GB1009440A - Tetrahydropyridine derivatives and process for their production - Google Patents

Abstract

The invention comprises compounds of the general formula <FORM:1009440/C2/1> wherein R1, R2 and R3 each independently represents an alkyl radical containing not more than 5 carbon atoms, and R4 represents an alkyl radical which may be substituted by one or more hydroxyl, alkoxy or dialkylamino groups, an alkenyl radical, a cycloalkyl radical, or an aralkyl radical which may be substituted by one or more halogen atoms or one or more hydroxyl, alkyl, alkoxy or alkylenedioxy groups, R4 containing a total of not more than 10 carbon atoms) and their preparation by condensing a compound of the general formula <FORM:1009440/C2/2> with cyanoacetyl chloride or bromide. The compounds are sedatives, analgesics, central nervous system depressants and antiphlogistic agents (see Division A5).ALSO:Pharmaceutical preparations comprise a compound of the general formula <FORM:1009440/A5-A6/1> (wherein R1, R2 and R3 each independently represents an alkyl radical containing not more than 5 carbon atoms, and R4 represents an alkyl radical which may be substituted by one or more hydroxyl, alkoxy or dialkylamino groups, an alkenyl radical, a cycloalkyl radical, or an aralkyl radical which may be substituted by one or more halogen atoms or one or more hydroxyl, alkyl, alkoxy or alkylenedioxy groups, R4 containing a total of not more than 10 carbon atoms) and a carrier, and may contain a solubility promoter such as sodium salicylate or the sodium salt of 1, 2-diphenyl-4-n-butyl-3, 5-dioxopyrazolidine or 1-(p-hydroxyphenyl)-2-phenyl-4-n-butyl-3, 5-dioxipyrazolidine. The preparations may be administered orally, rectally or parenterally and may be in the form of tablets, drag<\>ees, capsules, suppositories, solutions or emulsions. The active ingredients (see Division C2) are sedatives, analgesics, central nervous system depressants and antiphlogistic agents.