Biologically active amides
AssigneeBurroughs Wellcome Co.
InventorSamuel Wilkinson
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Abstract
The present invention provides novel peptides of formula (I): R--(X.sup.1).sub.m --(X.sup.2).sub.n --X.sup.3 --X.sup.4 --X.sup.5 --X.sup.6 --X.sup.7 --(X.sup.8).sub.p --(X.sup.9).sub.q --R.sup.1 (I) together with their salts, esters, amides, N-alkylamides and N,N-dialkylamides and acid addition salts thereof. These compounds exhibit morphine agonist activity in both in vitro and in vivo tests and may be used in the treatment of mammals in the fields of both human and veterinary medicine in any condition where an agent with a morphine-like effect is indicated.
Claims28
A compound of the formula:
- H.Tyr.Gly.Gly.Phe.X.sup.7.OR
- wherein:
- X.sup.7 is selected from the group consisting of Ile, Nle,Pro, Val, Ala, NVa, D-Leu and D-Met;
- R is lower alkyl of 1 to 6 carbon atoms;
- and the stereochemical configuration of the Tyr and Phe residues may independently be D, L or DL.
A pharmaceutical formulation for obtaining a morphine-like effect comprising a pharmaceutically acceptable carrier and an effective morphine-like treatment amount of a compound of the formula:
- H.Tyr.Gly.Gly.Phe.X.sup.7.OR
- or a pharmacologically and pharmaceutically acceptable salt, ester, amide, N-alkylamide or N,N-dialkylamide thereof, or a pharmacologically and pharmaceutically acceptable acid addition salt thereof, wherein:
- X.sup.7 is selected from the groups consisting of Ile, Nle, Pro, Val, Ala, NVa, D-Leu and D-Met;
- R is lower alkyl of 1 to 6 carbon atoms;
- and
- the stereochemical configuration of the Tyr and Phe residues may independently be D, L or DL.
A method for the treatment of a mammal for a condition therein an agent with a morphine-like effect is indicated, comprising the administration to the mammal of an effective morphine-like treatment, non-toxic amount of a peptide of the formula:
- H-Tyr.Gly.Gly.Phe.X.sup.7.OR
- or a pharmacologically and pharmaceutically acceptable salt, ester, amide, N-alkylamide or N,N-dialkylamide thereof, or a pharmacologically and pharmaceutically acceptable acid addition salt thereof, wherein
- X.sup.7 is selected from the group consisting of Ile, Nle, Pro, Val, Ala, NVa, D-Leu and D-Met;
- R is lower alkyl of 1 to 6 carbon atoms;
- and the stereochemical configuration of the Tyr and Phe residues may independently be D, L or DL.
Dependencies are inferred from the claim text.