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Novel application of benzopyran derivative in preparation of drug for treating hyperuricaemia

A benzopyran derivative, a technology for hyperuricemia, applied in the field of pharmaceutical compositions for treating hyperuricemia and gout, can solve problems such as large toxic and side effects, achieve no toxic and side effects, reduce serum uric acid levels, The effect of high safety

Inactive Publication Date: 2016-02-10
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But above-mentioned medicine toxic and side effects are big, for example allopurinol can cause severe toxic and side effects such as allergic reaction (incidence rate 10-15%), hypersensitivity syndrome (27.5% maculopapular patient's death), myelosuppression; Probenecid, phenyl bromide Malone has side effects such as gastrointestinal reactions, renal colic, and acute attacks of gout, which limits the clinical application of these drugs to a certain extent

Method used

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  • Novel application of benzopyran derivative in preparation of drug for treating hyperuricaemia
  • Novel application of benzopyran derivative in preparation of drug for treating hyperuricaemia
  • Novel application of benzopyran derivative in preparation of drug for treating hyperuricaemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Embodiment 1: Preparation and characterization of compound 4 of the present invention

[0103] Dissolve compound 3 in distilled water, prepare a solution with a mass percent concentration of 3%, adjust the pH of the solution to 4.0-6.0, put the reaction solution into an autoclave, and react at 120-130°C for 40-60 minute. After the reaction solution is cooled to room temperature, it is separated by D101 macroporous adsorption resin, eluted with distilled water and 70% ethanol in sequence, the eluate is concentrated and left to crystallize, and the collected crystal is compound 4 of the present invention, which is detected and characterized as follows:

[0104] 1 HNMR (DMSO-d 6 , 400MHz) δ: 11.90(1H, s), 10.78(1H, s), 6.16(1H, d, J=5.1Hz), 5.27(1H, brs), 4.02(1H, brd), 5.90(1H, brs ), 5.85 (1H, brs), 6.44 (2H, s), 8.20 (1H, brs); 13 C-NMR (DMSO-d 6 , 100MHz) δppm: 81.1, 71.0, 195.6, 163.9, 95.8, 166.7, 94.9, 162.7, 100.3, 126.1, 106.6, 145.5, 132.9. It can be seen ...

Embodiment 2

[0105] Embodiment 2: Preparation and characterization of compound 13 of the present invention

[0106] Dissolve compound 3 (500 mg) in 50 ml of ethanol, stir and add 200 mg of NaBH4, react at room temperature for 1 hour. Immediately after the reaction was completed, 50ml of 0.1N hydrochloric acid and 150ml of water were added, and the mixture was extracted with 150ml of ethyl acetate. The organic phase was evaporated to dryness, the residue was dissolved in an appropriate amount of water, and then separated on an ODS reversed-phase silica gel column, and gradient elution was carried out with ethanol-water, and the compound 13 of the present invention was isolated, and its detection and characterization data were as follows:

[0107] 1 H-NMR (DMSO-d 6 , 400MHz) δppm: 4.45 (1H, dd, J = 11.0, 3.5Hz), 4.56 (1H, dd, J = 11.0, 3.5Hz), 4.92 (1H, d, J = 11.0Hz), 5.88 (1H, d , J=1.2Hz), 5.92(1H, d, J=1.2Hz), 6.42(2H, s), 11.90(1H, s); 13 C-NMR (DMSO-d 6 , 100MHz) δppm: 72.34, 74.3...

Embodiment 3

[0108] Example 3: Extraction and characterization of compounds 7, 8, and 10 of the present invention

[0109] Take 1 kg of young leaves of vine tea (Ampelopsis grossedentata), and extract with 8 times the amount of 70% ethanol under reflux. The extract was concentrated to dryness in vacuo, the residue was suspended in water, and extracted with petroleum ether, ethyl acetate, and n-butanol in sequence. The ethyl acetate extract was separated by column chromatography repeatedly with forward silica gel, the eluent was chloroform-methanol system, the eluent was concentrated, and then further separated with ODS reversed-phase silica gel, and the gradient was carried out with ethanol-water as the eluent After elution, compound 7, compound 8 and compound 10 of the present invention can be obtained respectively; the detection and characterization data are as follows:

[0110] Compound 7: 1 H-NMR (DMSO-d 6 , 400MHz) δppm: 4.40 (1H, d, J = 11.0Hz), 4.92 (1H, d, J = 11.0Hz), 5.88 (1H,...

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PUM

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Abstract

The invention discloses an application of a benzopyran derivative represented as the formula (I) and a pharmaceutically acceptable salt thereof in preparation of drugs for treating hyperuricaemia. The benzopyran derivative not only has strong in-vitro inhibition effect on xanthine oxidase but also can significantly reduce the serum uric acid level of mice suffered from the hyperuricaemia. The benzopyran derivative has dose-dependent, is free of toxic and side effects, is good in safety and can be used as a potential xanthine oxidase inhibitor and a uric acid reducing medicine for treating the hyperuricaemia and gout or gout complications caused by the hyperuricaemia.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to the application of a benzopyran derivative and a pharmaceutically acceptable salt thereof in the preparation of a medicine for treating hyperuricemia, and a medicine for treating hyperuricemia and gout combination. Background technique [0002] In recent years, due to the increase in people's stress and the increase in intake of high-calorie, high-protein, and high-fat foods, the number of people suffering from hyperuricemia or gout symptoms caused by it has increased sharply. It is reported that about 20% of Adult males are in a state of hyperuricemia. [0003] In general, a state in which the uric acid level in the blood is 7.0 mg / dL or more is called hyperuricemia. Usually, a simple hyperuricemia state has no subjective symptoms, but if this state is left alone for a long time, urate in the blood crystallizes, and when this urate accumulates in joints, etc., it ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61K31/353A61P19/06A61P13/12A61P9/00A61P13/04
CPCA61K31/353A61K31/7048
Inventor 温尧林夏增华刘建南陈佳玲徐海霞
Owner CATCH BIO SCI & TECH
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