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Application of a class of glp-1r/gcgr dual agonists in hypoglycemic and weight loss drugs

A GLP-1R and dual agonist technology, applied in drug combinations, hormone peptides, pharmaceutical formulations, etc., can solve the problems of limited obesity treatment drugs, achieve convenient purification work, low production costs, and shorten the synthesis cycle.

Active Publication Date: 2020-03-31
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the treatment of obesity is mainly through surgery, and the treatment of obesity is very limited

Method used

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  • Application of a class of glp-1r/gcgr dual agonists in hypoglycemic and weight loss drugs
  • Application of a class of glp-1r/gcgr dual agonists in hypoglycemic and weight loss drugs
  • Application of a class of glp-1r/gcgr dual agonists in hypoglycemic and weight loss drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys- Cys -Leu-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr-NH 2 (SEQ.ID NO: 1) microwave-facilitated solid-phase synthesis

[0043] (1) Swelling of the resin

[0044] Weigh 50 mg of Fmoc-Rink amide-MBHA Resin (substitution amount 0.4 mmol / g), swell with 7 mL of DCM for 30 min, filter to remove DCM, then swell with 10 mL of NMP for 30 min, and finally rinse with NMP, DCM, and 7 mL of NMP respectively.

[0045] (2) Microwave promotes removal of Fmoc protecting group

[0046] Put the swollen resin into the reactor, add 7mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT, react in the microwave reactor for 1min, the microwave power is 15W, and the reaction temperature is controlled at 50°C Within the time period, use an air compressor to compress the air to cool, and filter the solution after the reaction; add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBT and react in a microwave reacto...

Embodiment 2～22

[0059]According to the method described in Example 1, the glucagon-related GLP-1R / GCGR dual agonist polypeptides of Examples 2-22 were synthesized according to the corresponding sequences, and their molecular weights were confirmed by electrospray mass spectrometry (ESI-MS).

Embodiment 2

[0061] His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr- Cys -Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr-NH2 (SEQ.ID NO: 2);

[0062] The theoretical relative molecular mass is 3471.7. ESI-MS m / z: found[M+3H] 3+ 1158.0, [M+4H] 4+ 868.6; calcu[M+3H] 3+ 1158.2, [M+4H] 4+ 868.9.

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Abstract

The invention relates to the field of medicines related to diabetes and obesity, and in particular to GLP-1R / GCGR dual agonist related to glucagon (Glu), a preparation method of the GLP-1R / GCGR dual agonist, a medicinal composition with the compound as an active component, and application of the GLP-1R / GCGR dual agonist and the medicinal composition in preparation of medicines for treating diabetes and obesity.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of a class of glucagon-related GLP-1R / GCGR dual agonists for preparation of hypoglycemic and weight-loss drugs. Background technique [0002] Obesity is an important risk factor for type 2 diabetes, hyperlipidemia and hypertension. One-third of the world's population is currently overweight or obese, and this is expected to increase to 500 million by 2025. At present, the treatment of obesity is mainly through surgery, and the treatment drugs for obesity are very limited. [0003] The proglucagon gene is located on the long arm of chromosome 2 and consists of 6 exons and 5 introns. It is expressed in the pancreas and intestinal L cells and produces proglucagon consisting of 160 amino acids ( proglucagon, PG). Proglucagon is cleaved and transformed into different products in the pancreas and gut. PG is mainly cracked in the intestine into: glucagon (Glicentin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/605C07K1/06C07K1/04A61K38/26A61P3/10A61P3/04
CPCA61K38/00C07K14/605
Inventor 黄文龙钱海周洁戴雨轩孙李丹
Owner CHINA PHARM UNIV
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