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A kind of medicine for preventing and treating diabetic retinopathy and preparation method thereof

A diabetes and drug technology, applied in the direction of drug combination, pharmaceutical formula, urinary system diseases, etc., can solve the problem of prolonging the effective vision of patients

Inactive Publication Date: 2018-11-13
佳木斯大学附属第一医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these treatments only prolong the patient's effective visual acuity and have no significant impact on the overall course of retinopathy

Method used

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  • A kind of medicine for preventing and treating diabetic retinopathy and preparation method thereof
  • A kind of medicine for preventing and treating diabetic retinopathy and preparation method thereof
  • A kind of medicine for preventing and treating diabetic retinopathy and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Example 1: Preparation of 1-(3'-fluorobiphenyl-4-yl)-4-(3-(4-methylthiophen-3-yl)propyl)piperazine (compound 1)

[0072]

[0073] Step 1. Dissolve 10.0 mmol of 3-(4-methylthiophen-3-yl)propan-1-ol in 100 mL of chloroform, and add 3 mL of triethylamine and 12.0 mmol of p-toluenesulfonyl chloride to it in sequence. After stirring the reaction at room temperature for 4 hours, 200 mL of water was added to quench. The organic phase was separated, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure, and the resulting residue was purified by silica gel column chromatography (cyclohexane / ethyl acetate (v / v)=3 / 1) to obtain 3-(4 -Methylthiophen-3-yl)propyl p-toluenesulfonate 2.54 g (82.1%).

[0074] Under nitrogen protection, 3-(4-methylthiophen-3-yl)propyl p-toluenesulfonate 6.0mmol, 1-(3'-fluorobiphenyl-4-yl)piperazine 5.0mol, sodium carbonate 15.0 mol and 0.4 mol of potassium iodide were added to 80 mL of acetonitrile, stirred and reacte...

Embodiment 2

[0077] Example 2: Preparation of 5-cyclobutyl-2-(4-(3-(5-dichloromethyl-thiophen-3-yl)-3-methylpiperazin-1-yl)pyrimidine (compound 2)

[0078]

[0079] Step 1. Dissolve 10.0 mmol of 3-(5-dichloromethyl-thiophen-3-yl)propan-1-ol in 100 mL of chloroform, and add 3 mL of triethylamine and 12.0 mmol of p-toluenesulfonyl chloride to it in sequence. After stirring the reaction at room temperature for 4 hours, 200 mL of water was added to quench. The organic phase was separated, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure, and the resulting residue was purified by silica gel column chromatography (cyclohexane / ethyl acetate (v / v)=4 / 1) to obtain 3-(5 -Dichloromethyl-thiophen-3-yl)propyl p-toluenesulfonate 3.19 g (84.3%).

[0080] Under nitrogen protection, 3-(5-dichloromethyl-thiophen-3-yl)propyl p-toluenesulfonate 6.0mmol, 5-cyclobutyl-2-(3-methyl-pipera-1- Base) 5.0 mol of pyrimidine, 15.0 mol of sodium carbonate and 0.4 mol of potassiu...

Embodiment 13

[0086] Embodiment 13: detection of aldose reductase activity

[0087] Refer to the literature method (Bovine lens aldehyde reductase (aldose reductase). Purification, kinetics and mechanism, A B, Halder; M J, Crabbe, The Biochemical journal, 1984, volume 219, phase 1, 33-39)

[0088] Take the rat lens and place it in homogenization buffer (135mM KH 2 PO 4 -NaH 2 PO 4 , 120mM Li 2 SO 4 , pH7.0), homogenate at 10000g, centrifuge at 40C for 20min, absorb the supernatant, and obtain the enzyme crude extract. Enzyme activity and sample activity detection methods are as follows, add buffer (0.1M KH 2 PO 4 , pH7.0), an appropriate amount of enzyme and the sample to be tested, mix well, measure the background OD value of the drug at 340nm (recorded as OD0 value), then add 0.15mM NADPH and 5mMDL-glyceraldehyde at 37°C for 10min , 20min, 340nm measured OD value (denoted as OD1 value), calculated inhibition rate and IC 50 . When measuring the activity, the sample with a concent...

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PUM

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Abstract

The invention relates to a novel compound with excellent inhibition effect on aldose reductase. The effect of the novel compound is even better than that of conventional aldose reductase inhibitors. The novel compound possesses excellent prevention and treatment effects on diabetic syndromes such as diabetic cardiovascular and cerebrovascular diseases, diabetic nephropathy, diabetic neuropathy, and especially diabetic retinopathy.

Description

technical field [0001] The invention relates to the field of medicines, in particular, the invention relates to a medicine for preventing and treating diabetic complications, especially diabetic retinopathy and a preparation method thereof. Background technique [0002] Diabetes mellitus is a metabolic disease of multiple etiologies characterized by chronic hyperglycemia with disturbances in carbohydrate, fat and protein metabolism due to defects in insulin secretion. Diabetes has been listed as the third major disease after cardiovascular disease and tumor in developed countries. [0003] The treatment of diabetes itself can be well managed by controlling the level of blood sugar in the patient's body. However, during the long-term treatment of diabetes, patients often develop some so-called long-term complications, ie diabetic complications. [0004] Diabetic retinopathy (DR) is the most common and serious microvascular complication of diabetes, and has become one of the...

Claims

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Application Information

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IPC IPC(8): C07D333/20C07D409/14C07D409/12C07D333/38A61K31/496A61K31/506A61K31/4439A61K31/551A61P3/10A61P9/10A61P13/12A61P25/00A61P27/02
CPCC07D333/20C07D333/38C07D409/12C07D409/14
Inventor 刘宏伟孟岩周萍萍
Owner 佳木斯大学附属第一医院
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