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Broad spectrum antiviral inhibitor

A virus infection and application technology, applied in the field of medicine, can solve the problems that the virus cannot be completely eliminated, and there is no effective preventive vaccine and treatment method for the virus.

Inactive Publication Date: 2018-06-08
NAT INST FOR FOOD & DRUG CONTROL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the above-mentioned drugs can usually only inhibit active virus replication, and cannot completely eliminate latent or hidden viruses in the host
[0004] In short, given that the currently available vaccines and antiviral drugs are limited by some defects, there are no effective preventive vaccines and treatments for infections caused by many viruses in clinical practice. Therefore, it is urgent to find new broad-spectrum antiviral drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Embodiment 1. Construction of pseudovirus

[0081] 1.1 Antiviral Drug Screening Principle Based on Pseudovirus

[0082] The envelope protein on the virus is responsible for recognizing receptors on the surface of target cells to initiate the process of adsorption and penetration, thereby invading cells. Furthermore, the phenotypic mixing that occurs when two viruses co-infect a cell suggests that the envelope of one virus can be integrated on the particle surface of a different virus. Based on the above two points, a new technology—pseudovirus technology has been developed in the study of the process of virus invasion into cells and its tissue tropism and receptors.

[0083] The current pseudovirus refers to a retrovirus that can integrate the envelope glycoprotein of another different type of virus to form an envelope with an exogenous virus, and the genome maintains the genomic characteristics of the retrovirus itself. virus. Pseudovirion is a viral protein provide...

Embodiment 2

[0107] Embodiment 2.RV-04 is to the evaluation of the inhibitory activity of multiple pseudoviruses

[0108] In this example, the RV pseudovirus, EBOV pseudovirus and MARV pseudovirus prepared in Example 1 were used to evaluate the inhibitory activity of RV-04 on the above three viruses.

[0109] 2.1 Experimental steps

[0110] Since the pseudovirus backbone plasmid pSG3Δenv.cmvFluc used in the present invention is derived from HIV, in order to exclude the possibility that the drug inhibits the pseudovirus by preventing the reverse transcription process of the backbone HIV, the present invention utilizes the pseudovirus containing Vesicular stomatitis virus (VSV) membrane protein chimeric pseudovirus was re-screened to exclude false positives. Calculate the ratio of the 50% inhibitory concentration (IC50) of the drug to the VSV membrane protein chimeric pseudovirus and the target virus membrane protein chimeric pseudovirus (that is, RV pseudovirus, EBOV pseudovirus or MARV ps...

Embodiment 3

[0126] Cytotoxicity evaluation of embodiment 3.RV-04

[0127] 3.1 Experimental steps

[0128] In this example, the effect of RV-04 drug on cell activity is evaluated by ATP quantitative determination, and its detection principle is as follows:

[0129] ATP is an indicator of metabolism in living cells, using Luminescence method cell viability detection kit, through the quantitative determination of ATP to detect the number of living cells in the culture after the action of drugs and cells, the cell lysis and the luminescent signal produced are proportional to the amount of ATP present, and the amount of ATP is directly related to the culture Proportional to the number of cells in . The 50% cytotoxic concentration (CC50) of the drug was calculated by the effect of the drug on the ATP luminescent signal in the cells. Calculate the ratio of the 50% cytotoxic concentration (CC50) of the drug to the IC50 of the drug to the target virus (that is, the therapeutic index SI=CC50 / IC...

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Abstract

The invention belongs to the technical field of medicines and relates to a broad spectrum antiviral inhibitor, in particular to an application of a compound of a structure as shown in a formula (I) asshown in the description for preventing and / or treating virus infection or diseases caused by virus infection. The invention also relates to an application of the compound of the structure as shown in the formula (I) for preventing and / or treating virus infection or diseases caused by virus infection.

Description

technical field [0001] The invention belongs to the technical field of medicine. In particular, the present invention relates to the use of compounds having the structure of formula (I) for preventing and / or treating viral infections or diseases caused by viral infections. The present application also relates to the use of the compound having the structure of formula (I) for the preparation of a medicament for preventing and / or treating viral infection or diseases caused by viral infection. [0002] Background technique [0003] The prevalence of viral infectious diseases has had a huge impact on human health and life. Currently, the prevention and treatment of viral infections mainly relies on vaccination and / or antiviral drug therapy. However, the high price of vaccines and the need for low-temperature storage make them difficult to use widely; moreover, vaccine research against many viruses has yet to achieve a real breakthrough. Antiviral drugs have gradually becom...

Claims

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Application Information

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IPC IPC(8): A61K31/4706A61P31/12
CPCA61K31/4706
Inventor 王佑春刘强黄维金曹守春李玉华
Owner NAT INST FOR FOOD & DRUG CONTROL
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