C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/278.1, 260/2
C07D 211/40 (2006.01) C07D 211/56 (2006.01) C07D 211/58 (2006.01) C07D 211/64 (2006.01) C07D 491/04 (2006.01)
Patent
CA 1053230
ABSTRACT OF THE DISCLOSURE The present invention is concerned with novel 4-aryl-3/4-amino/hydroxy-piperidine derivatives of the general formula I: Image ....I wherein R1 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 -(CH2)n-COOH; -(CH2)n-OH; Image or Image ; wherein X is hydrogen or halogen and n is 1, 2, 3 or 4; one of R2 and R3 represents a cyano, or a free amino group or a derivative thereof and the other represents a free or protected hydroxyl group; or R2 represents an azido group when R3 represents a free or protected hydroxyl group, or R2 and R3 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 CF3, 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 antidepress- ant activity. Illustrative of compounds of formula I is 1-methyl-4-phenyl-4-acetoxy-3-(1-piperidinyl)piperidine The present invention also provides processes for the production of, and pharmaceutical compositions containing the novel compounds of formula I.
242119
Do Nascimento Jose M. (jr.)
Kubela Rudolf
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