glp1/gip dual agonist or glp1/gip/glucagon triple agonist

A technology for hyperglycemia and body weight, applied in the direction of glucagon, hormone peptides, anti-toxins, etc., can solve the chemical instability of exendin-4 and other problems
CN104902919BInactive Publication Date: 2018-11-20SANOFI SA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SANOFI SA
Publication Date
2018-11-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates to exendin-4 derivatives and their use in medicine, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, and in reducing excess food intake.
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Description

[0001] manual field of invention

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

[0003] Exendin-4 is a 39 amino acid peptide produced by the Gila monster (Heloderma suspectum) (Eng J. et al., J. Biol. Chem. , 267:7402-05, 1992). Exendin-4 is an activator of the glucagon-like peptide-1 (GLP-1) receptor, however it shows only low activation of the GLP receptor and does not activate the glucagon receptor. body (see Table 1).

[0004] Table 1: Potency of exendin-4 at increasing concentrations on human GLP-1, GIP and glucagon receptors (expressed in pM), and cAMP formed measured as described i...

Claims

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