhibit inter alia, significant antidepressant activity. Illustrative of compounds of formula I is 1-methyl-4-phenyl-4-acetoxy-3-(4-piperidinyl)piperidine. The present invention also provides processes for the production of, and pharmaceutical compositions containing the novel compounds of formula I.
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patent: 3125574 (1964-03-01), Janssen
patent: 3158616 (1964-11-01), Adickes et al.
patent: 3371094 (1968-02-01), Zenitz et al.
patent: 3845064 (1974-10-01), Curren
Donascimento Jose M.
Kubela Rudolph
Delmar Chemicals Limited
Jiles Henry R.
Ramsuer R. W.
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