Bridged cyclic hexapeptide somatostatin analogs

Details Bridged cyclic hexapeptide somatostatin analogs Bridged cyclic hexapeptide somatostatin analogs

1985-06-24

1987-05-05

Phillips, Delbert R.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Somatostatin ; related peptides

530317, 514806, 540482, C07K 726, C07K 512, A61K 3724

Patent

active

046634355

ABSTRACT:
Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a bridged grouping which replaces eight of the ring amino acids of somatostatin. The bridged 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 selectively 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 bridged cyclic hexapeptides are prepared by the solid phase method.

REFERENCES:
patent: 3842067 (1974-10-01), Sarantakio
patent: 3972859 (1976-08-01), Fujino et al.
patent: 4139526 (1979-02-01), Veber
patent: 4235886 (1980-11-01), Freidinger et al.
patent: 4310518 (1982-01-01), Freidinger et al.
Brady, et al., Med. Chem. Symposium (Presentation).
Life Sciences 34, 1371-1378 (1984).

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