Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF9 Cites 7 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • GIP/GLP-1 analogue
  • GIP/GLP-1 analogue
  • GIP/GLP-1 analogue

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).

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products