Pharmaceutical amides, and preparation, formulations and use of thereof

Abstract

Abstract Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C 1-4 alkyl, amino, C 1-4 alkylamino, di-C 1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C 1-4 alkoxycarbonyl, amido, C 1-4 alkylamido C 1-4 alkoxy, C 2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; R a and R b , which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C 1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula: --NH--CH.sub.2 --CO-- or a group of formula: ##STR2## where R 1 is hydrogen or methyl; R 2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR 3 or --NR 4 R 5 where R 3 , R 4 and R 5 are each hydrogen or alkyl of 1 to 4 carbon atoms (i.e. methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or t-butyl) and R 3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkepalin analogues.

Inventors

• 👤 Samuel Wilkinson
• 👤 George W. Hardy
• 👤 Roger Wrigglesworth

Bibliographic Details