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8S-Deca-9-en-4,6-diyne-1,8-diol as well as pharmaceutical composition and application thereof

A technology of composition and medicine, applied in the direction of active ingredients of hydroxy compounds, separation/purification of hydroxy compounds, antiviral agents, etc., can solve the problem of hepatitis B virus with no reports of pharmaceutical compositions, no compounds and their pharmaceutical compositions Reports on drug application, low anti-HBV activity, etc.

Inactive Publication Date: 2018-11-16
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reports on the activity of these compounds in the existing literature mainly focus on protecting the liver and promoting choleresis, and there are few studies on their anti-HBV activity. In 2014, Zhao Yong et al. isolated a series of sesquiterpene and chlorogenic acid derivatives from Artemisia annua. substances, triterpenes, flavonoids, lignin and phenolic acids (Zhao Y., et al. Geng Chang'an et al. isolated pyridone and enyne glycoside esters from Artemisia marina (Geng CA, etc.) with in vitro anti-HBV activity
[0004] So far, there is no report of compound 8S-dec-9-ene-4,6-diyne-1,8-diol (1) in the prior art, and there is no report of its pharmaceutical composition as an active ingredient, nor Report on the application of the compound and its pharmaceutical composition in the preparation of medicines for treating hepatitis B

Method used

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  • 8S-Deca-9-en-4,6-diyne-1,8-diol as well as pharmaceutical composition and application thereof
  • 8S-Deca-9-en-4,6-diyne-1,8-diol as well as pharmaceutical composition and application thereof
  • 8S-Deca-9-en-4,6-diyne-1,8-diol as well as pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Preparation of 8S-dec-9-ene-4,6-diyne-1,8-diol (1):

[0056] Extraction and separation of 8S-dec-9-ene-4,6-diyne-1,8-diol (1):

[0057] Take the dried whole herb of Artemisia capriculum or Artemisia chinensis, crush it, and extract it twice with 90% ethanol under reflux, 2 hours each time, combine the ethanol extracts, recover the ethanol under reduced pressure to obtain the extract, dissolve and absorb the extract on silica gel with 75% ethanol Put it at room temperature to evaporate the solvent, grind and sieve, and go through silica gel column chromatography, using 9:1:0, 9:1:0.1, 8:2:0.2, 6:4:0.4 chloroform-methanol-water gradient Eluted to obtain 5 fractions A-E, fraction A was subjected to silica gel column chromatography, 9:1 to 6:4 petroleum ether-acetone gradient elution, and 5 fractions A-1 to A-5 were obtained. D-2 was subjected to silica gel column chromatography and eluted with 95:5 chloroform-methanol to obtain two fractions D-2-1 and D-2-2, and D-2-1 was...

Embodiment 2

[0073] Compound Combination Pharmaceutical Form - Tablet:

[0074] Preparation of the pharmaceutical combination tablet with compound 1 of the present invention as the active ingredient: use compound 1 as the active ingredient of the drug, use the excipients described in Table 3 as the auxiliary material components for the preparation of the combined drug tablet, and make each tablet according to the ratio For tablet samples containing 5-60 mg of the pharmaceutical ingredient of compound 1, Table 3 shows the formula ratio of common tablets:

[0075] Table 3. Crude drug and adjuvant formula of compound 1 combination drug tablet of the present invention

[0076]

[0077] The method for preparing a certain amount of compound 1 and excipients and auxiliary materials into different doses of tablet preparations is to uniformly mix several excipients and auxiliary materials with the bulk drug, add 1% hydroxymethylcellulose sodium solution in an appropriate amount to make a soft ma...

Embodiment 3

[0079] Compound Combination Pharmaceutical Form - Capsules:

[0080] Preparation of the drug combination capsule preparation containing compound 1 as the active ingredient: use the compound 1 sample as the drug active ingredient, use several excipients in Table 4 as the auxiliary material components for the preparation of the combination drug capsule preparation, and make each capsule according to the ratio The capsules contain 5-50 mg of the pharmaceutical ingredient of compound 1. Table 4 shows the formula ratio of common capsule preparations:

[0081] The bulk drug and adjuvant formula of the compound combination medicine capsule preparation of table 4 embodiment 1

[0082]

[0083] The method for preparing a certain amount of Compound 1 samples and excipients into capsule preparations is as follows: mix several excipients and Compound 1 in Example 1 evenly, add an appropriate amount of 1% sodium hydroxymethylcellulose solution, and prepare into wet granules, dried, sie...

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PUM

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Abstract

The invention provides a compound 8S-Deca-9-en-4,6-diyne-1,8-diol, 1 shown in structural formula (I) as well as a compound 1 containing 8S-Deca-9-en-4,6-diyne-1,8-diol as an active ingredient and pharmaceutical composition containing a pharmaceutically acceptable carrier or excipient. The invention further provides preparation methods of the compound and the pharmaceutical composition containing the compound and applications of the compound and the pharmaceutical composition in preparation of drugs for treating human diseases, especially in preparation of drugs for resisting viral hepatitis B.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to a new enyne compound 8S-dec-9-ene-4,6-diyne-1,8-diol (1), which is used as a drug for treating hepatitis B virus as an active ingredient The composition, its preparation method, and its application in pharmacy, especially the application in the preparation of anti-hepatitis B drugs. Background technique: [0002] Hepatitis B is an infectious disease caused by hepatitis B virus (HBV) in a chronic carrier state. Chronic hepatitis B (CHB) is one of the main causes of liver cirrhosis and liver cancer. According to World Health Organization (WHO) statistics, there are 2 billion HBV carriers in the world, of which about 350 million are CHB patients; about 120 million people are HBV carriers in China, and more than 30 million CHB patients (Lin Yonghuan. Hepatitis B Prevention and Treatment [M] .Beijing: Science and Technology Literature Press, 2007.; Lavanchy D.J Viral ...

Claims

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Application Information

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IPC IPC(8): C07C33/048C07C29/76A61K31/047A61P31/20
CPCA61P31/20C07C33/048
Inventor 陈纪军耿长安马云保黄晓燕张雪梅杨静
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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