Hepatitis treatment medicament

A drug, hepatitis technology, applied in the field of hepatitis treatment drugs, can solve problems such as slow onset

Inactive Publication Date: 2014-06-11
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Currently known nucleoside drugs such as lamivudine, adefovir dipivoxil, tenofovir dipivoxil

Method used

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  • Hepatitis treatment medicament
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 [[(R)-2-(6-amino-purin-9-yl)-1-methyl-ethoxy-]methyl]phosphonic acid bis(2-ethoxy)phenyl ester (I ) preparation

[0028] 144g (0.50mol) [[(R)-2-(6-amino-purin-9-yl)-1-methyl-ethoxy-]methyl]phosphonic acid, 276g (2.00mmol) o-ethoxy Base phenol and 390g of 1-methyl-2-pyrrolidone were heated to 85°C, then 63g of triethylamine was added, 309g (1.50mmol) of DCC was added, and heated and stirred at 100°C for 16 hours. After cooling, the solid was filtered off; the filtrate was concentrated under reduced pressure, separated by a silica gel (200-300 mesh) column, eluted with a mixed solvent of dichloromethane: methanol (20:1), and the required components were collected and evaporated to dryness under reduced pressure. The residue was recrystallized from ethyl acetate to obtain 35 g of I with a melting point of 110-112°C. Elemental Analysis C 25 h 27 N 5 o 6 Calculated P: C 56.92%, H 5.73%, N 13.28%, P 5.87%. Found values: C 56.72%, H 5.71%, N 13.18%, P 5.88%. ...

Embodiment 2

[0029] Example 2 [[(R)-2-(6-amino-purin-9-yl)-1-methyl-ethoxy-]methyl]phosphonic acid bis(2-ethoxy)phenyl ester salt Preparation of acid salt (I·HCl)

[0030] Dissolve 13g of I in 50ml of acetone, add diethyl ether solution of hydrogen chloride dropwise until the pH is 2-3, reflux for 10min, cool down naturally, precipitate a solid, and dry to obtain 13.3g of I·HCl with a melting point of 178-186°C. Elemental Analysis C 25 h 27 N 5 o 6 Calculated value of P·HCl: C 53.24%, H 5.54%, Cl 6.29%, N 12.42%, P 5.49%; measured value (%): C 53.31%, H 5.58%, Cl 6.19%, N 12.41%, P 5.40 %.

Embodiment 3

[0031] Embodiment 3 stability test

[0032] Determine the content of the sample according to high performance liquid chromatography (Chinese Pharmacopoeia 2000 edition two appendix V D).

[0033] Chromatographic conditions and system suitability test: amino-bonded silica gel was used as filler; acetonitrile-0.05mol / L potassium dihydrogen phosphate aqueous solution (22:78) was used as mobile phase, flow rate was 1.0ml / min, and detection wavelength was 260nm. The number of theoretical plates calculated by tenofovir disoproxil should not be less than 2000.

[0034]Determination method: Take about 25mg of the sample to be tested, weigh it accurately, put it in a 25ml measuring bottle, add mobile phase to dissolve and dilute to the mark, shake well, accurately draw 5ml, put it in a 25ml measuring bottle, add mobile phase to dilute to the mark, shake Uniform, as the test solution. Precisely measure 10 μl of the test solution, inject it into the liquid chromatograph, and record the...

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Abstract

The invention aims at providing an acyclic nucleotide derivative shown as a formula I and a non-toxic pharmaceutically acceptable salt thereof, a pharmaceutical composition which contains the acyclic nucleotide derivative shown as the formula I and the non-toxic pharmaceutically acceptable salt thereof as an active ingredient and employs common pharmaceutical excipients in the pharmacy field, and application of the pharmaceutical composition to treat hepatitis and virus hepatitis B as a medicine. The formula I is shown in the specification.

Description

technical field [0001] The present invention relates to the use of acyclic nucleotide analogs represented by formula I and their non-toxic pharmaceutically acceptable salts as medicines for treating hepatitis and viral hepatitis B: [0002] Background technique [0003] Hepatitis is a disease of liver damage caused by elevated transaminases, including liver damage caused by chemical drugs, liver damage caused by metabolic disorders, and liver damage caused by viruses such as hepatitis B virus or hepatitis C virus infection. Chronic persistent hepatitis will lead to liver fibrosis, and then further develop into cirrhosis and even liver cancer. The main goal of the treatment of hepatitis is to reduce transaminases by using drugs, inhibit the occurrence of liver inflammation, and inhibit the formation and development of liver fibrosis. Commonly used anti-hepatitis drugs mainly include silibinin, diammonium glycyrrhizinate, bifendate, and bicyclol; these drugs can effectivel...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61P31/20
Inventor 仲伯华何新华靳雪源樊士勇史卫国姚宜山贾红新
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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