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Long-effecting exenatide (Exendin-4) analogue and application thereof

A technology of exenatide and analogs, applied in the direction of medical preparations containing active ingredients, specific peptides, hormone peptides, etc., can solve the problems of prolonging the half-life of GLP-1, achieve stable chemical properties, and avoid local itching

Active Publication Date: 2017-09-08
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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  • Long-effecting exenatide (Exendin-4) analogue and application thereof
  • Long-effecting exenatide (Exendin-4) analogue and application thereof
  • Long-effecting exenatide (Exendin-4) analogue and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064]

[0065] solid-phase synthesis.

[0066] 1. Synthesis of cysteine-modified polypeptide chain

[0067] 1.1. Resin swelling

[0068] Weigh 50 mg of Fmoc-Rink amide-MBHA Resin (degree of substitution 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.

[0069] 1.2. Removal of Fmoc protecting group

[0070] 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.

[0071] 1.3. Synthesis of Fmoc-Ser(tBu)-Rink amide-MBHA Resin

[0072] Fmoc-Ser(tBu)-OH (15.3 mg, 0.04 mmol), HBTU (15.1 mg, 0.04 mmol), HOBt (5.4 mg, 0.04 mmo...

Embodiment 2

[0089]

[0090] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 5009.2. ESI-MS m / z: Calcd.[M+3H] 3+ 1670.7, [M+4H] 4+ 1253.3; Found[M+3H] 3+ 1670.4, [M+4H] 4+ 1253.2.

Embodiment 3

[0092]

[0093] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 4996.1. ESI-MS m / z: Calcd.[M+3H] 3+ 1666.4, [M+4H] 4+ 1250.0; Found[M+3H] 3+ 1666.6, [M+4H] 4+ 1250.1.

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PUM

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Abstract

The invention relates to a long-effecting exenatide (Exendin-4) analogue and a synthetic method thereof. The Exendin-4 is modified to obtain the Exendin-4 analogue with longer pharmacologic action time, the synthesis of target polypeptide is quickly realized through an orthogonally protection strategy solid-phase synthesis method, and a crude product is purified and freeze-dried to obtain the Exendin-4 analogue.

Description

technical field [0001] The invention relates to a class of long-acting exenatide (Exendin-4) analogs in the field of diabetes treatment 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 hypoglycemic 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 proper...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/575A61K38/22A61P3/10
CPCA61K38/00C07K14/57563
Inventor 黄文龙钱海蔡星光戴雨轩孙李丹刘春霞毕昕洲
Owner CHINA PHARM UNIV
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