Host-Targeted Antiviral Compound for Coronavirus Variant Resistance

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Solution Overview

Problem

There is an urgent need for an effective treatment for Coronavirus (CoV) infections, particularly for COVID-19, that is not dependent on targeting viral proteins and can address variants, as existing treatments are inadequate and hospitalization rates remain high due to viral mutation and other factors.

Innovation Solution

A compound of general formula I, specifically PLD or its pharmaceutically acceptable salts/stereoisomers, is used for treating CoV infections, including COVID-19, by administering a therapeutically effective amount to reduce viral load, severity of symptoms, and complications such as hospitalization and death, potentially in combination with corticosteroids like dexamethasone.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments targeting viral proteins are used, then specific antiviral effect is achieved, but effectiveness is lost against viral variants due to mutation

Engineering Contradiction:

Improveeffectiveness against viral variantsVSAvoidspecificity to viral proteins

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent uses host cell factors (eEF1A, PKR, UPR pathways) as intermediaries to achieve antiviral effect. Instead of directly targeting viral proteins which mutate, the compound interferes with host factors that viruses depend on for replication, thereby maintaining effectiveness against variants while achieving specific antiviral action through the host-mediated mechanism

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If vaccines are developed for prevention, then immunization is achieved, but treatment need remains unmet due to viral mutation and hospitalization rates

Engineering Contradiction:

Improveprotection against infectionVSAvoidhospitalization and death rates

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent provides preliminary therapeutic action by interfering with early viral replication processes through host cell factor modulation. The compound acts preemptively to block viral propagation before it can cause severe disease progression, thereby reducing hospitalization and death rates even when infection occurs despite vaccination

Inventive Principle:

Principle #10Preliminary action

3Reliability

If compound of formula I is used, then viral load and symptom severity are reduced, but potential side effects from host cell factor interference may occur

Engineering Contradiction:

Improveantiviral efficacyVSAvoidside effects from host target interference

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modulates the activity parameters of host cell factors (eEF1A, PKR, UPR pathways) rather than completely inhibiting them. By changing the functional state or activity level of these factors rather than blocking them entirely, the compound achieves antiviral efficacy while maintaining physiological homeostasis and reducing potential side effects

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20230158102A1Compounds for use in the treatment of coronavirus infection

Publication Date: 2023.05.25 PHARMA MAR SA

AI summary

A compound of general formula (I) wherein X, Y, n, p, q, and R1-R17 take various meanings, for use in the treatment of Coronavirus infection.