Formula I Compounds Inhibit RNA Virus Replication

Solution Overview

Problem

Current treatments for viral diseases caused by RNA viruses, such as influenza and SARS-CoV-2, are inadequate in effectively preventing or treating these conditions.

Innovation Solution

A composition comprising compounds of Formula (I), including p-cymene and its derivatives, which are used to inhibit the reproduction of RNA viruses by binding to viral nucleoprotein or nucleocapsid proteins, thereby preventing the formation of the nucleoprotein-RNA complex and reducing viral RNA production.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If known treatments are used for RNA virus infections, then some therapeutic effect is achieved, but the treatment effectiveness remains inadequate

Engineering Contradiction:
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by designing compounds of Formula (I) that can inhibit multiple RNA viruses (influenza A, influenza B, SARS-CoV-2, MERS-CoV) through a common mechanism of action. The compounds bind to the nucleoprotein-RNA complex interface, a conserved target across different RNA viruses, enabling broad-spectrum activity from a single compound structure.

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

Solution Approach 2:

The patent employs parameter changes by modifying the chemical structure of p-cymene through systematic variation of substituents at positions R1, R2, R3, and R4 to optimize anti-viral potency and selectivity. This structure-activity relationship approach allows tuning of the compounds' effectiveness against different RNA viruses while maintaining the core mechanism of nucleoprotein binding.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If existing anti-viral drugs are administered, then viral replication is partially inhibited, but the reduction in viral load is insufficient

Engineering Contradiction:
Core Design Contradiction:
ProductivityVSQuantity of substance

Solution Approach 1:

The patent applies the extraction principle by specifically targeting and binding to the nucleoprotein-RNA complex, extracting or sequestering the viral nucleoprotein from the replication process. This prevents the nucleoprotein from performing its essential function in viral RNA synthesis and assembly, thereby reducing viral load more effectively than existing treatments.

Inventive Principle:
Principle #2Taking out (Extraction)

3Adaptability or versatility

If broad-spectrum anti-viral coverage is achieved, then multiple RNA viruses are targeted, but the mechanism of action remains insufficiently understood

Engineering Contradiction:
Core Design Contradiction:
Adaptability or versatilityVSDifficulty of detecting and measuring

Solution Approach 1:

The patent uses the nucleoprotein-RNA complex as an intermediary target that mediates the anti-viral effect across different virus types. By focusing on this conserved complex rather than virus-specific surface proteins, the compounds achieve broad-spectrum activity while the mechanism becomes more tractable for study through biochemical assays of nucleoprotein binding.

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compounds demonstrate significant anti-viral activity, as shown by reduced plaque formation, viral nucleoprotein concentration, and viral titer, offering a potential therapeutic solution for diseases caused by RNA viruses like influenza and SARS-CoV-2.

Implementation Method 1

inhibit the reproduction of RNA viruses by binding to viral nucleoprotein or nucleocapsid proteins, thereby preventing the formation of the nucleoprotein-RNA complex

Methodology Applied
Scientific EffectBinding: Chemical Bonding

Data Source

PatentUS20230101903A1Compounds useful as Anti-viral agents
Publication Date: 2023.03.30
  • US20230101903A1 patent drawing
  • US20230101903A1 patent drawing
  • US20230101903A1 patent drawing

AI summary

The present invention relates to compounds of Formula (I) and compositions containing one or more compounds of Formula (I). The compounds and compositions are useful as anti-viral agents and may be used in the treatment or prevention of diseases caused by ribonucleic acid (RNA) viruses.