Peptide and pseudopeptide derivatives

Details Peptide and pseudopeptide derivatives Peptide and pseudopeptide derivatives

1983-08-16

1984-10-02

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Immunoglobulin, antiserum, antibody, or antibody fragment,...

Reduced antigenicity, reduced ability to bind complement, or...

2601125E, A61K 3700, C07C10352

Patent

active

044747675

ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sup.1 stands for an alk-2-enyl radical of not more than 5 carbon atoms or a furylmethyl radical, R.sup.2 stands for an alk-2-enyl or alkyl radical of not more than 5 carbon atoms or a furylmethyl radical, >N--A, B, D, E and F stand for defined amino acid or aza-amino-acid residues, and in particular one or both of B and D stand(s) for an amino acid residue of the formula --NH.C(1-3C alkyl)(1-3C alkyl).CO-- or a similar residue, and X stands for --OR.sup.7 or --NR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, stand for hydrogen or a (1-4C)alkyl radical, and wherein the linkages are all conventional peptide linkages or in the case of D-E the peptide linkage is replaced by the group --CH.sub.2 S--, and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutically-acceptable diluent or carrier. The compounds are selective opiate .delta.-receptor antagonists.

REFERENCES:
patent: 4221682 (1980-09-01), Sarantakis
patent: 4320051 (1982-03-01), Sarantakis
patent: 4322342 (1982-03-01), Smithwick, Jr. et al.
patent: 4331593 (1982-05-01), Smithwick, Jr. et al.
Shaw et al., Life Sciences, 1982, 31, 1259-1262 (Pergamon Press).
Gormley et al., Life Sciences, 1982, 31, 1263-1266.
Nagaraj et al., FEBS Letters, 1979, 106, No. 2, 271-274.
Belton et al., Life Sciences, 1983, 33, Suppl. I, 443-446.

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