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Targeting carrier suitable for anti-African swine fever virus siRNA drugs and application of targeting carrier

A technology of African swine fever virus and medicine, which is applied in antiviral agents, pharmaceutical formulas, medical preparations of non-active ingredients, etc., to achieve the effects of strong targeting, high safety, and strong affinity

Pending Publication Date: 2020-08-25
杭州濡湜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

African swine fever occurs and is endemic in many countries, but so far, there are no vaccines and drugs to prevent or treat the disease

Method used

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  • Targeting carrier suitable for anti-African swine fever virus siRNA drugs and application of targeting carrier
  • Targeting carrier suitable for anti-African swine fever virus siRNA drugs and application of targeting carrier
  • Targeting carrier suitable for anti-African swine fever virus siRNA drugs and application of targeting carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1: Acetylation of D-Mannose

[0055] At 0°C, 100 g of D-mannose in acetic anhydride (Ac 2 O) (400 milliliters) add 500 milliliters of anhydrous pyridine (Py) in the suspension liquid, logical nitrogen protection, and stir for 15 minutes; Then add 5 grams of 4-dimethylaminopyridine (DMAP) and 100 milliliters of Triethylamine (Et 3 N), stirred overnight. After the reaction was complete (reaction monitored by thin-layer chromatography), the precipitated solid was collected, washed twice with toluene and water, and dried in vacuo to obtain 160 g of fully acetylated D-mannose.

Embodiment 2

[0056]Example 2: Protection of glycosyl-linked carboxylates

[0057] Add 1 liter of anhydrous dichloroethane (DCE) to 120 grams of full acetyl-D-mannose, and protect with nitrogen gas, then slowly add 60 milliliters of trimethylsilyl trifluoromethanesulfonate (TMSOTf) dropwise, Stir at 25-30°C for 16 hours. Then the reactant was transferred to 3 liters of ice-water suspension containing 15wt% sodium bicarbonate and stirred for 1 hour, then left to stand, the organic layer was collected, the aqueous layer was extracted twice with dichloromethane (DCM), and the combined organic layer and dried over anhydrous magnesium sulfate, filtered and concentrated to dryness to obtain 105 g of product which was directly used in the next step.

[0058] 105 grams of the above product and 105 grams of benzyl 4-hydroxybutyrate were dissolved in 600 milliliters of anhydrous dichloroethane (DCE), added 80 grams of molecular sieves and stirred for 20 minutes, then added 14 milliliters of trifluor...

Embodiment 3

[0059] Example 3: Carboxylate Debenzylation

[0060] Dissolve 100 grams of the benzyl ester of Example 2 in 1 liter of methanol / tetrahydrofuran (THF) mixed solvent (methanol: tetrahydrofuran volume ratio = 1:1), pass nitrogen to remove a small amount of air in the solution, and under nitrogen protection 10 grams of 10 wt% palladium on carbon (Pd / C) was added. Then replace nitrogen with hydrogen three times, and stir overnight at 25-30°C under hydrogen. The reactant was filtered through palladium carbon with celite and washed with methanol, and the filtrate was collected and concentrated to dryness to obtain 87 g of product.

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PUM

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Abstract

The invention discloses a targeting carrier suitable for anti-African swine fever virus siRNA drugs. The targeting carrier comprises a polyvalent carbohydrate chain and a linker, wherein a carbohydrate unit at the tail end of the carbohydrate chain is D-mannose that can be recognized by a mannose receptor; the linker is used for connecting the polyvalent carbohydrate chain and the anti-African swine fever virus siRNA drug, and at least one carboxyl group and at least one hydroxy group are arranged at the tail end of the linker, and are correspondingly used for connecting the polyvalent carbohydrate chain and the anti-African swine fever virus siRNA drug. The targeting carrier provided by the invention is a novel mannose receptor carrier, can be combined with the siRNA drug special for resisting African swine fever viruses, recognize the mannose receptors of macrophage or dendritic cells in a targeted mode, and enters the cells through endocytosis, so that the treatment effect of the drug is improved and toxic and side effects on other tissues are reduced, the targeting effect is strong, and the safety is high. In the cells, the siRNA drug can inhibit the expression of a target gene, so that the target gene is silent, and thus the purpose of killing the viruses is achieved.

Description

technical field [0001] The invention relates to the technical field of drug targeting carriers, in particular to a targeting carrier suitable for anti-African swine fever virus siRNA drugs and its application. Background technique [0002] Receptor is a macromolecular substance that can recognize and selectively bind certain molecules. Receptor-mediated endocytosis is an important way for most animal cells to capture biological macromolecules from extracellular fluid. Most of the drugs enter the cells and change the physiological and biochemical functions of the cells to produce effects. Generally, traditional drugs do not have active targeting. While treating diseases, they will have certain toxic and side effects, and even some adverse reactions. The research and application of drug-targeted carriers can make up for these shortcomings. It can concentrate the drug on the target cells to maximize the drug's effect, and at the same time reduce the toxicity of the drug to nor...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K31/713A61P31/20
CPCA61K47/549A61K47/545A61K31/713A61P31/20
Inventor 王喆明
Owner 杭州濡湜生物科技有限公司
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