Cyclic hexapeptide somatostatin analogs

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Somatostatin ; related peptides

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514806, C07K 726, A61K 3724

Patent

active

046110542

ABSTRACT:
Cyclic hexapeptide somatostatin analogs are prepared wherein a peptide surrogate replaces eight of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

REFERENCES:
patent: 4310518 (1982-01-01), Freidinger et al.
Spatola (I), Chemistry and Biochemistry of Amino Acids Peptides and Protein, B. Weinstein (Ed) Marcel Dekker Inc., New York, pp. 267-357 (1984).
Spatola (II), Proceedings of the 8th American Peptide Symposium, Tucson, Arizona, May 22-27, 1983, pp. 341-344.

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