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A drug used to prevent and treat kidney stones

A pharmacy and compound technology, applied in the field of medicine, can solve the problems of high residual rate and recurrence rate of stones, and many side effects.

Active Publication Date: 2019-11-12
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method can discharge stones, it has many side effects, and the residual rate and recurrence rate of stones are very high.

Method used

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  • A drug used to prevent and treat kidney stones
  • A drug used to prevent and treat kidney stones
  • A drug used to prevent and treat kidney stones

Examples

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Effect test

Embodiment 1

[0065] Example 1: 1-(3-(2,4-dioxo-6-(pyridin-2-yl)-3,4-dihydropyrimidin-1(2H)-yl)propyl)-3-( pyrimidin-2-yl)urea (compound 1)

[0066]

[0067] Step 1. Add 6-chloropyrimidine-2,4(1H,3H)-dione (0.29g, 2.0mmol), pyridin-2-ylboronic acid (0.30g, 2.2mmol), tetra (Triphenylphosphine) palladium (29mg, 0.025mmol), K 2 CO 3 (0.33g, 2.4mmol), under the protection of nitrogen, add 1,4-dioxane (10mL), water (2mL), and react at 45°C for 4h. After the reaction was completed, the solvent was removed under reduced pressure, and the residue was dissolved in ethyl acetate and separated by silica gel column chromatography, eluted with petroleum ether / ethyl acetate 20:1 to obtain a light yellow solid 6-(pyridin-2-yl)pyrimidine - 2,4(1H,3H)-dione, which is 0.28 g of a light yellow solid, with a purity of 98% and a yield of 74%. ESI-MS: 190.05[M+H] + .

[0068] Step 2: 1,3-dibromopropane (1.00g, 5.0mmol), KHCO 3 (1.03g, 7.5.0mmol), CuI (0.095g, 0.5mmol) and toluene (50ml) were mixed toge...

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Abstract

The invention discloses a pyrimidinedione compound with a chemical formula represented by formula I, and pharmaceutically acceptable salts, prodrugs, and solvates thereof. It is shown by pharmacological tests that: the pyrimidinedione compound is capable of reducing renal calculus rate, kidney calcium content, serum urea nitrogen, and serum creatinine obviously, and increasing kidney coefficient obviously, and possesses excellent prevention and treatment effect on renal calculus.

Description

technical field [0001] The invention relates to the technical field of medicine, and the invention discloses medicines for preventing and treating kidney stones. Background technique [0002] Kidney stones refer to stones that occur in the renal calices, renal pelvis, and the junction of the renal pelvis and ureter. Most of them are located in the renal pelvis and calices, and renal parenchymal stones are rare. Plain radiographs show that there are single or multiple round, oval or obtuse triangular dense shadows in the renal area, with high and uniform density and smooth edges, but some are not smooth and mulberry-shaped . Stones in any part of the urinary system can originate in the kidney. According to the different stone components, kidney stones can be divided into calcium oxalate stones, calcium phosphate stones, uric acid (uric acid salt) stones, ammonium magnesium phosphate stones, cystine stones and purine stones. Kidney stones are caused by the imbalance of coll...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/14C07D417/14A61K31/506A61P13/12
CPCC07D401/14C07D417/14
Inventor 宋静孙治国韩光宇李海林王维
Owner MUDANJIANG MEDICAL UNIV
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