Peptidic dual GLP-1 / glucagon receptor agonists derived from exendin-4

A receptor and selected technology, applied in the direction of glucagon, peptide/protein components, hormone peptides, etc., can solve the chemical instability of exendin-4 and other problems
CN106414488AActive Publication Date: 2017-02-15SANOFI SA

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SANOFI SA
Publication Date
2017-02-15

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Abstract

Peptidic dual GLP-1 / Glucagon Receptor Agonists derived from Exendin-4 The present invention relates to dual GLP-1 / glucagon receptor agonists or optionally trigonal GLP-1 / glucagon / GIP receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.
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Description

[0001] field of invention

[0002] The present invention relates to exendin-4 (exendin-4) peptide analogs, which activate glucagon-like peptide-1 (GLP-1) and glucagon (GCG) receptors and optionally glucose- Dependent insulinotropic polypeptide (GIP) receptors, and their medical uses, for example in the treatment of disorders of the metabolic syndrome (including diabetes and obesity) and in reducing excess food intake.

[0003] Background of the invention

[0004] Exendin-4 is a 39-amino acid peptide produced by the salivary glands of the monster monster (Heloderma suspectum) (Eng J. et al., J. Biol. Chem., 1992, 267, 7402- 05). Exendin-4 is an activator of the glucagon-like peptide-1 (GLP-1) receptor, but it shows only very low activation of the GIP receptor and does not activate the glucagon receptor (see Table 1).

[0005] Table 1: Potency (expressed in pM) of increasing concentrations of exendin-4 on GLP-1, GIP and glucagon receptors and cAMP formed measured as described ...

Claims

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