Bis-amide Compounds Inhibiting SARS-CoV-2

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Solution Overview

Problem

There is an urgent need for effective treatments against SARS-CoV-2, as current therapies are inadequate for addressing the severe acute respiratory syndrome caused by this virus, particularly given its rapid evolution and high mortality rates.

Innovation Solution

Development of novel bis-amide compounds that inhibit SARS-CoV-2, specifically described by their chemical formulae and structures, which can be administered as pharmaceutical compositions to treat severe acute respiratory syndrome.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used against SARS-CoV-2, then treatment availability is maintained, but treatment effectiveness is inadequate due to the virus's rapid evolution and high mortality rates

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidvirus evolution resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by developing a series of bis-amide compounds with systematically varied molecular structures (different R groups, linkers, and substitutions) to optimize antiviral activity. This approach allows tuning of compound properties to effectively counter evolving viral strains while maintaining reliable treatment outcomes.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel bis-amide compounds are developed to inhibit SARS-CoV-2, then treatment effectiveness is improved, but development complexity and time are increased

Engineering Contradiction:
Improveantiviral activityVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The bis-amide compounds are designed with segmented modular structures consisting of distinct functional domains (R1, R2, R3, R4 groups and linkers). This segmentation allows independent optimization of each module for antiviral activity while simplifying the overall development process through systematic combination of proven structural elements.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The core bis-amide structure serves multiple functions: it provides the fundamental antiviral mechanism while allowing diverse substituent groups to target different viral proteins or entry pathways. This multi-functionality enables a single compound class to address multiple aspects of SARS-CoV-2 pathogenesis and adapt to viral evolution.

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

3Reliability

If novel bis-amide compounds are developed to inhibit SARS-CoV-2, then treatment effectiveness is improved, but development time and resource investment are increased

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoiddrug development time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent performs preliminary action by conducting extensive in silico screenings and in vitro validations of bis-amide compounds before clinical development. This advance preparation of compound libraries and preliminary efficacy data reduces the time required for later development stages while ensuring therapeutic effectiveness is established early in the process.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS20240409510A1Compounds for the treatment of sars
Publication Date: 2024.12.12 PURDUE RES FOUND
  • US20240409510A1 patent drawing
  • US20240409510A1 patent drawing
  • US20240409510A1 patent drawing

AI summary

Bis-amide inhibitors of SARS-CoV-2 (COVID), compositions, and methods of treating a severe acute respiratory syndrome.