N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodiben

Details N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodiben N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodiben

1986-01-24

1987-07-07

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544375, 549 12, A61K 31495, C07D40904

Patent

active

046787887

ABSTRACT:
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.

REFERENCES:
patent: 4144337 (1979-03-01), Bastian
patent: 4243805 (1981-01-01), Protiva et al.

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