Heterocyclic compounds which have pharmacodynamic activity and/or which are intermediates in the preparation of products having pharmacodynamic activity

摘要

Novel compounds which have pharmacodynamic activity or are intermediates for products having such activity are obtained by reacting a compound of the general formula FORM:1059175/C2/1 (wherein X is N and ring A is aromatic, or X is C and ring A is either saturated or ethylenically or aromatically unsaturated, and wherein R1 is an unsubstituted or substituted alkyl, aralkyl or aryl radical, and ring A may be further substituted) or a functional derivative thereof (including lactols) with a diamide of the general formula R-NH-Z-NH2 (wherein R is H or alkyl and Z is an optionally substituted alkylene radical containing 2-4 carbon atoms in a straight chain or an optionally substituted o-arylene radical). The products may be converted into acid addition salts or, when they contain a secondary amino group, may be acylated. Preferred compounds have the general formula FORM:1059175/C2/2 wherein ring A is a substituted or unsubstituted benzene ring or a cyclohexane or cyclohexene ring. Pharmaceutical compositions, preferably in oral or parenteral unit dosage form, comprise the compounds of the invention in association with a pharmaceutically acceptable carrier. They have central nervous system depressant, appetite depressant, anticonvulsant, tranquillizing, antitremorine, mydriatic and/or analgesic activity, or, in some cases, antidepressant activity.