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Exendin-4 derivatives

A peptide compound, compound technology, applied in the direction of antitoxins, hormone peptides, specific peptides, etc., can solve problems such as chemical instability of Exendin-4

Inactive Publication Date: 2015-09-09
SANOFI SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] But exendin-4 is chemically unstable due to the oxidation of methionine at position 14 (Hargrove DM et al., Regul. Pept., 141:113-9, 2007), and the methionine at position 28. Asparagine deamination and isomerization (WO 2004 / 035623)

Method used

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Embodiment Construction

[0352] definition

[0353] The amino acid sequences of the present invention contain the conventional one-letter or three-letter codes for naturally occurring amino acids, as well as the generally accepted three-letter codes for other amino acids, such as Aib (alpha-aminoisobutyric acid), Orn (ornithine ), Dab (2,4-diaminobutyric acid), Dap (2,3-diaminopropionic acid), Nle (norleucine), GABA (γ-aminobutyric acid) or Ahx (ε-aminocaproic acid )

[0354] In addition, the following codes were used for the amino acids shown in Table 4.

[0355] Table 4:

[0356]

[0357] The term "natural exendin-4" means a compound having the sequence HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 Native Exendin-4 of (SEQ ID NO: 1).

[0358] The present invention provides a peptide compound as defined above.

[0359] The peptidic compounds of the present invention comprise a linear backbone of aminocarboxylic acids linked by peptide bonds, ie, carboxamide bonds. Preferably, the aminocarboxy...

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Abstract

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

Description

[0001] manual Field of Invention [0002] The present invention relates to exendin-4 (exendin-4) peptide analogs that activate glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors, and optionally Glucagon receptors (GCGs) are actively activated, and their medicinal uses, such as in the treatment of conditions of the metabolic syndrome including diabetes and obesity, and reduction of 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 glucagon-like peptide-1 (GLP-1) receptors, however it shows only very low activation of GLP receptors and does not activate glucagon receptors. body (see Table 1). [0004] Table 1: Potency of exendin-4 at increasing concentrations at human GLP-1, GIP and glucagon receptors (in pM), and measured cAMP formed as described in Meth...

Claims

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Application Information

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IPC IPC(8): A61K38/26C07K14/605
CPCA61K38/00A61K38/26A61K38/28A61K38/2264A61K45/06C07K14/605A61P1/00A61P1/16A61P25/00A61P25/28A61P25/30A61P3/00A61P3/04A61P3/06A61P3/08A61P39/02A61P43/00A61P9/00A61P9/10A61P9/12A61P3/10Y02A50/30A61K2300/00A61K9/0019
Inventor T·哈克M·瓦格纳B·亨克尔S·斯滕格林A·埃弗斯M·洛伦茨K·洛伦茨
Owner SANOFI SA
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