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GLP-1 (glucagon-like peptide-1) compound

A GLP-1 and compound technology, applied in the field of semaglutide analogs, can solve the problems of instability of GLP-1 and limit the clinical application of GLP-1, and achieve the effect of stable properties and significant hypoglycemic effect.

Active Publication Date: 2019-12-20
BEIJING LEPU PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the clinical application of GLP-1 also faces huge problems. The GLP-1 produced by the human body is very unstable and easily degraded by dipeptidyl peptidase IV (DPP-IV) in the body, and its plasma half-life is only 1 to 2 minutes , that is, continuous intravenous infusion or continuous subcutaneous injection is necessary to produce curative effect, which greatly limits the clinical application of GLP-1

Method used

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Examples

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Effect test

Embodiment 1

[0038] Example 1 Preparation of Compound 1

[0039]

[0040] The preparation method includes: preparing the peptide resin by solid-phase polypeptide synthesis method, acid hydrolyzing the peptide resin to obtain a crude product, and finally purifying the crude product to obtain a pure product; wherein the step of preparing the peptide resin by the solid-phase polypeptide synthesis method is to pass solid-phase The phase-coupled synthesis method sequentially inserts the corresponding protected amino acids or fragments in the following sequences to prepare peptide resins:

[0041] In the above preparation method, the amount of the Fmoc-protected amino acid or protected amino acid fragment is 1.2-6 times of the total moles of the resin fed; preferably 2.5-3.5 times.

[0042] In the above preparation method, the substitution value of the carrier resin is 0.2-1.0 mmol / g resin, and the preferred substitution value is 0.3-0.5 mmol / g resin.

[0043] As a preferred solution of the ...

Embodiment 2

[0079] Example 2 Preparation of Compound 2

[0080]

[0081] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0082]

[0083]

[0084] 8.5 g of pure product was obtained, the purity was 97.5%, and the total yield was 20.7%. Molecular weight 4124.2 (100% M+H).

Embodiment 3

[0085] Example 3 Preparation of compound 3

[0086]

[0087] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0088]

[0089]

[0090] 5.1 g of pure product was obtained with a purity of 97.0% and a total yield of 12.4%. Molecular weight 4097.6 (100% M+H).

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Abstract

The invention relates to the field of medicine synthesis, and discloses a GLP-1 (glucagon-like peptide-1) compound. The Semaglutide analogue disclosed by the invention is used for preparing a medicinecomposition used for treating diseases. The medicine composition has purposes for preparing medicines for treating at least one of the following diseases, including diabetes mellitus II, impaired glucose tolerance, diabetes mellitus I, obesity, hypertension, metabolic syndrome, dyslipidemia, cognitive disorder, atherosclerosis, myocardial infarction, coronary heart diseases, cardiovascular diseases, stroke, inflammatory bowel syndromes and / or dyspepsia or gastrohelcosis, hepatic fibrosis diseases and pulmonary fibrosis diseases.

Description

technical field [0001] The present invention relates to a semaglutide analogue and use thereof, the analogue being a glucagon-like peptide-1 (GLP-1) analogue. Background technique [0002] Diabetes has become the third non-communicable disease after cardiovascular and cerebrovascular diseases and tumors. The World Health Organization (WHO) predicts that there will be more than 360 million diabetics in the world in 2030, of which more than 90% are type II diabetes. GLP-1 is a secreted secreted by intestinal L cells, which has the functions of promoting insulin secretion, inhibiting the release of glucagon, stimulating the proliferation of islet B cells, inducing the regeneration of islet B cells, preventing the apoptosis of islet B cells, improving Insulin sensitivity and increased glucose utilization play an important role in the occurrence and development of type II diabetes. In patients with type II diabetes, the "insulin-stimulating islet effect" is impaired, mainly mani...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/26A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P25/00A61P9/10A61P9/00A61P1/00A61P29/00A61P1/14A61P1/04A61P1/16A61P11/00
CPCC07K14/605A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P25/00A61P9/10A61P9/00A61P1/00A61P29/00A61P1/14A61P1/04A61P1/16A61P11/00A61K38/00A61K38/26A61K31/417A61K38/16
Inventor 周述靓王鹏邓岚
Owner BEIJING LEPU PHARM TECH CO LTD
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