Substituted phenothiazine derivatives

Details Substituted phenothiazine derivatives Substituted phenothiazine derivatives

C - Chemistry, Metallurgy

07

D

260/243.5

C07D 417/00 (2006.01) C07C 43/225 (2006.01) C07C 43/23 (2006.01) C07C 217/62 (2006.01) C07D 279/26 (2006.01) C07D 279/28 (2006.01)

Patent

CA 1209139

ABSTRACT The substituted (10H-phenothiazin-10-yl)propyl-1- piperazines of the formula Image 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 antipsycho- tics, 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 sub- stituted phenol.

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