Antiviral compound and preparation method thereof

A compound and pharmaceutical technology, applied in the field of medicine, can solve problems such as the lack of effective therapeutic drugs, the inability to directly kill viruses, and the increase in demand for therapeutic drugs

Inactive Publication Date: 2008-06-04
SHANDONG XUANZHU PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is still a lack of effective therapeutic drugs for a wide variety of viral infectious diseases. The existing antiviral drugs are only virus inhibitors and cannot directly kill viruses. Therefore, the demand for such therapeutic drugs has increased sharply

Method used

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  • Antiviral compound and preparation method thereof
  • Antiviral compound and preparation method thereof
  • Antiviral compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] The preparation of embodiment 1 compound of the present invention

[0122] 1. Preparation of 3,19-diacetyl-12-(N-3-formylamino-1H-1,2,4-triazole)-14-deoxy-andrographolide (compound 1 for short)

[0123] Put 3.5g (10mmol) of andrographolide into the reaction flask, then add 50ml of acetic anhydride, reflux for 10min, recover the acetic anhydride after the reaction is completed, pour the residue into 200ml of ice water, extract with 50ml of chloroform × 2, combine the organic layers, Washed with water, dried, and the solvent was recovered under reduced pressure to obtain a crude product of 3,14,19-triacetyl-andrographolide, which was recrystallized from absolute ethanol to obtain 3.4 g of a refined product, yield: 71%.

[0124] Dissolve 1.1g (10mmol) 3-formylamino-1H-1,2,4-triazole in 20ml chloroform, add 2.7g (25mmol) / 20ml chloroform containing trimethylchlorosilane dropwise, and stir at room temperature for reaction 3 Hour. The reaction solution was transferred into...

Embodiment 2

[0149] The preparation of embodiment 2 compound tablet of the present invention

[0150] Prescription 1:

[0151] Any one of compounds 1-7 or its derivatives 100g (based on compound)

[0152] Microcrystalline Cellulose 50g

[0153] 60g pregelatinized starch

[0154] Magnesium Stearate 1.5g

[0155] Carboxymethyl Starch Sodium 5g

[0156]

[0157] A total of 1000 tablets were prepared

[0158] Prescription 2:

[0159] Any one of compounds 1-7 or its derivatives 200g (based on compound)

[0160] Microcrystalline Cellulose 100g

[0161] 120g pregelatinized starch

[0162] Magnesium Stearate 3g

[0163] Carboxymethyl Starch Sodium 10g

[0164]

[0165] A total of 1000 tablets were prepared

[0166] 2. Preparation process: pass the raw materials and auxiliary materials through 100 mesh sieve respectively, and set aside; weigh the raw materials and aux...

Embodiment 3

[0167] The preparation of embodiment 3 compound capsules of the present invention

[0168] 1. Prescription

[0169] Prescription 1:

[0170] Any one of compounds 1-7 or its derivatives 50g

[0171] 20g pregelatinized starch

[0172] Microcrystalline Cellulose 10g

[0173] 10% PVPK30 ethanol solution appropriate amount

[0174] Magnesium stearate 0.5g

[0175]

[0176] A total of 1000 capsules were prepared

[0177] Prescription 2:

[0178] Any one of compounds 1-7 or its derivatives 75g

[0179] 30g pregelatinized starch

[0180] Microcrystalline Cellulose 15g

[0181] 2% HPMC aqueous solution appropriate amount

[0182] Micronized silica gel 1.5g

[0183] Magnesium stearate 0.75g

[0184]

[0185] A total of 1000 capsules were prepared

[0186] Prescription 3:

[0187] Any one of compounds 1-7 or its derivatives 100g

[0188] 40g...

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Abstract

The invention pertains to the field of medical technology and relates to novel compounds with antiviral activity, isomer or pharmaceutically acceptable salts thereof shown in the formula (I), wherein, R<1>, R<2> and R<3> are defined as the instruction. The invention also relates to preparation methods of the compounds, a medical composition which contains the compounds and the application of the compounds in preparation of drugs which are used for curing and / or preventing diseases caused by viral infection.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and relates to a novel antiviral compound, its isomer or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound and a preparation method. 2. Background technology [0002] Virus infection can cause a variety of diseases and seriously endanger human health and life. According to incomplete statistics, about 60% of epidemic infectious diseases are caused by viruses. With the development of medicine and related science and technology, the incidence of viral infectious diseases such as smallpox, measles, rubella and other diseases that ravaged the world in the 20th century has been decreasing day by day, but new viruses, especially highly pathogenic viruses, are constantly being used. It was found that some even broke out and became popular, while old viruses fluctuated from time to time, posing a serious potential threat. In November 2002, the first ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/06C07D307/58C07D473/18C07D417/12A61K31/4196A61K31/365A61K31/506A61K31/522A61K31/427A61P31/12A61P29/00
Inventor 黄振华
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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