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Uses of hydroxybenzophenone in preparation of antiviral and antitumor drugs

a technology of hydroxybenzophenone and antiviral and antitumor drugs, which is applied in the direction of drug compositions, viruses/bacteriophages, and dsdna viruses, can solve the problems of lack of effective drugs for treating genital warts, significant differences in structure of hydroxybenzophenone, and increase the risk of suffering from alzheimer's disease in individuals, so as to prevent the recurrence of viral infection and high antiviral and antitumor activity

Inactive Publication Date: 2018-01-25
GUANGZHOU JIECHENG BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent aims to discover a group of compounds that have excellent antiviral and antitumor activity, specifically against herpes virus, human papillomavirus (HPV), and HIV. These compounds also inhibit the action of the viral integrase protein, which prevents the viruses from getting into the host cell's chromosome and causing recurring infections. The patent is useful for creating drugs to treat various viral diseases such as herpes, AIDS, genital warts, and can also help prevent cancer caused by high-risk HPV.

Problems solved by technology

However, they are significantly different from the hydroxybenzophenone in structures.
In two study reports published in the international magazine Alzheimer's & Dementia on Oct. 22, 2014, the researchers from Umea University in Sweden find that the infection of herpes simplex virus may increase the risk of suffering from the Alzheimer's disease for individuals.
Currently, there is relatively a lack of effective drugs for treating genital warts and cervical erosion, because some drugs such as podophyllotoxin d have the problem of being very irritating and generating great toxic side effects, despite the advantage of short treatment course.
But these drugs cannot eradicate the virus integrated into the human cells, so the infection lasts for a long time and is unhealed, and finally transforms into a malignant tumor.
Malignant tumors are a serious threat to human health and life.
At present, chemotherapy drugs for the clinical application are relatively very toxic, and have poor effects on solid tumors, and the vast majority of patients receiving chemotherapy eventually died of tumor cell metastasis.
But 3,4,5-trihydroxybenzoic acid is known to be unstable in human environmental conditions.

Method used

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  • Uses of hydroxybenzophenone in preparation of antiviral and antitumor drugs

Examples

Experimental program
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Effect test

example 1

Preparation of Anti-HPV Microemulsion

[0067]20 ml 1,2-propylene glycol, 15 ml Tween 80 and 5 ml ketone are mixed and added with sterilized distilled water to a total volume of 100 ml, so as to obtain an external preparation solution. 10 g 2,4,2′,4′-tetrahydroxybenzophenone is added to 50 ml of the external preparation solution, the pH thereof is adjusted to 5.5, and then the solution is added with the external preparation solution to 100 ml, so as to obtain 10% anti-HPV microemulsion of the present invention.

example 2 preparation

of Anti-HPV 2,3,4,2′,4′,5-hexahydroxybenzophenone Injection

[0068]10 g 2,3,4,2′,4′,5-hexahydroxybenzophenone, 8.5 g sodium chloride, 10 ml 1,2-propanediol and 80 ml Tween 80 are mixed and added with the sterilized distilled water to be dissolved, then added with the sterilized distilled water to 100 ml, the pH is adjusted to 7.4, and then the solution is filtered, potted and sterilized at 100° C. for 30 mins. Consequently, 2,3,4,2′,4′,5-hexahydroxybenzophenone injection is obtained.

example 3

Preparation of 2,3,4,2′,4′,5-hexahydroxybenzophenone Compound Effervescent Tablets

[0069]0.25 g 2,3,4,2′,4′,5-hexahydroxybenzophenone, 0.01 g polyinoside and 0.45 g tartaric acid are screened separately by 80 mesh sieve, and prepared with anhydrous ethanol into damp mass, and then screened by 12 mesh sieve to obtain wet granules, then the wet granules are dried at 50° C. for use. Besides, 0.65 g sodium bicarbonate and 0.02 g dextrin in addition with the sterilized distilled water are prepared into damp mass, and are screened by 12 mesh sieve to obtain wet granules, then the wet granules are dried at 50° C. These granules are mixed with the above dry granules, and the mixed granules are granulated, added with an appropriated amount of sterilized distilled water, baked for a while, added with 0.01 g PEG6000, uniformly mixed, and finally compressed into tablets.

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Abstract

The present invention relates to uses of a benzophenone compound and analogues thereof having a symmetrical core structure and having same or different number of hydroxyl substitutions in benzene rings in the preparation of drugs for preventing and treating viral infections and anti-tumor drugs, in particular the use in the preparation of drugs for preventing and treating HIV, herpes virus and papillomavirus infection and the diseases induced thereby, wherein such viral infections include AIDS, genital warts, flat warts, common warts, herpes simplex, herpes zoster, vaginitis, cervicitis, cervical erosion and senile dementia, as well as cervical cancer, lung cancer, gastric cancer and colon cancer induced thereby, by means of preparing the hydroxy-substituted benzophenones and analogues thereof together with various compatible excipients into different medicaments or personal disinfected sanitary articles.

Description

RELATED APPLICATIONS[0001]This is a continuation application of the International Application PCT / CN2016 / 078411, with an international filing date of Apr. 2, 2016. The present application claims the benefit of the Chinese Patent Application CN201510154291.4 filed Apr. 2, 2015, which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to uses of a hydroxy-substituted benzophenone compound having a symmetrical or asymmetric structure in the preparation of antiviral and antitumor drugs, and more particularly relates to uses of one or more hydroxy-substituted benzophenone compounds or analogues thereof as highly effective inhibitors for viruses and tumors in the preparation of drugs resistant against HIV, herpes virus and human papilloma virus and anti-tumor drugs, and preparations thereof.BACKGROUND OF THE INVENTION[0003]Hydroxy-substituted benzophenones and analogs thereof refer to derivatives having more than one hydroxyl subs...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61K31/05
CPCC12N2710/20063C12N2740/16061A61K31/12A61K31/05A61P11/02A61P15/02A61P17/12A61P25/28A61P31/12A61P31/18A61P31/20A61P31/22A61P35/00
Inventor QIN, WEIHUAJIANG, GUANGYU
Owner GUANGZHOU JIECHENG BIOLOGICAL TECH
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