Antiviral Compounds Targeting Viral mRNA Export and Processing

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Solution Overview

Problem

Current antiretroviral therapies for HIV/AIDS, such as HAART, have low specificity, are highly toxic, expensive, and do not address the issue of HIV reservoirs in resting T cells, while stilbene-based compounds like 5350150 face photolabile/toxic properties, limiting their anti-HIV efficacy.

Innovation Solution

Development of compounds that interfere with the processing and export of viral mRNAs from the nucleus to the cytoplasm, inhibiting HIV, adenovirus, and coronavirus replication, using structures represented by Formulas I and II with various substituents to enhance specificity and reduce toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If HAART is used to treat HIV/AIDS, then viral load is reduced and CD4+ T cells are replenished, but the treatment has low specificity, is highly toxic and expensive

Engineering Contradiction:

Improveeffectiveness in reducing viral loadVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds that specifically target nuclear RNA processing mechanisms unique to viral replication, rather than broadly inhibiting multiple viral proteins as HAART does. The compounds concentrate their action on specific cellular processes (RNA splicing, polyadenylation, export) that are critical for viral but not cellular survival, achieving high local specificity at the molecular level.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent uses host cell RNA processing factors as intermediaries to achieve antiviral effects. Instead of directly targeting viral enzymes, the compounds modulate host factors (SR proteins, hnRNPs, RNA polymerase II) that the virus depends on for replication. This intermediary approach allows the virus to be inhibited while sparing direct viral targets, reducing the need for multiple drugs and lowering toxicity.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If HAART is used to treat HIV/AIDS, then viral replication is suppressed, but it does not address the problem of HIV reservoir where dormant virus may reside in resting T cells

Engineering Contradiction:

Improvesuppression of active viral replicationVSAvoidability to address dormant virus reservoirs

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies preliminary action by interfering with RNA processing early in the viral replication cycle, before viral proteins are assembled and before integration into the host genome. By blocking RNA splicing, polyadenylation, or nuclear export at these early stages, the compounds prevent the formation of new viral particles and may also affect latent reservoirs that depend on ongoing RNA processing for maintenance or reactivation.

Inventive Principle:

Principle #10Preliminary action

3Reliability

If stilbene-based compound 5350150 is used to block HIV replication, then HIV mRNA export from nucleus to cytoplasm is interfered with, but the compound has photolabile/toxic properties that limit therapeutic potential

Engineering Contradiction:

Improveinhibition of HIV replicationVSAvoidphotolabile/toxic properties

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of stilbene-based compounds to eliminate photolabile properties. The inventors changed key structural parameters (replacing the central stilbene double bond with single bonds, modifying aromatic rings, adjusting substituent positions) while preserving the ability to interfere with mRNA export. This structural parameter optimization maintains antiviral activity while removing toxic side effects.

Inventive Principle:

Principle #35Parameter changes

4Reliability

If compounds are designed to interfere with RNA processing of HIV and adenovirus, then viral replication is inhibited, but the mechanism requires modification of cellular proteins involved in regulating RNA processing

Engineering Contradiction:

Improveinhibition of viral replicationVSAvoidcomplexity of modulating cellular protein mechanisms

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies universality by designing compounds that target conserved RNA processing mechanisms shared across different viruses (HIV, adenovirus, coronavirus). The host RNA processing factors (SR proteins, hnRNPs, spliceosomes, polyadenylation complexes) are universal machinery used by multiple viruses, so a single compound class can inhibit diverse viruses by interfering with these common cellular processes, reducing the complexity of developing virus-specific therapies.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS12622896B2Antiviral compounds, compositions and methods of use

Publication Date: 2026.05.12 SOCIETE DE COMMERCIALISATION DES PRODUITS DE LA RECHERCHE APPLIQUEE SOCPRA ET HUMAINES S E C

AI summary

Provided herein are antiviral compounds having the structure of Formula (I) and compositions thereof for use in the treatment of viral infection. In particular, the compounds of Formula (I) are capable of interfering with the export of viral mRNA processing as reflected in the altered accumulation of viral RNA isoforms as well as transport from the nucleus to the cytoplasm. Such compounds show a reduction of HIV, adenovirus and coronavirus infection of cells. The invention provides compounds that may be suitable for the treatment of HIV/AIDS.