O-substituted tyrosyl dipeptide amides

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.

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C07K 508

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active

047974702

ABSTRACT:
This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -R.sup.9 may be the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein C.sub.w is an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v is an asymmetric carbon atom and may be racemic or may have the D or L configuration.
The compounds of this invention are useful because they possess analgesic activity in mammals.

REFERENCES:
patent: 4127535 (1978-11-01), Coy et al.
patent: 4316892 (1982-02-01), Jones
patent: 4407746 (1983-10-01), Mazur et al.
patent: 4579841 (1986-04-01), Stewart et al.
patent: 4603121 (1986-07-01), Hansen, Jr. et al.

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