Bicyclic oligopeptides

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Reexamination Certificate

active

07101848

ABSTRACT:
The invention relates to a bicyclic oligopeptide or ester thereof having the capability to inhibit the glucagon receptor, comprised of:(a) a first cyclic group, which comprises at least one cysteine group and is formed by an amide bonding of the N-terminal amino acid with the second carboxylate group of a diacid amino acid, and(b) a second cyclic group which is formed by an amide bonding of an amino acid with the α-carboxylate group of said diacid amino acid, and by a disulfide bonding of the C-terminal cysteine and a cysteine group within the first cyclic group (a); andto the use of such bicyclic oligopeptides for the preparation of a medicament for the treatment or prevention of diseases, in which glucagon receptors are involved.

REFERENCES:
patent: 4139526 (1979-02-01), Veber
patent: 6211145 (2001-04-01), Yanai et al.
Yano, et al., 1996, Bioorganic & Medicinal Chemistry, 4, 115-120.
Renner, et al., 1999, J. Am. Chem. Sco., 121, 11273-76.
He, et al., 1995, Bioorganic & Medicinal Chemistry, 5, 621-626.
Janice C. Parker, et al., “Effects of Skyrin, a Receptor-Selective Glucagon Antagonist, in Rat and Human Hepatocytes”, Diabetes, vol. 49, 2079-2086 Dec. 2000, XP-001154854.
James G. McCormack, et al., “Pharmacological Approaches to Inhibit Endogenous Glucose Production as a Means of Anti-diabetic Therapy”, Current Pharmaceutical Design, 2001, 7, 1451-1474, XP-001154855.
K.F.Peterson, et al., “Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans”, Diabetologia (2001) 44:2018-2024, XP-002259423.

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