Novel antiviral medicines and application thereof

A drug and virus technology, applied in the field of virus treatment, can solve problems such as high cost and long research and development cycle

Pending Publication Date: 2018-11-02
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To develop different drugs for different viruses,

Method used

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  • Novel antiviral medicines and application thereof
  • Novel antiviral medicines and application thereof
  • Novel antiviral medicines and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1. Activity Evaluation

[0052] Activity test for inhibiting virus replication at the cellular level

[0053] The present inventors tested the activity of the compounds of the present invention in inhibiting the replication of each virus at the cellular level as described in the "Materials and Methods" section above.

[0054] The half maximal inhibitory concentration IC of compound of the present invention to H3N2 (influenza virus) in host cell MDCK 50 and drug half toxic concentration TC 50

[0055] compound

IC 50 (uM)

TC 50 (uM)

SI(TC 50 / IC 50 )

Leflunomide

18

>50

>2.8

Teriflunomide

2.5

>50

>25

Buquina

1

>50

>50

[0056] The half inhibitory concentration IC of the compound against RSV (human respiratory syncytial virus) in the host cell Vero (African green monkey kidney cells) 50 and drug half toxic concentration TC 50

[0057] compound

IC 50 (uM)

TC 50...

Embodiment 2

[0066] Example 2. Combination with other antiviral drugs

[0067] The present inventor has further tested leflunomide, teriflunomide, buquinar and other antiviral drugs of the prior art, oseltamivir, ribavirin, zanamivir, Tamiflu, lanimide The combined use of Weiwei or Peramivir.

[0068] It was found that the combination of leflunomide, teriflunomide, and buquinar with these antiviral drugs can produce better therapeutic effect; among them, the therapeutic effect of combination with oseltamivir is relatively better.

[0069] discuss:

[0070] Through in vitro cell experiments and in vivo mouse challenge experiments, the compounds of the present invention have better anti-influenza virus, anti-hand-foot-mouth virus, anti-dengue fever virus and other acute infection virus capabilities. Compared with existing antiviral drugs, For example, the combination of oseltamivir can increase the survival rate of H7N9 severely infected mice by 25%. It has the prospect of being developed...

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PUM

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Abstract

The invention discloses application of leflunomide, teriflunomide, brequinar and derivatives thereof to treatment of virus infection, especially RNA virus infection. RNA viruses include but are not limited to influenza viruses, respiratory syncytial viruses, hand, foot and mouth viruses (EV71), dengue viruses (type-2 dengue viruses), Zika viruses and Japanese encephalitis viruses. The medicines have broad-spectrum and excellent antiviral activity and have relatively low toxicity to normal cells.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry; Specifically, leflunomide, teriflunomide, buquinal and derivatives thereof of the present invention are used in the preparation of drugs for the treatment of viruses, such as RNA virus infections and in the treatment of viruses, such as RNA virus infections in the application. Background technique [0002] Diseases caused by acute viral infections are an important threat to public health security. These viruses include not only the well-known influenza virus (avian influenza virus), hand-foot-mouth virus, and dengue virus, but also some new and sudden new virulent viruses such as Ebola. Viruses, coronaviruses and other RNA viruses. The diseases caused by acute viral infection all have some common characteristics: 1) short course of disease (1-2 weeks), rapid development (rapid development within a few days after onset); 2) severe illness and even death are easily caused in high-risk gr...

Claims

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Application Information

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IPC IPC(8): A61K31/42A61K31/277A61K31/215A61K31/47A61K45/06A61P31/14
CPCA61K31/215A61K31/277A61K31/42A61K31/47A61K45/06A61K2300/00Y02A50/30
Inventor 李洪林徐可赵振江熊芮
Owner EAST CHINA UNIV OF SCI & TECH
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