Pharmaceutical amides, and preparation, formulations and use the

Details Pharmaceutical amides, and preparation, formulations and use the Pharmaceutical amides, and preparation, formulations and use the

1982-09-24

1985-03-12

Trousof, Natalie

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

260465B, 260465D, 260465E, 514534, 514603, 514616, 560 13, 560 16, 560 22, 560 39, 562426, 562430, 562437, 562448, 564 82, 564 86, 564153, A61K 31275, A61K 31215, A61K 31195, C07C10124

Patent

active

045044929

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.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido, C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl, or methylsulphonyl; Y is a group of formula ##STR2## where R.sup.1 is hydrogen or methyl; R.sup.2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR.sup.3 or --NR.sup.4 R.sup.5 where R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R.sup.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 enkephalin analogues.

REFERENCES:
patent: 4105789 (1978-08-01), Ondetti et al.
patent: 4228184 (1980-10-01), Ondetti et al.
patent: 4386031 (1983-05-01), Hillboll et al.
patent: 4423242 (1983-12-01), Wilkinson et al.
European Journal of Pharmacology, vol. 57, pp. 279-281, (1979), Swerts et al.
Nature, vol. 258, pp. 577-579, (1975), Hughes et al.
Nature, vol. 276, pp. 523-526, (1978), Malfroy et al.

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