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A class of long-acting glucagon-like peptide-1 (glp-1) analogs and their applications

A technology for glucagon and analogues, applied in the field of long-acting glucagon-like peptide-1 analogues, which can solve problems such as prolonging the half-life of GLP-1, achieve stable chemical properties, and avoid local itching

Active Publication Date: 2021-03-09
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 eliminated by rapid renal filtration, 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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  • A class of long-acting glucagon-like peptide-1 (glp-1) analogs and their applications
  • A class of long-acting glucagon-like peptide-1 (glp-1) analogs and their applications
  • A class of long-acting glucagon-like peptide-1 (glp-1) analogs and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066]

[0067] solid-phase synthesis.

[0068] 1. Synthesis of cysteine-modified polypeptide chain

[0069] 1.1. Resin swelling

[0070] 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.

[0071] 1.2. Removal of Fmoc protecting group

[0072] 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.

[0073] 1.3. Synthesis of Fmoc-Arg(pbf)-Rink amide-MBHA Resin

[0074] Fmoc-Arg(pbf)-OH (32.0 mg, 0.04 mmol), HBTU (15.1 mg, 0.04 mmol), HOBt (5.4 mg, 0....

Embodiment 2

[0091]

[0092] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 4020.1. ESI-MS m / z: Calcd.[M+3H] 3+ 1341.0, [M+4H] 4+ 1006.0; Found[M+3H] 3+ 1341.2, [M+4H] 4+ 1006.9.

Embodiment 3

[0094]

[0095] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 3979.0. ESI-MS m / z: Calcd.[M+3H] 3+ 1327.3, [M+4H] 4+ 995.8; Found[M+3H] 3+ 1327.2, [M+4H] 4+ 995.3.

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PUM

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Abstract

The invention relates to a class of long-acting glucagon-like peptide-1 (GLP-1) analogs and a synthesis method thereof. GLP-1 analogues with longer pharmacological action time were obtained by modifying GLP-1. The synthesis of the target polypeptide was quickly realized through the solid-phase synthesis method of orthogonal protection strategy. The crude product was purified and lyophilized to obtain GLP-1 analogues. thing.

Description

technical field [0001] The invention relates to a class of long-acting glucagon-like peptide-1 (GLP-1) analogs and applications thereof. 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 property avoids The risk of hy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/605A61K38/26A61P3/10
CPCA61K38/00C07K14/605
Inventor 黄文龙钱海蔡星光孙李丹戴雨轩韩京
Owner CHINA PHARM UNIV
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