Opioid peptides

Details Opioid peptides Opioid peptides

1994-12-08

1997-09-02

Tsang, Cecilia

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

4 to 5 amino acid residues in defined sequence

530329, A61K 3800, C07K 700, C07K 706

Patent

active

056632959

ABSTRACT:
Opioid peptides including those of the formula ##STR1## in which A.sub.1 is the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, azatyrosine, and 2,6-dimethyltyrosine; A.sub.2 is the identifying group of an amino acid selected from D-Ala and D-Arg; A.sub.3 is H, or the identifying group of an amino acid selected from of 3,4-dihydroxyphenylalanine and 3,4-dimethoxyphenylalanine, A.sub.4 is H, cyclohexylmethyl, the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, Phe, and substituted Phe with its benzene ring substituted by halogen, NO.sub.2, OH, or CH.sub.3 ; A.sub.5 is the identifying group of a D- or L-amino acid selected from Leu, Nle, Lys, Met and Met(O), or is deleted together with R.sub.4 --CH attached thereto; each R.sub.1 and R.sub.2 is --H, --C(NH.sub.2).dbd.NH, or C.sub.1-12 alkyl; R.sub.3 is ##STR2## R.sub.4 is ##STR3## and R.sub.5 is --(CH.sub.2).sub.n+1 OH, ##STR4## wherein m is 0-6, n is 0-6, and X is H, C.sub.1-12 alkyl, C.sub.6-12 aryl, C.sub.7-18 aralkyl, C.sub.7-18 alkaryl, C.sub.7-18 alkayl, C.sub.6-17 pyridylalkyl, or C.sub.6-17 alkylpyridyl; provided that when one of R.sub.1 and R.sub.2 is --C(NH.sub.2).dbd.NH, the other must be H; or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 4216128 (1980-08-01), Sarantokis
patent: 4599325 (1986-07-01), Hansen, Jr. et al.
Salvadori et al., "Synthesis and Pharmacological Activity of the N-terminal Dermorphin Tetrapeptide Analogs with CH.sub.2 -NH Peptide Bond Isosteres", Int. J. Peptide Protein Res. 40:437-444, 1992.
Kubota, et al, vol. 28, Chem. Pharm. Bull. vol. 28, 1980.
Coy et al., "Solid Phase Reductive Alkylation Techniques in Analogue Peptide Bond and Side Modification", Tetrahedron, 44:835-844, 1988.
Hruby et al., "Recent Developments in the Design of Receptor Specific Opioid Peptides" Medical Research Reviews 9:343-401, 1989.
Sasaki et al., "Studies on Analgesic Oligopeptides. VII. Solid Phase synthesis and Biological Properties of Tyr-D-Arg-Phe-.beta.Ala-NH2 & Its Fluorinated Aromatic Amino Acid Der . . . ", Chem. Pharm. Bull 39:2316-2318, 1991.
Vavrek et al., "Minimum Structure Opioids-Dipeptide and Tripeptide Analogs of the Erkephalins" Peptides 2:303-308, 1981.

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