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Liver targeted medicine

A liver targeting and drug technology, applied in the field of biomedicine, can solve the problem of unpredictable connection between targeting molecules and drug molecules, and achieve the effect of improving liver targeting, improving drug targeting and high activity.

Inactive Publication Date: 2018-04-20
崔坤元
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

That is to say, before the disclosure, those skilled in the art cannot predict whether a certain unused connection method of targeting molecules and drug molecules can achieve satisfactory results

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0040] Preparation of trivalent acetylgalactosamine TBA-3

[0041] Prepare trivalent acetylgalactosamine TBA-3 with the steps in the following order, its structural formula and preparation flow chart are shown in figure 1 ,in:

[0042] (1) Preparation of compound PTT-1:

[0043]Take 10.0 g (55.8 mmol) of acetylgalactosamine hydrochloride (purchased from TCI (Shanghai) Chemical Industry Development Co., Ltd., product code: G0007), and add it to 100 mL of dichloromethane, and add 0.16 g ( 1.3mmol) of 4-dimethylaminopyridine (DMAP) and 20mL of triethylamine, after dissolving, start ice bathing; while ice bathing, add 60mL (635.2mmol) of acetic anhydride dropwise to it, after the dropwise addition, react at room temperature , after monitoring the reaction completely with thin layer chromatography (TLC); 100mL of water washes the organic layer, repeats 3 times, the organic layer is dried, evaporated to dryness under reduced pressure to obtain white solid 18.0g, and its structural...

Embodiment 2

[0062] A liver targeting drug TBA-4, its structural formula is as follows Figure 4 As shown, the drug is trivalent acetylgalactosamine and thyroxine T3 (its structural formula is as follows Figure 4 Shown, represented by compound T3) is obtained by direct connection.

[0063] The preparation steps of TBA-4 are as follows: Take 0.38g (0.21mmol) of TBA-3, dissolve it with 20mL of dimethylformamide (DMF), then add 74.2mg (0.23mmol) of HBTU and 0.12mL (0.69mmol) DIEA, stirred for 5 min; then added compound T3 (0.15 g, 0.23 mmol) dissolved in 10 mL of DMF (purchased from TCI (Shanghai) Chemical Industry Development Co., Ltd., product code: T0453), stirred overnight at room temperature to obtain a reaction Liquid A; Evaporate the reaction liquid A under reduced pressure. 3 and 25 mL of water; the organic layer was washed with anhydrous Na 2 SO 4 Dry, evaporate to dryness under reduced pressure, add 5mL methylamine ethanol solution, react at room temperature for 2h; evaporate t...

Embodiment 3

[0065] A liver targeting drug TBA-5, its structural formula is as follows Figure 4 As shown, the drug is obtained by connecting trivalent acetylgalactosamine and thyroxine T3 through a straight chain.

[0066] The preparation steps of TBA-5 are as follows: Take 0.38g (0.21mmol) of TBA-3, dissolve it with 20mL of DMF, then add 74.2mg (0.23mmol) of HBTU and 0.12mL (0.69mmol) of DIEA, stir the reaction for 5min; then add With the compound T3-1 (0.15g, 0.23mmol) dissolved in 10mL DMF, its structural formula is as follows Figure 4 shown), stirred and reacted at room temperature overnight to obtain reaction solution A; the reaction solution A was evaporated to dryness under reduced pressure. 3 and 25 mL of water; the organic layer was washed with anhydrous Na 2 SO 4 Dry, evaporate to dryness under reduced pressure, add 5mL methylamine ethanol solution, react at room temperature for 2h; evaporate the solvent under reduced pressure, and purify by silica gel column chromatography ...

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Abstract

The invention relates to the field of biological medicine, and in particular relates to liver targeted medicine. The medicine is chemical micromolecular medicine connecting galactosamine. The chemicalmicromolecular medicine is medicine for treating liver diseases or liver-related diseases. The chemical micromolecular medicine is prepared from but not limited to thyroxine T3, sorafenib, taxol, regorafenib, lamivudine, entecavir, telbivudine, statins, fibrates, niacin, bile acid sequestrants, other hepatitis virus DNA (RNA) polymerase inhibition compounds and the like. The galactosamine is tervalent acetylgalactosamine. The connection is the direct connection of the galactosamine and the chemical micromolecular medicine or the connection through linking fragments; the linking fragments comprise but not limited to carbon chains, disulfide bonds, pyrophosphate diester, cysteic acid, polypeptide and thioether or valine-citrulline. The medicine provided by the invention has the advantages that the liver targeted performance is improved; the medicine curative effect is enhanced; the toxic and side reactions on other non-targeted tissues are few.

Description

technical field [0001] The present invention relates to the field of biomedicine, and more specifically relates to a liver-targeting drug. Background technique [0002] Liver disease is a common and extremely harmful disease. Common liver diseases include hepatitis B, hepatitis A, hepatitis C, cirrhosis, fatty liver, liver cancer, alcoholic liver, etc. Most of the current clinical drugs for the treatment of liver diseases are not targeted. In addition to entering the liver, they can also enter other parts of the body, causing unnecessary side effects. Clinically approved drugs for the treatment of liver diseases or related to liver diseases, such as nucleoside (acid) drugs for the treatment of hepatitis B, drugs for the treatment of liver cancer, hepatitis C, and cirrhosis, all have unnecessary side effects due to non-targeting; Some drugs that fail in clinical trials are not because of efficacy, but because of too many side effects, making them unsuitable for clinical appl...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61K31/44A61K47/54A61P1/16A61P35/00
CPCA61K47/549A61K47/61A61P1/16A61K31/198A61K31/44
Inventor 崔坤元
Owner 崔坤元
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