Piperazinoisothiazolones with psychotropic activity

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/14 (2006.01) C07D 275/03 (2006.01) C07D 275/04 (2006.01) C07D 275/06 (2006.01) C07D 417/12 (2006.01) C07D 513/04 (2006.01) C07D 513/14 (2006.01) C07D 513/18 (2006.01)

Patent

CA 1272197

PIPERAZINOISOTHIAZOLONES WITH PSYCHOTROPIC ACTIVITY Abstract of the Disclosure There are disclosed compounds of the formula Image wherein R1 and R2 are each, independently, hydrogen, lower alkyl, aryl of 6 to 10 carbon atoms or halo, or R1 and R2 taken together represent -CH2-, -CH2CH2-, Image Image Image Image or where the dotted lines represent optional double bonds; R3, R4, R5 and R6 are each, independently, hydrogen, lower alkyl, aryl of 6 to 10 carbon atoms or halo; R7 is 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl or phenyl or any of the foregoing R7 moieties substituted by lower alkyl, trifluorormethyl, cyano, nitro or halo, with the proviso that when R1 and R2 taken together represent Image , then R7 is other than 2-pyridinyl, 2-pyrimidinyl, substituted pyrimidin-2-yl, phenyl or substituted phenyl; Z is -(CH2)n-, vinylene, -O-, or Image X is lower alkylene, vinylene, O or NH; m is 2- 5; n is 0- 4; o is 1- 3; p is 1- 4; and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/- anxiolytic agents having a low liability for extrapyramidal side effects.

520188

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