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Tiripa peptide analogue

A technology of ripatide and analogues, applied in the field of tiripatide analogues, can solve the problems of inability to achieve full-effect blood sugar control and weight loss, and achieve the effects of stable properties, weight loss, and weight loss

Inactive Publication Date: 2020-01-03
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 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

[0038] Example 1 Preparation of Compound 1

[0039] Tyr-Dhthr-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhthr-

[0040] Leu-Asp-Lys-Ile-Ala-Gln-Lys (AEEA-AEEA-γGlu-18 alkanedioic acid)-

[0041] Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-

[0042] Ala-Pro-Pro-Pro-Ser-NH 2

[0043] 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:

[0044] 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; prefera...

Embodiment 2

[0078] Example 2 Preparation of Compound 2

[0079] Tyr-Dhval-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhval-

[0080] Leu-Asp-Lys-Ile-Ala-Gln-Lys (AEEA-AEEA-γ-Glu-18 alkanedioic acid)-

[0081] Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-

[0082] Ala-Pro-Pro-Pro-Ser-NH 2

[0083] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0084]

[0085]

[0086] 6.1 g of pure product was obtained, the purity was 96.9%, and the total yield was 12.5%. Molecular weight 4865.2 (100% M+H).

Embodiment 3

[0087] Example 3 Preparation of compound 3

[0088] Tyr-Dhthr-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Dhthr-

[0089] Leu-Asp-Lys-Ile-Ala-Gln-Lys (PEG 5 CH2 CO-γGlu-18 alkanedioic acid)-

[0090] Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-

[0091] Ala-Pro-Pro-Pro-Ser-NH 2

[0092] The preparation method is the same as in Example 1, and the protected amino acids used are as follows:

[0093]

[0094]

[0095] 7.4 g of pure product was obtained, the purity was 96.3%, and the total yield was 15.3%. Molecular weight 4824.8 (100% M+H).

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Abstract

The invention relates to the field of pharmaceutical synthesis, and discloses a tiripa peptide analogue. The tiripa peptide analogue is used for preparing pharmaceutical compositions for treatment ofdiseases, use of the pharmaceutical compositions to preparation of drugs for treatment of one or more of the following diseases is disclosed, and the diseases include type II diabetes, impaired glucose tolerance, type I diabetes, obesity, hypertension, metabolic syndrome, dyslipidemia, cognitive impairment, atherosclerosis, myocardial infarction, coronary heart disease, cardiovascular disease, stroke, inflammatory bowel syndrome and / or dyspepsia or gastric ulcer, liver fibrosis diseases and pulmonary fibrosis diseases.

Description

technical field [0001] The present invention relates to a kind of analogue of tiriparatide and its use, the 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 enhance...

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
Owner CHENGDU AODA BIOTECHNOLOGY CO LTD
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