Polycyclic pyridone compound as well as pharmaceutical composition and application thereof

A technology of heterocyclic compounds and drugs, which is applied in the field of polycyclic pyridone compounds and their drug combinations and uses, and can solve problems such as drug resistance and the impact of therapeutic effectiveness

Inactive Publication Date: 2019-03-22
赵蕾 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are reports that influenza viruses have shown resistance to these drugs, compromising treatment effectiveness

Method used

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  • Polycyclic pyridone compound as well as pharmaceutical composition and application thereof
  • Polycyclic pyridone compound as well as pharmaceutical composition and application thereof
  • Polycyclic pyridone compound as well as pharmaceutical composition and application thereof

Examples

Experimental program
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Embodiment Construction

[0033] The present invention will be described in further detail below through examples, but the present invention is not limited to these examples. The reagents and raw materials used in the examples of the present invention are all commercially available.

[0034]

[0035] Preparation of Compound 2

[0036]Under a nitrogen atmosphere, to a solution of compound 1 (10.0 g, 99.0 mmol) in THF (150 mL) was added 2.5 M n-butyllithium-hexane solution (39.6 mL, 99.0 mmol), and the mixture was stirred at -78 ° C for 2 Hour. A solution of allyl chloroformate (11.92 g, 99.0 mmol) in THF (40 mL) was added dropwise to the reaction mixture, stirred at -78°C for 2 hours, the reaction solution was quenched with saturated aqueous ammonium chloride solution, raised to room temperature, Extract with ethyl acetate. Wash with saturated brine, dry the organic layer with anhydrous magnesium sulfate, and distill off the solvent under reduced pressure to obtain compound 2 (11.87 g, yield 65%)....

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Abstract

The invention provides a polycyclic pyridone compound as well as pharmaceutical composition and an application thereof. Specifically, the polycyclic pyridone compound is a compound shown as the formula (I) or pharmaceutically acceptable salt, solvate or hydrate of the compound. The compound can be used for preparing drugs for preventing or treating infectious diseases of mammals, and is particularly used for preparing drugs for preventing, treating, relieving and/or treating orthomyxovirus infection such as influenza A virus, influenza B virus and influenza C virus.

Description

technical field [0001] The application relates to a polycyclic pyridone compound and its pharmaceutical combination and application. Background technique [0002] Human influenza virus (influenza virus) is a representative species of Orthomyxoviridae (Orthomyxoviridae), referred to as influenza virus. Human influenza virus can be divided into three classes according to the antigenicity of its nucleoprotein: influenza A virus (Influenza A virus), also known as type A influenza virus, type B influenza virus (Influenza B virus), also known as type B influenza virus and Influenza C virus (Influenza C virus), also known as C influenza virus. Among them, the antigenicity of influenza A virus is easy to mutate, causing worldwide pandemics many times. For example, in the pandemic from 1918 to 1919, at least 20 million to 40 million people died of influenza in the world; influenza B virus is also relatively pathogenic to humans; influenza C virus only causes inconspicuous or mild s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/14C07D513/14C07F9/6561A61K31/675A61K31/685A61K31/5383A61K31/542A61P31/16
CPCC07D498/14C07D513/14C07F9/6561
Inventor 赵蕾杨学聪刘江黄新全
Owner 赵蕾
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