GIP/GLP-1 analogue

An analog, the technology of reparatide, which is applied in the field of tireparatide analogs, can solve the problems of not being able to achieve full-effect blood sugar control and weight loss, and achieve the effects of stable properties, weight reduction, and hypoglycemic weight loss.

Active Publication Date: 2020-06-23
CHENGDU AODA BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The most common side effects of GLP-1 analogues are administration that does not achieve full glycemic control and weight loss, whereas GIP alone has a very modest glucose lowering capacity in type 2 diabetics
Both native GIP and GLP-1 are rapidly inactivated by the ubiquitous protease DPP IV and therefore should only be used for short-term metabolic control

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation of embodiment 1 compound 1

[0033] Tyr-Dhthr-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhthr-Leu-Asp-Lys-Ile-Ala-Gln-Lys (AEEA-AEEA-γGlu-18 alkanedioic acid )-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH 2

[0034] 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:

[0035] 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.

[0...

Embodiment 2

[0069] The preparation of embodiment 2 compound 2

[0070] Tyr-Dhval-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhval-Leu-Asp-Lys-Ile-Ala-Gln-Lys (AEEA-AEEA-γ-Glu-18 alkane Diacid)-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH 2

[0071] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0072]

[0073]

[0074] 6.1 g of pure product was obtained, the purity was 96.9%, and the total yield was 12.5%. Molecular weight 4809.5 (100% M+H).

Embodiment 3

[0075] The preparation of embodiment 3 compound 3

[0076] Tyr-Dhthr-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhthr-Leu-Asp-Lys-Ile-Ala-Gln-Lys(PEG 5 CH 2 CO-γGlu-18 alkanedioic acid)-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH 2

[0077] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0078]

[0079]

[0080] 7.4 g of pure product was obtained, the purity was 96.3%, and the total yield was 15.3%. Molecular weight 4768.4 (100% M+H).

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Abstract

The invention relates to the field of medicine synthesis, and discloses a GIP / GLP-1 analogue. The GIP / GLP-1 analogue is used for preparing a pharmaceutical composition for treating diseases, and the pharmaceutical composition is used for preparing a medicine 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 disease, cardiovascular disease, stroke, inflammatory intestinal syndrome and / or dyspepsia orgastric ulcer, hepatic fibrosis disease and pulmonary fibrosis disease.

Description

technical field [0001] The present invention relates to a kind of tiriparatide analogue and its application, this analogue is a kind of dual function of stimulating human glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor Incretin peptide mimetic compounds. Background technique [0002] GIP is a 42 amino acid gastrointestinal regulatory peptide that plays a physiological role in glucose homeostasis by stimulating insulin secretion from pancreatic β cells in the presence of glucose and protecting pancreatic β cells. GLP-1 is a 37 amino acid peptide that stimulates insulin secretion, protects pancreatic beta cells, and inhibits glucagon secretion, gastric emptying and food intake, leading to weight loss. GIP and GLP-1 are known as incretins; incretin receptor signaling plays a key physiologically relevant role for glucose homeostasis. In normal physiology, GIP and GLP-1 are secreted from the gut after a meal, and these incretins e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575C07K14/605A61K38/22A61K38/26A61P3/10A61P3/04A61P9/12A61P3/00A61P9/10A61P9/00A61P1/14A61P1/16
CPCC07K14/575C07K14/605A61P3/10A61P3/04A61P9/12A61P3/00A61P9/10A61P9/00A61P1/14A61P1/16A61K38/00
Inventor 周述靓王鹏邓岚潘文强
Owner CHENGDU AODA BIOTECHNOLOGY CO LTD
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