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Pharmaceutical composition for treating influenza and preparation containing pharmaceutical composition

A composition and drug technology, applied in medical preparations containing active ingredients, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve the problems of high mutation rate of influenza virus, high risk of patients taking drugs, and prolonged treatment time, etc. Achieve the effect of good anti-influenza virus, excellent anti-influenza virus and good market prospect

Active Publication Date: 2021-07-16
GUANGDONG RAYNOVENT BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] It can be seen that influenza virus has the characteristics of high mutation rate and frequent recombination between viruses, which affects the therapeutic effect of drugs; although active compounds with new structures and new mechanisms are constantly being used However, in the long run, the use of a single antiviral drug may have the disadvantage of being unable to effectively inhibit / reduce the virus concentration in the body and cure viral colds in a short period of time, and the corresponding increase in dosage and prolonged treatment time also pose a threat to patients. Brings a greater risk of drug use

Method used

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  • Pharmaceutical composition for treating influenza and preparation containing pharmaceutical composition
  • Pharmaceutical composition for treating influenza and preparation containing pharmaceutical composition
  • Pharmaceutical composition for treating influenza and preparation containing pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1 prepares compound 1

[0060] The free substance of compound 1 was prepared by the method disclosed in Example 4 of WO2018041263, and the structural characterization proved that the obtained product was the free substance of compound 1.

Embodiment 2

[0061] Embodiment 2 prepares the hydrochloride of compound 1

[0062] Take 5g of compound 1 and put it into a 250mL eggplant-shaped flask, add THF (100mL), add hydrochloric acid (0.98mL, dissolved in 9mLTHF), stir at 30°C for 12 hours, filter the solid, and dry the filter cake in vacuum at 40°C to obtain the salt of compound 1 salt.

Embodiment 3

[0063] Embodiment 3 prepares the p-toluenesulfonate of compound 1

[0064] Take 5g of compound 1 and put it into a 250mL eggplant-shaped flask, add THF (100mL), add p-toluenesulfonic acid monohydrate (2.26g, dissolved in 10mL THF), stir at 30°C for 12 hours, filter the solid, and vacuum the filter cake at 40°C Drying gave a solid (0.425g). This solid (0.101 g) was added into acetone (2 mL) and slurried for 12 h to obtain p-toluenesulfonate of compound 1.

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PUM

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Abstract

The invention discloses a pharmaceutical composition, the pharmaceutical composition comprises a first effective component, a second effective component and an optional third effective component, the effective components have a good drug synergistic effect, and the pharmaceutical composition has a good patent medicine prospect after comprehensive evaluation.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a pharmaceutical composition for treating influenza and a preparation containing the pharmaceutical composition. Background technique [0002] Influenza virus, namely influenza virus (IFV), is a segmented single-stranded antisense RNA virus that can cause influenza in humans and animals. According to the statistics of the World Health Organization (WHO), the annual seasonal influenza epidemic can lead to 3 million to 5 million severe cases and 290,000 to 650,000 deaths worldwide. Each influenza pandemic has caused great harm to global public health and economy. havoc. [0003] Current clinical protocols for influenza include vaccination and chemotherapy and chemoprophylaxis with antiviral drugs. Patent WO2018041263 discloses a series of pyrimidine derivatives with PB2 Cap binding inhibitory effect. In vitro activity data show that some compounds show positive effects in the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K31/53A61K45/06A61K9/20A61P31/16A61K31/215A61K31/351A61K31/196
CPCA61K31/506A61K31/53A61K45/06A61K9/2095A61P31/16A61K31/215A61K31/351A61K31/196A61K2300/00A61K9/20C07D403/04C07D471/04
Inventor 陈小新李海军刘卓伟黄淑娟刘志强龙超峰
Owner GUANGDONG RAYNOVENT BIOTECH CO LTD
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