Exenatide analog

A technology of exenatide and analogues, applied in the field of glucagon-like peptide-1 analogues, can solve the problems of short plasma half-life, instability of GLP-1, and limitation of clinical application of GLP-1, and achieve remarkable results , Stable properties, hypoglycemic effect

Active Publication Date: 2019-12-10
CHENGDU AODA BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, GLP-1 is also facing a huge problem in clinical application. The GLP-1 produced by the human body is very unstable, and it is easily absorbed by dipeptidyl peptidase IV in the body. (DPP-IV) degradation, its short plasma half-life limits the clinical application of GLP-1

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of Compound 1

[0038]

[0039] 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:

[0040] 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.

[0041] In the above preparation method, the substitution value of the carrier resin is 0.2-1.0 mmol / g resin, preferably 0.3-0.5 mmol / g resin.

[0042] As a preferred solution of the present invention, the solid-...

Embodiment 2

[0074] Example 2 Preparation of Compound 2

[0075]

[0076] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0077]

[0078]

[0079] 6.2 g of pure product was obtained, the purity was 95.8%, and the total yield was 12.2%. Molecular weight 5070.6 (100% M+H).

Embodiment 3

[0080] Example 3 Preparation of compound 3

[0081]

[0082] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0083]

[0084]

[0085] 8.9 g of pure product was obtained, the purity was 98.5%, and the total yield was 17.6%. The molecular weight is 5043.2 (100% M+H).

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Abstract

The invention relates to the field of medicine synthesis and discloses an exenatide analog. The exenatide analog disclosed by the invention is used for preparing a medicine composition for treating diseases. The invention discloses application of medicine composition in preparing medicines for treating at least one of the following diseases: type-II diabetes, impaired glucose tolerance, type-I diabetes, obesity, hypertension, metabolic syndrome, dyslipidemia, cognitive disorder, atherosclerosis, myocardial infarction, coronary heart diseases, cardiovascular diseases, stroke, inflammatory intestinal tract syndrome and / or dyspepsia or gastric ulcer, hepatic fibrosis diseases and pulmonary fibrosis diseases.

Description

technical field [0001] The present invention relates to an exenatide analogue and its application, the analogue is 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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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605C07K14/575A61K38/26A61K38/22A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P9/10A61P25/00A61P9/00A61P1/00A61P29/00A61P1/14A61P1/16A61P11/00
CPCC07K14/605C07K14/57563A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P9/10A61P25/00A61P9/00A61P1/00A61P29/00A61P1/14A61P1/16A61P11/00A61K38/00A61K38/26
Inventor 周述靓王鹏邓岚
Owner CHENGDU AODA BIOTECHNOLOGY CO LTD
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