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Application of novel compound in preparation of medicine for preventing and/or treating coronavirus infection

A coronavirus and compound technology, which is applied in the direction of antiviral agents, drug combinations, and pharmaceutical formulas, can solve the problems of high prices, achieve low preparation costs, good antiviral effects, and facilitate clinical promotion and application

Pending Publication Date: 2022-02-18
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main clinical treatment drugs are antiviral drugs, such as HIV protease inhibitor lopinavir / ritonavir, broad-spectrum nucleoside antiviral drug ribavirin, chloroquine, and antimalarial drug chloroquine phosphate, liver protection The anti-inflammatory drug Diamine Glycyrrhizinate and some Chinese patent medicines for dispelling wind and relieving exterior, clearing away heat and detoxification, clearing lung and expel heat, and anti-influenza. However, the existing clinical data show that the above-mentioned drugs are not suitable for all people, and some drugs are more expensive

Method used

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  • Application of novel compound in preparation of medicine for preventing and/or treating coronavirus infection
  • Application of novel compound in preparation of medicine for preventing and/or treating coronavirus infection
  • Application of novel compound in preparation of medicine for preventing and/or treating coronavirus infection

Examples

Experimental program
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Effect test

Embodiment 1

[0079] When this embodiment provides n=1, a kind of preparation method of the compound shown in formula (I) and formula (III), comprises the following steps:

[0080] (1) Dissolve 16mmol of 4-bromobutyryl bromide in dichloromethane and cool down to -60°C, slowly add 32mmol of sodium bicarbonate, and then add 0.1mmol of catalyst DMAP to obtain 4-bromobutyryl bromide / sodium carbonate Chloroform system of / DMAP; synthesized according to the method described in patent CN110305188B to obtain BHA-Lys-Lys2-Lys4-Lys8-16TFA, get 1mmol of BHA-Lys-Lys2-Lys4-Lys8-16TFA dissolved in dichloromethane solution, After pre-cooling to -40°C, add dropwise to the chloroform system of 4-bromobutyryl bromide / sodium carbonate / DMAP, and slowly raise the temperature to -10°C to react; there is no BHA-Lys-Lys2-Lys4-Lys8- in the detection system After 16TFA remains, slowly add saturated brine to the system dropwise to quench the reaction, stir, separate liquids, separate the dichloromethane layer, wash w...

Embodiment 2

[0084] When this embodiment provides n=2, a kind of preparation method of the compound shown in formula (I) and formula (III), comprises the following steps:

[0085] (1) Dissolve 32 mmol of 3-bromopropionyl bromide in chloroform and cool to 0°C, slowly add 64 mmol of sodium carbonate, and then add 0.1 mmol of catalyst DMAP to obtain 3-bromopropionyl bromide / sodium bicarbonate / DMAP dichloromethane system; synthesized according to the method described in patent CN110305188B to obtain BHA-Lys-Lys2-Lys4-Lys8-16TFA, get 1mmol of BHA-Lys-Lys2-Lys4-Lys8-16TFA dissolved in chloroform solution, After precooling to -20°C, add dropwise to the dichloromethane system of 3-bromopropionyl bromide / sodium bicarbonate / DMAP, and slowly raise the temperature to 10°C to react; there is no BHA-Lys-Lys2-Lys4-Lys8- in the detection system After 16TFA remains, slowly add saturated brine to the system dropwise to quench the reaction, stir, separate liquids, separate the chloroform layer, wash with 0....

Embodiment 3

[0089] When this embodiment provides n=3, a kind of preparation method of the compound shown in formula (I) and formula (III), comprises the following steps:

[0090] (1) Dissolve 19 mmol of 5-bromopentanoyl bromide in ethyl acetate and cool down to -40°C, slowly add 35 mmol of sodium hydride, and then add 0.1 mmol of catalyst DMAP to obtain 5-bromopentanoyl bromide / sodium hydride / DMAP ethyl acetate system; synthesized according to the method described in patent CN110305188B to obtain BHA-Lys-Lys2-Lys4-Lys8-16TFA, take 1mmol of BHA-Lys-Lys2-Lys4-Lys8-16TFA dissolved in ethyl acetate solution, After pre-cooling to -30°C, add dropwise to the ethyl acetate system of 5-bromovaleryl bromide / sodium hydride / DMAP, and slowly raise the temperature to -5°C to react; there is no BHA-Lys-Lys2-Lys4-Lys8- in the detection system After 16TFA remains, slowly add saturated brine to the system dropwise to quench the reaction, stir, separate liquids, separate the ethyl acetate layer, wash with ...

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Abstract

The invention discloses application of a novel compound in preparation of a medicine for preventing and / or treating coronavirus infection. The coronavirus targeted by the invention at least comprises SARS-CoV-2, SARS-CoV and MERS-CoV. In-vitro test results show that the novel compound, including drugs prepared from a compound III and a compound IV, have an obvious effect of resisting coronavirus infection; the medicine can be applied to prevention and / or treatment of novel coronavirus pneumonia, severe acute respiratory syndrome, middle east respiratory syndrome and other diseases caused by SARS-CoV-2, SARS-CoV, MERS-CoV and other coronaviruses. The compound III and the compound IV are high in activity and good in antiviral effect. The compound is low in preparation cost, simple in preparation method, suitable for large-scale production and convenient for later clinical popularization and application.

Description

technical field [0001] The invention relates to the technical field of chemical industry and medicine, in particular to the application of novel compounds in the preparation of drugs for preventing and / or treating coronavirus infection. Background technique [0002] Coronaviruses are a large family of viruses ranging in severity from colds to severe illnesses such as Middle East Respiratory Syndrome (MERS), Severe Acute Respiratory Syndrome (SARS) and the current global pandemic of Corona Virus Disease 2019 , COVID-19). [0003] SARS virus β belongs to subgroup B coronavirus. It is an infectious disease with rapid onset, rapid spread and high fatality rate. Most of the infected patients have direct or indirect contact with patients, or live in endemic areas. [0004] MERS virus is a β genus C subgroup coronavirus, its full name is Middle East Respiratory Syndrome Coronavirus (MERS-CoV for short), and it causes Middle East Respiratory Syndrome (Middle East Respiratory Syndro...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61P31/14A61P11/00
CPCA61K38/08A61P31/14A61P11/00
Inventor 卢智俊赵志荣陈伟强袁永玲赵玉姣赵芹
Owner REGENEX PHARMA LTD
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