Antidepressant 4-aryl-piperidines and salts - some having local anaesthetic and antiarrhythmic activity

摘要

4-Aryl-amino-hydroxypiperidines of formula (I) are new together with their acid-addn. salts (where R' is H,alkyl, alkenyl, alkynyl, aralkyl, acyl, 2-6C alkylamino opt. substd. by one or two alkyls or opt. substd. by alkylene to complete a satd. N-heterocycle; a gp. where R7 and R8 are H, phenyl opt. substd. by halo, or alkyl; or R7 + R8 and the attached N-atom form a 6 or 7-membered heterocyclic ring opt. contg. an O-atom; n is 1, 2, 3 or 4; a gp. -(CH2)n. CO2H; a gp. where X is H or halo; one of R2 and R3 is CN, free NH2 or a radical derived from it; the other is a free or protected OH; or R2 is where R3 is free or protected OH; or R2 + R3 and the attached C atoms form an oxazepin ring; Ar is aryl opt. substd. by one or more alkyl, alkoxy, halo or CF3). One subgp. has antidepressant activity, another gp. has local anaesthetic and antiarrhythmic activity. Other activities in the gp. include antihistamine, anticholinergic, spasmolytic, and diuretic activity.