Alkylene-Chain Antiviral Compounds for Coronavirus and ASFV Treatment

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Solution Overview

Problem

There is a need for new antiviral treatments for COVID-19 and African Swine Fever, as existing treatments are inadequate in addressing the severity and transmission of these diseases.

Innovation Solution

Development of compounds, such as those of formulae IV to XIV, which are used in pharmaceutical compositions to treat infections caused by coronaviruses like SARS-CoV-2 and African Swine Fever virus, utilizing alkylene chains and anions to inhibit viral replication.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing antiviral treatments are used, then treatment availability is maintained, but treatment efficacy is insufficient for severe diseases like COVID-19 and African Swine Fever

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtreatment applicability to new viruses
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent describes compounds with a core chemical structure that can treat multiple different viral infections including COVID-19 (SARS-CoV-2), African Swine Fever (ASFV), and other coronaviruses. The compounds of formula (I) and their salts are designed to have broad-spectrum antiviral activity, allowing one treatment to address multiple viral threats rather than requiring virus-specific medications.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Reliability

If new antiviral compounds are developed, then treatment efficacy improves, but development time and complexity increase

Engineering Contradiction:
Improveviral replication inhibitionVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The antiviral compound is designed with a segmented molecular structure consisting of a core structure with specific substituents (formula I), where R represents different alkyl groups and A represents anionic groups. This segmentation allows systematic modification of different parts of the molecule to optimize antiviral activity while maintaining a manageable structural framework that can be synthesized through established chemical methods.

Inventive Principle:
Principle #1Segmentation

3Reliability

If high concentration of antiviral compounds is used, then viral replication inhibition increases, but potential side effects increase

Engineering Contradiction:
Improveviral infection treatmentVSAvoidpotential toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs compounds with specific chemical parameters including the alkyl chain length (R group) and anionic group composition (A group) in formula (I). By carefully selecting and optimizing these molecular parameters, the compounds achieve effective antiviral activity at lower concentrations, thereby reducing potential toxicity. The structural parameters are tuned to maximize therapeutic index.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4232018B1Compounds for use in treating coronavirus infection and african swine fever virus infection
Publication Date: 2025.08.20 RHEA GENETICS PTE LTD
  • EP4232018B1 patent drawingFigure 1
  • EP4232018B1 patent drawingFigure 2
  • EP4232018B1 patent drawing

AI summary

There is disclosed a compound for use in the treatment of an infection caused by a coronavirus or African Swine fever virus, wherein the compound has formula (I): wherein R is an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of -2, or R is a quaternary amine having the following formula: (la) wherein Ra and Rb are each an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of -3; R1, R2, R3, R4, R5 and R6 are each independently selected from C1-10 alkyl and H; E has the following formula (lb), wherein the ester oxygen is bonded to the aromatic ring of each E at the same position, the position being position 2 or 3; and wherein RE is H or a halide.