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Exendin-4 derivatives as selective glucagon receptor agonists

A solvate and peptide compound technology, applied in the direction of glucagon, hormone peptide, vasoactive intestinal peptide, etc., can solve the problem of not significantly activating glucagon receptors

Active Publication Date: 2020-09-15
SANOFI SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Exendin-4 is an activator of the glucagon-like peptide-1 (GLP-1) receptor, but it does not significantly activate the glucagon receptor

Method used

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  • Exendin-4 derivatives as selective glucagon receptor agonists
  • Exendin-4 derivatives as selective glucagon receptor agonists
  • Exendin-4 derivatives as selective glucagon receptor agonists

Examples

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Embodiment Construction

[0119] definition

[0120] The amino acid sequences of the invention contain the conventional one-letter and three-letter codes for naturally occurring amino acids, as well as the generally accepted three-letter codes for other amino acids, such as Nle (norleucine).

[0121] Alternatively, use the following codes for the amino acids shown in Table 1:

[0122]

[0123] The term "natural exendin-4" refers to 2 Native Exendin-4 of (SEQ ID NO: 1).

[0124] The present invention provides a peptide compound as defined above.

[0125] The peptidic compounds of the present invention comprise a linear backbone of aminocarboxylic acids linked by peptides (ie, carboxamide bonds). Preferably, the aminocarboxylic acid is an alpha-aminocarboxylic acid and more preferably an L-alpha-aminocarboxylic acid, unless otherwise specified. The peptide compound contains a backbone sequence of 39 aminocarboxylic acids.

[0126] For the avoidance of doubt, in the definitions provided herein, it...

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Abstract

The present invention relates to glucagon receptor agonists and their medical use, for example for the treatment of severe hypoglycemia. Exendin-4 analogs are provided that potently and selectively activate the glucagon receptor and exhibit higher solubility at near neutral pH and enhanced in solution compared to native glucagon chemical stability. The analog has the artificial amino acid 4-thiazolealanine at position 1. This resulted in a higher selectivity for the glucagon receptor over the GLP1 receptor when compared to each other for the same compounds differing only in position 1 (Tza instead of His at position 1). The present invention provides highly selective glucagon receptor agonists.

Description

[0001] manual [0002] field of invention [0003] The present invention relates to peptide analogs of exendin-4 that activate the glucagon receptor, and their medical use, for example in the treatment of severe hypoglycemia. [0004] Background of the invention [0005] Exendin-4 is a 39 amino acid peptide produced by the salivary glands of 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, but it does not significantly activate the glucagon receptor. [0006] The amino acid sequence of Exendin-4 is shown in SEQ ID NO:1: [0007] HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 [0008] Glucagon is a 29 amino acid peptide that is released into the bloodstream when circulating glucose is low. The amino acid sequence of glucagon is shown in SEQ ID NO:2: [0009] HSQGTFTSDYSKYLDSRRAQDFVQWLMNT-OH [0010] During hypoglycemia, when blood sugar levels drop below no...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/575A61K38/16A61P3/10A61P3/08A61P5/48
CPCC07K14/57563A61K38/00A61P1/00A61P3/00A61P3/08A61P39/02A61P43/00A61P5/48A61P3/10A61K38/2278A61K45/06C07K14/605
Inventor T·哈克S·斯坦格林A·艾弗斯M·瓦格纳B·亨克尔
Owner SANOFI SA
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