Ciba-geigy Corporation

Hans Blattner

Angelo Storni

Azatetracyclic compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow. The novel compounds can be used as tranquillizing, antipsychotic and excitation-inhibiting compounds for the treatment of states of agitation. Specific embodiments are 3-methyl-2,3,4,5-tetrahydro-1H-dibenzo[2,3:6,7]thiepino[4,5-d]azepine and 3-methyl-2,3,4,5-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-d]azepine.

Treating states of agitation with azatetracyclic compounds

Azatetracyclic carbonitriles of the formula ##STR1## in which R represents hydrogen, lower alkyl, cycloalkyl-lower alkyl having up to 10 carbon atoms, lower alkenyl, lower alkynyl or free, etherified or esterified hydroxy-lower alkyl, and acid addition salts thereof, processes for their manufacture, pharmaceutical compositions that contain such compounds and their use. They are distinguished especially by their central nervous system-depressant, agitation-inhibitory (amphetamine-antagonistic) action. They can therefore be used as tranquillizing, anti-psychotic, agitation-inhibitory compounds for the treatment of agitated states having various causes.

Azatetracyclic carbonitriles

Azatetracyclic carbonitriles of the formula I ##STR1## in which R.sub.1 is hydrogen, lower alkyl, cycloalkyl-lower alkyl, lower alkenyl or free, etherified or esterified hydroxy-lower alkyl, and X is epoxy, epithio, methylene of a divalent radical of the partial formula ##STR2## in which R.sub.2 is hydrogen or lower alkyl, and salts of such compounds, their preparation, pharmaceutical preparations which contain these compounds and the use thereof.

The substituted 5H-dibenz[b,f]azepine of the formula ##STR1## a process for its manufacture, pharmaceutical compositions which contain the novel compound, and a method of treating epilepsy which comprises the use thereof.

Substituted 5H-dibenz[b,f]azepine

The present invention provides imidazole derivatives of the formula I ##STR1## wherein Het represents 1H-imidazol-1-yl which is unsubstituted or is substituted by lower alkyl,

1-Naphthothienylalkyl-1H-imidazoles

5-Oxygenated azatetracyclic compounds of the formula ##STR1## wherein X represents oxygen or sulphur, R represents a hydroxy group optionally esterified by an alkanecarboxylic acid, and R.sub.1 stands for a lower alkyl, lower alkenyl or allyl, or salts thereof, such compounds having a central-depressant and agitation-inhibiting action connected with cataleptic effects to a very low extent only these properties rendering the new compounds suitable as tranquillizing, antipsychotic and agitation-inhibiting substances.

Oxygenated azatetracyclic compounds

2,3-Dihydro-1H-dibenz[e,g]isoindoles substituted in the 2-position by a lower alkyl or a lower alkenyl, or a lower haloalkyl, or a free or an esterified or etherified lower hydroxyalkyl, or a lower oxoalkyl, or a free or an esterified lower carboxyalkyl group, and therapeutically usable salts thereof, such compounds having an antagonistic action against reserpine as well as against tetrabenazine such pharmacological properties characterizing these new compounds as antidepressants.

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Riehen, Switzerland

Hans Blattner