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Application of compound to treatment of SARS-CoV-2 infection

A sars-cov-2 and compound technology, applied in the field of pharmaceutical technology and viral infection diseases, can solve the problems of ineffective reversal of severe patients, multiple, diffuse lesions, etc.

Inactive Publication Date: 2020-11-27
SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA +1
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0005] At present, there is no clear therapeutic drug for severe acute respiratory syndrome type 2 coronavirus infection. Clinical treatment mainly adopts isolation, anti-virus, symptomatic support and other therapies, but these treatments still cannot meet the clinical needs
On the one hand, commonly used antiviral drugs are likely to cause side effects such as neurotoxicity, diarrhea, arrhythmia, abnormal liver function, etc., especially for the elderly who suffer from basic metabolic disorders, low immune function, or cancer and other basic diseases.
On the other hand, symptomatic treatment is not effective in reversing the condition of severe patients, or the effect is not good, and it is easy to cause co-infection, resulting in multiple and diffuse lesions

Method used

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  • Application of compound to treatment of SARS-CoV-2 infection
  • Application of compound to treatment of SARS-CoV-2 infection
  • Application of compound to treatment of SARS-CoV-2 infection

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Embodiment Construction

[0012] According to literature reports, the activity data in a variety of different species of viruses show that the antiviral activity of remdesivir is superior to that of compound 69-0. For example, remdesivir inhibits EBOV virus in Hela cells, inhibits EBOV in HMVEC cells, inhibits RSV in Hep-2 cells, inhibits HCV in Huh-7 cells, and inhibits the IC50 of SARS-CoV proliferation in HAE cells They were 0.1 μM, 0.053 μM, 0.015 μM, 0.057 μM, and 0.069 μM, and the virus-inhibiting activity of compound 69-0 in the same experiment was >20 μM, 0.78 μM, 0.53 μM, 4.1 μM, and 0.18 μM, respectively. Compared with remdesivir, the activity of compound 69-0 to inhibit virus was reduced by 3~>200 times. Ribose monophosphorylation in compound 69-0 is considered to be the rate-limiting step in the activation of compound 69-0, and remdesivir directly introduces monophosphate into ribonucleosides, and connects with polar groups through phosphoramide bonds to form phosphorus Amide prodrugs redu...

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Abstract

The invention provides an application of a compound 69-0 and / or tautomers and / or pharmaceutically acceptable salts thereof to prevention, alleviation and / or treatment of COVID19 / SARS-CoV-2. Products containing the compounds can effectively inhibit replication or reproduction of SARS-CoV-2 or homologous variant viruses of SARS-CoV-2 and the cytopathic effect produced by SARS-CoV-2. The compound 69-0 has good curative effect, good safety and low toxic and side effects. The invention also provides combined therapeutic pharmaceutical composition. The combined therapeutic pharmaceutical compositioncan effectively inhibit proliferation of SARS-CoV-2 in cells, and has good curative effect, low safety and low toxic and side effects, can reduce drug resistance of viruses and has obvious synergistic effect.

Description

technical field [0001] The present invention relates to the fields of pharmaceutical technology and virus infection disease technology, and specifically relates to the application of compound 69-0 and / or its tautomer and the like. Background technique [0002] Severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2), also known as 2019 novel coronavirus, was discovered in the outbreak of 2019 novel coronavirus pneumonia (COVID-19). SARS-CoV-2 is a virus with a high ability to spread. The disease is mainly transmitted by respiratory droplets and contact, and the crowd is generally susceptible and highly contagious. [0003] SARS-CoV-2 is an enveloped, single-stranded RNA betacoronavirus. The infection of the new coronavirus begins with the binding of the spike glycoprotein (Spike, S protein) on the surface of the virus particle to the angiotensin-converting enzyme (ACE2) receptor on the cell surface. After the coronavirus enters the host cell, it disintegrates and...

Claims

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Application Information

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IPC IPC(8): A61K31/53A61P31/14A61P11/00
CPCA61K31/53A61P11/00A61P31/14
Inventor 张绪穆郭德银李迎君曹流李官官邢帆
Owner SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
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