Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Spofa United Pharmaceutical Works

Irena Cervena

Miroslav Protiva

Antonin Dlabac

Jirina Metysova

Karel Sindelar

Martin Valchar

Jiri Jilek

Josef Pomykacek

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)

Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula ##STR1## wherein R.sup.2, R.sup.3, R.sup.7 and R.sup.8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R.sup.2, R.sup.3, R.sup.7 and R.sup.8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.

Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine

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Prague, Czechia

Irena Cervena