SUBSTITUTED PHENOTHIAZINE DERIVATIVES

The substituted (10H-phenothiazin-10-yl)propyl-1-piperazines of the formula I wherein R1 is hydrogen, halogen, alkyl, alkylthio, alkoxy, trihalomethyl or the group -SO2NR2R3, X is oxygen or sulfur, m is an integer from 2 to 6, n and s are, independently, the integer zero or 1, A is alkylene and, whe...

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Hauptverfasser: DAVIDSON, ARNOLD B, KIERSTEAD, RICHARD W, ZIERING, ALBERT, GUTHRIE, ROBERT W
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:The substituted (10H-phenothiazin-10-yl)propyl-1-piperazines of the formula I wherein R1 is hydrogen, halogen, alkyl, alkylthio, alkoxy, trihalomethyl or the group -SO2NR2R3, X is oxygen or sulfur, m is an integer from 2 to 6, n and s are, independently, the integer zero or 1, A is alkylene and, when X is oxygen, also 2-hydroxytri-methylene, and R2 and R3, independently, are hydrogen or alkyl or taken together with the nitrogen atom a 5-, 6- or 7-membered unsubstituted or substituted heterocyclic ring, the enantiomers of those compounds wherein A is 2-hydroxy-trimethylene, and the pharmaceutically acceptable acid addition salts thereof exhibit neuroleptic activity of long duration, and thus, can be used as long acting antipsychotics, particularly in the treatment of schizophrenia. They can be prepared by reacting a 1-¢3-(10H-phenothiazin-10-yl)-propyl!-4-haloalkylpiperazine with a corresponding substituted phenol.