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Drug benzophenoxazines compound for treating cataract and preparation method thereof

A technology of benzophenoxazines and compounds, applied in the application field of pharmaceutical compositions in cataract diseases, can solve problems such as the reversal of cataract processes, and achieve the effects of strong affinity, increased reaction yield, and high yield

Inactive Publication Date: 2018-09-21
RIZHAO PUDA PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] While many medications are available to treat cataracts, none can reverse the progression of cataracts

Method used

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  • Drug benzophenoxazines compound for treating cataract and preparation method thereof
  • Drug benzophenoxazines compound for treating cataract and preparation method thereof
  • Drug benzophenoxazines compound for treating cataract and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Preparation of 1-methoxy-5-oxo-9-amino-5H-pyrido-[3,2-a]-phenoxazine-3-carboxylic acid.

[0059]

[0060] The synthesis steps are:

[0061] In the first step, pure water (50ml), 4-methoxy-2-methylpyridine compound (1) (10g) and succinic anhydride (8g) are added to a three-necked flask equipped with a stirrer, thermometer and condenser. ), after the water bath is heated to 80°C, add potassium permanganate (total 6g) in three batches, keep the temperature at 84°C, the potassium permanganate to be added has reacted completely, and the solution in the reaction flask is dark brown without purple , Then add the next batch of potassium permanganate, and proceed in this way. After all the potassium permanganate has been reacted, keep stirring at 82°C for at least 45 minutes, filter while hot to remove manganese dioxide, and wash twice with hot distilled water. Manganese oxide until the filtrate is a colorless and transparent solution to obtain a solution containing potassium 1-meth...

Embodiment 2

[0068] Preparation of 1-methoxy-5-oxo-9-chloro-5H-pyrido-[3,2-a]-phenoxazine-3-carboxylic acid.

[0069]

[0070] The synthesis steps are:

[0071] In the first step, pure water (50ml), 4-methoxy-2-methylpyridine compound (1) (15g) and succinic anhydride (8.9) are added to a three-necked flask equipped with a stirrer, thermometer and condenser. g) After the water bath is heated to 80°C, add potassium permanganate (8g in total) in three batches, keep the temperature at 80°C, the potassium permanganate to be added has reacted completely, and the solution in the reaction flask is dark brown without purple When the time, add the next batch of potassium permanganate, and proceed in this way. After all the potassium permanganate has reacted, keep stirring at 82°C for at least 45 minutes, filter while hot to remove manganese dioxide, and wash with hot distilled water several times Manganese dioxide, until the filtrate is a colorless and transparent solution, a solution containing potassi...

Embodiment 3

[0078] The compound of Example 3 1-methoxy-5-oxo-9-carboxy-5H-pyrido-[3,2-a]-phenoxazine-3-carboxylic acid.

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PUM

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Abstract

The invention provides a drug benzophenoxazines compound for treating cataract and a preparation method thereof. The chemical structural formula of the drug benzophenoxazines compound for treating thecataract is shown in the description. The provided drug benzophenoxazines compound is a mydriasis drug, is similar to a xanthommatin compound, can have stronger affinity with a crystalline lens soluble protein, can competitively inhibit the oxidation, degeneration and turbidity functions of quinoid substances on the crystalline lens soluble protein, prevent the development of the cataract, have good therapeutic effects on senile cataract, cataract caused by diabetes, traumatic and congenital cataract and retinitis pigmentosa, and can be used for further study and development of cataract diseases.

Description

Technical field [0001] The present invention relates to the technical field of medicine. Specifically, the present invention relates to a benzophenoxazine compound for the treatment of cataracts and a preparation method thereof, and also relates to a pharmaceutical composition prepared from a benzophenoxazine compound in cataract diseases application. Background technique [0002] Cataract is a common eye disease, including age-related cataract, traumatic cataract, mild diabetic cataract, concurrent cataract and congenital cataract. It is a disease that can cause blindness in patients. There are many factors that cause cataracts, mainly It is related to nutrient metabolism, sunlight and ultraviolet rays, external temperature, hypoxia, endocrine disorders, dehydration in the human body, etc., such as aging, genetics, metabolic abnormalities, trauma, radiation, poisoning, and local malnutrition, etc., can cause lens capsule Injury or lead to lens metabolism disorder, resulting in ...

Claims

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Application Information

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IPC IPC(8): C07D498/04A61K31/5383A61P27/12
CPCA61P27/12C07D498/04
Inventor 不公告发明人
Owner RIZHAO PUDA PHARMA TECH CO LTD
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