Pyridine Compounds for Antiviral Specificity

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Solution Overview

Problem

Current antiviral compounds are ineffective in inhibiting enteroviruses, paramyxoviruses, respiratory viruses, flaviviridae viruses, bunyaviridae viruses, togaviridae viruses, and rabies, particularly in treating infections caused by these viruses in humans and animals, as they lack specificity and often result in off-target effects.

Innovation Solution

Development of a pharmaceutical composition containing a compound represented by Formula I, which includes a specific pyridine-containing structure, administered in effective amounts to treat infections by inhibiting viral replication and reducing symptoms associated with these viruses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current antiviral compounds are used to treat viral infections, then treatment coverage is provided, but the compounds lack specificity and cause off-target effects

Engineering Contradiction:
Improvespecificity of antiviral compoundsVSAvoidoff-target effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds with specific functional groups positioned at particular locations on the pyridine core structure. The substituents at positions 2, 4, 6 on the pyridine ring are carefully selected to interact with specific viral targets, ensuring that the antiviral activity is concentrated at the desired molecular interaction sites while minimizing interactions with off-target biological molecules.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying the chemical parameters of the pyridine-based compounds, including different substituents (R1, R2, R3, R4, R5, R6), their positions, and their chemical nature (halogen, alkyl, aryl, etc.). This systematic parameter optimization allows tuning of the compound's specificity and potency, enabling high-affinity binding to viral targets while reducing off-target effects through precise molecular characterization.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If broad-spectrum antiviral compounds are developed to cover multiple virus types, then treatment versatility is improved, but compound specificity decreases

Engineering Contradiction:
Improvetreatment coverage across virus typesVSAvoidcompound specificity
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent implements universality by designing a pyridine-based compound scaffold that can target multiple virus types through a common mechanism of action. The core pyridine structure with specific functional groups (such as hydroxylamine-O-sulfonate derivatives) provides a universal binding motif that interacts with conserved viral targets across different virus families, including picornaviruses, paramyxoviruses, and other RNA viruses, enabling broad-spectrum activity without sacrificing reasonable specificity.

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

Solution Approach 2:

The patent uses parameter changes to balance versatility and specificity by modifying the substituent parameters on the pyridine ring. Different substituent combinations allow the same core structure to adapt to slightly different viral targets while maintaining the fundamental binding mode, thus achieving broad coverage across virus types with controlled specificity through systematic structure-activity relationship optimization.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3687529B1Potent antiviral pyridine-containing compounds
Publication Date: 2023.07.12 RGT UNIV OF CALIFORNIA
  • EP3687529B1 patent drawing
  • EP3687529B1 patent drawing
  • EP3687529B1 patent drawing

AI summary

The present technology provides compounds according to Formula I: (I) expected to be useful in inhibiting an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus in a cell and/or treating subjects suffering from an enterovirus, paramyxovirus, respiratory virus, flaviviridae virus, bunyaviridae virus, togaviridae virus, or rabies virus.