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Glucagon-like peptide-1(GLP-1) analogue with ether bond and application thereof

A technology of glucagon and analogs, applied in glucagon, medical preparations containing active ingredients, hormone peptides, etc., can solve problems such as prolonging the half-life of GLP-1, and achieve strong GLP-1 receptor stimulation Active, avoiding local itching, reducing pain

Active Publication Date: 2017-10-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since GLP-1 is rapidly filtered and eliminated by the kidneys, resistance to degradation by DPP-IV enzymes can only prolong the half-life of GLP-1 to a certain extent

Method used

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  • Glucagon-like peptide-1(GLP-1) analogue with ether bond and application thereof
  • Glucagon-like peptide-1(GLP-1) analogue with ether bond and application thereof
  • Glucagon-like peptide-1(GLP-1) analogue with ether bond and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062]

[0063] solid-phase synthesis.

[0064] 1. Synthesis of cysteine-modified polypeptide chain

[0065] 1.1. Resin swelling

[0066] Weigh 50mg of Fmoc-Rink amide-MBHA Resin (degree of substitution 0.4mmol / g), swell with 7mL of DCM for 30min, filter to remove DCM, then swell with 10mL of NMP for 30min, and finally rinse with NMP, DCM, and 7mL of NMP respectively.

[0067] 1.2. Removal of Fmoc protecting group

[0068] Put the swollen resin into the reactor, add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBt, react for 1 min, and filter off the solution after completion; then add 25% piperidine containing 0.1M HOBt Pyridine / NMP (V / V) solution 7mL, reacted for 4min, filtered off the solution after completion, washed with NMP. A resin free of the initially attached Fmoc protecting group is obtained.

[0069] 1.3. Synthesis of Fmoc-Arg(pbf)-Rink amide-MBHA Resin

[0070] Fmoc-Arg(pbf)-OH (32.0 mg, 0.04 mmol), HBTU (15.1 mg, 0.04 mmol), HOBt (5.4 mg, 0....

Embodiment 2

[0093]

[0094] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 4039.1. ESI-MS m / z: Calcd.[M+3H] 3+ 1347.4, [M+4H] 4+ 1010.8; Found[M+3H] 3+ 1347.6, [M+4H] 4+ 1010.7.

Embodiment 3

[0096]

[0097] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 3998.0. ESI-MS m / z: Calcd.[M+3H] 3+ 1333.7, [M+4H] 4+ 1000.5; Found[M+3H] 3+ 1333.6, [M+4H] 4+ 1000.3.

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PUM

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Abstract

The invention relates to a long-acting glucagon-like peptide-1(GLP-1) analogue and a synthetic method thereof. The GLP-1 analogue with longer pharmacological action time is obtained through modifying GLP-1; the synthesis of target polypeptides is rapidly realized by an orthogonal protection strategy solid-phase synthesis method; a crude product is purified and freeze-dried to obtain the GLP-1 analogue.

Description

technical field [0001] The present invention relates to a glucagon-like peptide-1 (GLP-1) analog with ether bond and its application in the field of diabetes treatment. Background technique [0002] Diabetes is the third chronic non-communicable disease that seriously threatens human health after tumors and cardiovascular diseases. Currently, there are about 300 million diabetics in the world, which is expected to increase to 500 million by 2025. Clinically, intensive insulin therapy is used to delay the progression of diabetes, but insulin injections have the risk of hypoglycemia. The therapeutic effect is affected by factors such as dose, injection site, and injection route, and there are large individual differences. If insulin is used carelessly, severe hypoglycemia side effects will occur. [0003] Glucagon-like peptide-1 (GLP-1) is a glucose-dependent incretin hormone. GLP-1 stimulates insulin secretion without hypoglycemia. This glucose-dependent insulin-stimulating...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605A61K38/26A61P3/10C07K1/04C07K1/06C07K1/107
CPCA61K38/00C07K14/605
Inventor 黄文龙钱海蔡星光戴雨轩孙李丹韩京
Owner CHINA PHARM UNIV
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