GB874217A — Normorphine derivatives

USPTO Abstract

The invention comprises quaternary salts having a cation of the general formula <FORM:0874217/IV (b)/1> (wherein R and R1 are the same or different and each represent a hydrogen atom or a C1-C3 acyl group, and R1 and R2 are the same or different and each represent an allyl, propyl or propargyl group) in association with a non-toxic anion, the preparation of those containing a halide anion by reacting normorphine or N-propyl-, N-allyl- or N-propargyl-normorphine, or an acyl derivative thereof, with an allyl, propyl or propargyl halide, and pharmaceutical compositions containing the salts (see Group VI).ALSO:Pharmaceutical compositions having an antagonistic action against morphine comprise, in association with a pharmaceutical carrier, a quarternary salt of normorphine containing a cation of the general formula <FORM:0874217/VI/1> (wherein R and R1 are the same or different and each represent a hydrogen atom or a C1-3 acyl group, and R1 and R2 are the same or different and each represent an allyl, propyl or propargyl group) in association with a non-toxic anion (e.g. a halide ion). The compositions may be in orally and parenterally administrable forms and may also be in suppository form. Examples are given of ampoules and tablets containing N-diallylnormorphinium bromide.