Spofa, Spojene Podniky Pro Zdravotnickou Vyrobu

Vyzkumny Ustav Pro Farmacii a Biochemii

Martin Valchar

Evzen Kasafirek

Miroslav Protiva

Ivan Krejci

Antonin Dlabac

Milan Pesak

Irena Cervena

Jiri Jilek

Josef Pomykacek

Arnost Pospisil

Zdenek Hlinak

Karel Dobrovsky

Antonin Struc

The present application is directed to a method of treating central nervous system disorders originating as a consequence of head injury or brain ischemia. The method comprises administering an effective amount of cyclo-(L-alanyl-1-amino-1-cyclopentane carbonyl) to treat a central nervous system disorder in a mammalian organism in need of such treatment. The administration may be conducted either orally or parenterally.

Neuroprotective composition for preventing or treating of central

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)

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Prague, Czechia

Martin Valchar