Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Josef Pomykacek

Antonin Dlabac

Miroslav Protiva

Jiri Jilek

Miroslav Rajsner

Karel Sindelar

Jirina Metysova

Martin Valchar

Irena Cervena

Vaclav Bartl

Leon Langsadl

Frantisek Miksik

N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepins are disclosed of the general formula I, ##STR1## in which R represents an aminocarbonyl, amino-oximinomethyl, 1,3-dioxolan-2-yl or 1,3-dioxan-2-yl, group and their addition salts with convenient organic and inorganic acids. These compounds are highly potent antidopaminergic, non-cataleptic neuroleptics of use in the treatment of schizophrenia. According to recent pharmacological assay results, the subject compounds are expected to be substantially free of the usual undesired extrapyramidal side effects. They can be obtained by common preparative methods from the respective starting compounds of formula III, IV or V, or also by appropriate interconversion reactions of other compounds of formula I. If required, the resulting bases are neutralized with suitable acids, preferably methanesulfonic, maleic or hydrochloric acid, to yield the corresponding addition salts that can be used in formulating proper dosage forms for pharmacological evaluation and therapeutical application.

N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo (B,F)

Techniques for the preparation of 3-fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(b,f) thiepins and their addition salts with organic and inorganic acids are disclosed. The described compositions evidence psychotropic activity and low toxicity and are characterized as neuroliptics with a high degree of cataleptic, anti-apomorphine and central depressant action.

3 Fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo-(bf) thiepins

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Prague, Czechia

Josef Pomykacek