Cyclic hexapeptide somatostatin analogs

Details Cyclic hexapeptide somatostatin analogs Cyclic hexapeptide somatostatin analogs

1983-10-27

1985-06-11

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125R, C07C10352, A61K 3702

Patent

active

045228132

ABSTRACT:
Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven 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: 4235886 (1980-11-01), Freidinger et al.
patent: 4310518 (1982-01-01), Freidinger et al.
patent: 4360516 (1982-11-01), Freidinger et al.
patent: 4427661 (1984-01-01), Curley et al.
Organic Chemistry, Cram and Hammond, p. 530, (1959).
Organic Chemistry, Morrison and Boyd, p. 866, (1959).
Veber et al., Nature, 22, 55-58, (1981).
Rivier et al., Biochemical and Biophysical Research Communications, 65, (No. 2), 746-751, (1975).

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