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Use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine for preparing neuraminidase inhibitor

A neuraminidase, acetyl group technology, applied in the direction of antiviral agents, active ingredients of heterocyclic compounds, etc.

Inactive Publication Date: 2011-10-05
HUNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But studies have found that some virus strains are resistant to oseltamivir

Method used

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  • Use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine for preparing neuraminidase inhibitor
  • Use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine for preparing neuraminidase inhibitor
  • Use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine for preparing neuraminidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 14

[0019] Preparation of Example 14-Alkyl-6-aryl-5-acetyl-2-amino-1,3-thiazine (I) and its salts

[0020] 4-Alkyl-6-aryl-5-acetyl-2-amino-1,3-thiazine (I) and its salts were prepared according to the literature [CN 201010595032.2].

[0021]

[0022] Wherein, X is selected from: 2-chloro, 2-fluoro, 2-hydroxy, 2-methoxy, 2-ethoxy, 2-nitro, 3-dimethylamino, 3-chloro, 3-bromo, 3 -Fluoro, 3-methyl, 3-ethyl, 3-trifluoromethyl, 3-hydroxy, 3-methoxy, 3-ethoxy, 3-nitro, 3-sulfonic acid, 3-methyl Sulfonylamino, 3-sulfamoyl, 4-dimethylamino, 4-chloro, 4-bromo, 4-fluoro, 4-methyl, 4-ethyl, 4-trifluoromethyl, 4-hydroxyl, 4 -methoxy, 4-ethoxy, 4-acetoxy, 4-nitro, 4-sulfonate, 4-methanesulfonylamino, 4-sulfamoyl, 2-chloro-5-nitro, 3-ethyl-4-hydroxy, 3,4-dimethoxy or 2,4,5-trimethoxy; R 1 Selected from: C 1 ~C 2 Alkyl, C 3 ~C 4 Linear alkyl or branched alkyl; salt selected from hydrochloride, hydrobromide, phosphate, sulfate, nitrate, methanesulfonate or p-toluenesulfonate.

Embodiment 24

[0023] Preparation of Example 24-Alkyl-6-aryl-5-acetyl-2-acylamino-1,3-thiazine (II) and its salts

[0024] 4-Alkyl-6-aryl-5-acetyl-2-acylamino-1,3-thiazine (II) and its salts were prepared according to the literature [CN 201010595032.2].

[0025]

[0026] Compounds of the invention

[0027] It can be seen from the data in the table that the preferred compounds have better inhibitory activity on neuraminidase and can be applied to the preparation of neuraminidase inhibitors. The inhibitory rate of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine on neuraminidase was higher than that of corresponding 4-alkyl-6-aryl-2-amido-1,3- Thiazine-5-carboxylate has a high rate of inhibition of neuraminidase.

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PUM

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Abstract

The invention discloses use of 4-alkyl-6-aryl-5-acetyl-1,3-thiazine represented by a chemical structural formula I and 4-alkyl-6-aryl-5-acetyl-2-amino-1,3-thiazine salts, or 4-alkyl-6-aryl-5-acetyl-2-amido-1,3-thiazine represented by a chemical structural formula II and 4-alkyl-6-aryl-5-acetyl-2-amido-1,3-thiazine salts for preparing a neuraminidase inhibitor of influenza viruses.

Description

technical field [0001] The present invention relates to the application of a class of compound 4-alkyl-6-aryl-5-acetyl-1,3-thiazine in the pharmaceutical industry, specifically including 4-alkyl-6-aryl-5-acetyl -2-amino-1,3-thiazine and its salt and 4-alkyl-6-aryl-5-acetyl-2-acylamino-1,3-thiazine and its salt are used in the preparation of influenza virus nerve ammonia Application in acidase inhibitors. Background technique [0002] According to the latest report on the 2009 Influenza A (H1N1) global situation released by the World Health Organization on February 26, 2010, at least 16,226 patients in 213 countries and regions have died from this pandemic. Neuraminidase (NA) inhibitors are the first-line drugs against influenza A virus. Neuraminidase (NA) inhibitors include compounds such as Zanamivir, Oseltamivir and Peramivir, among which Oseltamivir is widely used. But studies have found that some virus strains are resistant to oseltamivir. Chinese patent describes 4-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/54A61P31/16
Inventor 胡艾希李婉夏曙彭俊梅叶姣谭卫清
Owner HUNAN UNIV
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