Picolinic Acid Antiviral Entry Inhibition

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Solution Overview

Problem

Current antiviral therapies lack broad-spectrum effectiveness against multiple viral infections, particularly those caused by enveloped viruses, and often lead to the development of drug resistance.

Innovation Solution

The use of picolinic acid or its salts/derivatives to inhibit the entry of enveloped viruses into host cells, thereby preventing viral infections across various virus families.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If pathogen-specific antivirals are used to target one or more components directly associated with the virus life cycle, then antiviral activity is achieved against specific viruses, but the spectrum of activity is limited to closely related viruses within the same virus family

Engineering Contradiction:
Improveantiviral activityVSAvoidspectrum of activity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies host-targeting drugs that can inhibit multiple virus families through a common mechanism. The compound targets host cellular processes (such as endocytosis or membrane fusion) that are universally exploited by enveloped viruses, thereby achieving broad-spectrum antiviral activity against diverse virus families including coronaviruses, influenza viruses, and other enveloped viruses, rather than being limited to a single virus family.

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

2Adaptability or versatility

If nucleoside analogues such as cidofovir, favipiravir and ribavirin are used to achieve broad-spectrum antiviral activity, then effectiveness against multiple viruses is improved, but the risk of developing antiviral resistance increases mainly among RNA viruses

Engineering Contradiction:
Improvespectrum of activityVSAvoidrisk of resistance
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent uses host-targeting compounds as intermediaries that do not directly interact with viral components but rather disrupt essential host cellular processes that viruses exploit for entry and replication. By targeting host mechanisms (such as endocytic pathways or membrane fusion proteins) rather than viral nucleoside analogues, the approach avoids direct selective pressure on viral genomes, thereby minimizing the development of antiviral resistance while maintaining broad-spectrum efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If host-targeting drugs are used to minimize the risk of virus-drug resistance, then the spectrum of activity against multiple viruses is improved, but the mechanism of action becomes more complex

Engineering Contradiction:
Improverisk of resistanceVSAvoidmechanism of action
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the antiviral mechanism into distinct functional steps: (1) the host-targeting compound binds to or interacts with a specific host cellular component, (2) this interaction disrupts a specific host process (such as endocytosis or membrane fusion), and (3) the disruption prevents viral entry or early replication. This segmentation allows for a clearer understanding of the complex mechanism while maintaining the advantage of broad-spectrum activity and reduced resistance risk.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS12268676B2Antiviral applications of picolinic acid and its derivatives
Publication Date: 2025.04.08 INDIAN INSTITUTE OF SCIENCE
  • US12268676B2 patent drawing
  • US12268676B2 patent drawing
  • US12268676B2 patent drawing

AI summary

The present disclosure provides methods for inhibiting entry of a virus into a host cell using picolinic acid or a salt or derivative thereof. The present disclosure also provides methods for treating or preventing a viral infection in a subject by administering picolinic acid or a salt or derivative thereof. In particular, the methods of the present disclosure are effective for enveloped viruses and syncytium-forming viruses. In some embodiments, the present disclosure provides methods of treating or preventing a SARS CoV-2, Influenza A virus, human parainfluenza virus, herpes simplex virus, Japanese encephalitis virus, Zika virus, or a flavivirus infection.