PHARMACEUTICAL AMIDES AND PREPARATION FORMULATIONS AND USE THEREOF

• Main Authors: SAMUEL WILKINSON, GEORGE WILLIAM HARDY
• Format: Patent
• Language: English
• Published: 11.05.1983
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Compounds of the general formulawherein Ph is a phenyi group which is optionally substituted by one or more substituents selected from halo (ie fluoro, chloro, bromo or iodo), C1-4alkyl, amino, C1-4alkylamino, di-C1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C1-4alkoxycarbonyl, amido, C1-4alkylamido, C1-4alkoxy, C2-4alkenyl, cyano, aminomethyl, or methylsulphonyl;Y is a group of formulawhere R1 is hydrogen or methyl;R2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is -OR3 or -NR4R5 where R3, R4 and R5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R3 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, eg. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkehalin analogues.