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GIP and GLP-1 double-agonistic polypeptide compound and pharmaceutically acceptable salt and application thereof

A GLP-1, peptide compound technology, applied in hormone peptides, organic chemistry, hormone receptors, etc., can solve problems such as prolonging the half-life of peptides

Active Publication Date: 2020-01-14
杭州禾泰健宇生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the use of fatty acids can improve the half-life of the peptides, applicants discovered that, as part of the present invention, the length, composition and location of the fatty acid chains and the linker between the peptide and the fatty acid chains may have unexpected effects on GIP and GLP-1 agonist activity Balanced effects while prolonging the half-life of the peptide

Method used

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  • GIP and GLP-1 double-agonistic polypeptide compound and pharmaceutically acceptable salt and application thereof
  • GIP and GLP-1 double-agonistic polypeptide compound and pharmaceutically acceptable salt and application thereof
  • GIP and GLP-1 double-agonistic polypeptide compound and pharmaceutically acceptable salt and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Embodiment 1, the synthesis of SEQ ID NO: 1 polypeptide compound:

[0091] YVEGTFTSDYSIVLDKIAQK(HOOC-(CH 2 ) 16 -CO-γ-Glu-AEEA-AEEA)AFVQWLIAGGPSSGAPPPS-NH 2

[0092] 1. Synthesis of peptide chains

[0093] 1.1 Resin swelling

[0094] Weigh 10g of Fmoc-Rink Amide AM Resin (degree of substitution 0.35mmol / g), swell with 100mL of DCM for 30min, filter to remove DCM, then swell with 100mL of DMF for 30min, rinse with DMF and 100mL of DCM respectively.

[0095] 1.2 Synthesis of Fmoc-Ser(tBu)-Rink Amide AM Resin

[0096]Dissolve Fmoc-Ser(tBu)-OH (8mmol), HOBT (16mmol) and DIC (16mmol) in 100mL of DMF, then add this solution to the resin obtained in the previous step to react for 2 hours, and filter the reaction solution after completion. The resin was washed 3 times with 100 mL each of DCM and DMF.

[0097] 1.3 Removal of Fmoc protecting group

[0098] Add 25% piperidine / DMF (V / V) solution containing 0.1M HOBt to the washed resin to remove Fmoc, and wash the resin 3 t...

Embodiment 2

[0108] Embodiment 2, the synthesis of SEQ ID NO:2 polypeptide compound:

[0109] YXEGTFTSDYSIXLDKIAQK(HOOC-(CH 2 ) 16 -CO-γ-Glu-AEEA-AEEA)AFVQWLIAGGPSSGAPPPS-NH 2

[0110]

[0111] The synthesis method was the same as in Example 1, and the collected solution was freeze-dried to obtain 1.45 g of pure product.

Embodiment 3

[0112] Embodiment 3, the synthesis of SEQ ID NO:3 polypeptide compound:

[0113] YXEGTFTSDYSIXLDKIAQK(HOOC-(CH 2 ) 16 -CO-γ-Glu-AEEA-AEEA)AFVQWLIAGGPSSGAPPPS-NH 2

[0114]

[0115] The synthesis method was the same as in Example 1, and the collected solution was lyophilized to obtain 1.51 g of pure product.

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PUM

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Abstract

The invention discloses a GIP and GLP-1 double-agonistic polypeptide compound, and belongs to the technical field of polypeptide medicinal chemistry. The GIP and GLP-1 double-agonistic polypeptide compound has an amino acid sequence as follows: YXaa1EGTFTSDYSIXaa2LDKIAQXaa3AFVQWLIAGGPSSGAPPPS, and C-terminal amino acid of the polypeptide compound is amidated as a C-terminal primary amide. The invention relates to a preparation method, a pharmaceutically acceptable salt, a pharmaceutical composition and a medicament of the polypeptide compound. The polypeptide compound disclosed by the invention has effects of reducing blood glucose and losing weight, and can be used as an effective raw material for preparing a medicament for treating or preventing diabetes or a weight-losing medicament.

Description

technical field [0001] The present invention relates to the field of polypeptide compounds, in particular to a polypeptide compound with double incretin peptide analogues, which stimulates the receptors of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) body, and can be used to treat type 2 diabetes. The present invention also relates to the pharmaceutically acceptable salt of the polypeptide compound, the polypeptide pharmaceutical composition, the preparation method of the medicament and the use thereof. Background technique [0002] The cause of metabolic syndrome is abnormal metabolism of various substances such as protein, fat and carbohydrates. Overnutrition and reduced physical activity can lead to obesity and obesity-related diseases such as diabetes. In recent years, the incidence of type 2 diabetes and abnormal blood lipid metabolism has been increasing; type 2 diabetes is the most common form of diabetes, accounting for abo...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K1/06C07K1/04A61K38/16A61P3/04A61P3/10
CPCC07K14/00A61P3/04A61P3/10A61K38/00C07K14/605C07K14/72C07K14/595A61K38/16A61K45/06C07K14/001
Inventor 赵呈青谷海涛施国强姜建军王蔡典
Owner 杭州禾泰健宇生物科技有限公司
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