A kind of styrene acid compound, its composition and its application

A technology of styrene acid and composition, which is applied in the field of styrene acid compounds, can solve the problems of diabetic eye disease research, increase the risk of drug use, increase the frequency of drug administration, etc., achieve improvement of optic neuropathy or choroidal lesions, prolong the action time, improve The effect of permeability

Active Publication Date: 2018-11-02
DONGGUAN ANHAO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the published literature or patents only involve the use of styrene acid compounds in the treatment of fundus angiogenesis, and no further research has been carried out on diabetic eye disease, and it was found in follow-up studies that these disclosed styrene acid The time is short, and the frequency of dosing needs to be increased to increase the risk of medication

Method used

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  • A kind of styrene acid compound, its composition and its application
  • A kind of styrene acid compound, its composition and its application
  • A kind of styrene acid compound, its composition and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: (E)-3-(3'-Hydroxy-4'-methoxyphenyl)-2-(3", 4", 5"-trimethoxyphenyl) 2-n-butylammonium acrylate salt preparation

[0044] Mix 3,4,5-trimethoxyphenylacetic acid (610mmol), 3-hydroxy-4 methoxybenzaldehyde (724mmol), acetic anhydride (200mmol) and triethylamine (717mmol), stir and reflux at 150°C for 2.5 h, distill the solvent off under reduced pressure, add a sufficient amount of 1N hydrochloric acid (about 300ml), stir at room temperature overnight, filter the resulting solid and recrystallize it with ethanol to obtain (E)-3-(3'-hydroxy-4'-methoxy Phenylphenyl)-2-(3”, 4”, 5”-trimethoxyphenyl) 2-acrylic acid. Dissolve the obtained phenylacrylic acid derivative in acetone (about 30ml), and drop it under the protection of argon at 0℃ Add an equivalent amount of n-butylamine acetone solution, heat up to 20°C and react for 1h, concentrate under reduced pressure to remove the solvent, add ethyl acetate (about 30ml), heat to 80°C for reflux, then cool to 0°C, filter ...

Embodiment 2

[0046] Example 2: Effects of phenylacrylic acid compounds on neovascularization in rats with diabetic retinopathy

[0047] Experimental animals: 180 healthy male Wistar rats aged 6 weeks, weighing 180-220 g. The feeding conditions are stored at room temperature 18-25° C., air circulation, relative humidity 55-75%, and 12-hour light maintenance.

[0048] Modeling method: above normal adult male Wistar rats, the lenses of both eyes are completely transparent without any turbidity. After feeding for one week, the body weight was measured after fasting for 12 hours. Streptozotocin (purchased from Laibo Bio-Experimental Materials Research Institute) was dissolved in 0.1ml / L, pH4.2 in citric acid buffer solution to prepare 1% streptozotocin solution, the experimental group was 60mg / L One-time intraperitoneal injection of the above solution with a body weight of kg, followed by adequate drinking water and food, induced diabetic retinopathy for modeling. The normal control group wa...

Embodiment 3

[0072] Example 3: Study on drug action time based on the effect of phenylacrylic acid compounds on the neovascularization of rat diabetic retinopathy

[0073] The test was repeated according to the method of Example 2, only the administration method was replaced by each group adopting administration once every two days. The normal control group and the experimental control group were intraocularly injected with 1.0 μL of phosphate buffer solution every two days, and the treatment groups A-F were intraocularly injected with 1.0 μL of drug solution every two days, with a drug concentration of 1.0 μg / μL.

[0074] test results:

[0075] 1) Immunization result:

[0076] In the normal control group, there was no positive expression of vascular endothelial growth factor (ie, VEGF) and fibroblast production chair (ie, bFGF), and the retinal cells were arranged neatly, and the cell morphology was normal; in the test control group, VEGF and bFGF were strongly positive in the whole laye...

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PUM

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Abstract

The invention relates to a cinnamic acid compound of which the structure is as shown in the formula (I), wherein R1, R2, R3, R4 and R5 are separately selected from a group consisting of hydrogen, hydroxyl and methoxy, and R6 is a linear chain alkyl group with 3-6 carbon atoms. The invention further relates to a medical composition which comprises a styrene acid compound, organic carboxylic acid, a pH-regulating agent and one or more optional auxiliary materials which are pharmaceutically acceptable, and the pH value of the medical composition is 6-8. The styrene acid compound accounts for 0.05-1.00wt% of the medical composition, and the organic carboxylic acid accounts for 0.01-0.50wt% of the medical composition. The invention further relates to the application of the cinnamic acid compound and the medical composition for preparing medicines for preventing and / or treating eye diseases caused by diabetes.

Description

technical field [0001] The present invention relates to a styrene acid compound, its composition and its application, in particular to its application in the preparation of medicines for preventing and / or treating diabetic eye disease. Background technique [0002] Diabetes is an endocrine and metabolic disease with hyperglycemia as the main symptom, and its prevalence is increasing year by year with the improvement of people's living standards and changes in diet structure. Diabetes can affect every organ in the body, but it is more closely related to the eyes, which can cause cataracts, retinopathy, glaucoma, temporary refractive errors, and extraocular muscle paralysis. [0003] Diabetic eye disease is one of the most common chronic complications of diabetes. It can cause vision loss in patients and eventually lead to blindness. The blindness rate is 25 times that of normal people. According to domestic reports, the rate of fundus change is 38%-39% for those with a disea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C59/64C07C51/41C07C209/00C07C211/07A61K31/205A61P27/02A61P27/06A61P27/12A61P27/14
Inventor 雍智全
Owner DONGGUAN ANHAO PHARMA CO LTD
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