Antiviral Compounds Inhibiting Paramyxovirus Replication

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Solution Overview

Problem

Current treatments for respiratory syncytial virus (RSV) infections, which are part of the Paramyxoviridae family, are limited, with no effective antibiotics or over-the-counter medications available, and existing treatments like nebulized bronchodilators only alleviate symptoms, while severe cases require specific medications like ribavirin by aerosol, which may not be universally effective.

Innovation Solution

Development of new antiviral compounds, specifically those of Formula (I) or their pharmaceutically acceptable salts, which can be administered to treat or prevent Paramyxovirus infections, including RSV, by inhibiting viral replication in infected cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If existing treatments like nebulized bronchodilators are used, then symptoms are alleviated, but the underlying viral infection is not treated

Engineering Contradiction:
Improvesymptom reliefVSAvoidinfection treatment effectiveness
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent extracts and targets the specific viral replication mechanism from the overall infection process. The compounds are designed to specifically inhibit the paramyxovirus replication machinery, separating the antiviral action from general symptom management, thereby treating the root cause rather than just symptoms

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The small molecule compounds of Formula (I) act as intermediary substances that block the interaction between the virus and host cell machinery during replication. These compounds mediate the inhibition of viral protein synthesis and replication without directly killing the virus, providing a targeted therapeutic effect

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If specific medications like ribavirin are used for severe cases, then treatment effectiveness may be improved, but universal effectiveness is not achieved

Engineering Contradiction:
Improvetreatment effectiveness for severe casesVSAvoiduniversal effectiveness across different paramyxoviruses
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The compounds of Formula (I) are designed with a core structure that targets a conserved mechanism across the Paramyxoviridae family. The molecular framework allows these compounds to function against multiple genera including henipavirus, morbillivirus, respirovirus, rubulavirus, pneumovirus, and metapneumovirus, providing universal effectiveness while maintaining reliability

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

Solution Approach 2:

The patent employs systematic variation of molecular parameters in the compounds of Formula (I) to optimize both potency and broad-spectrum activity. By modifying substituents R1 through R6 and the core structure, the compounds maintain effective inhibition across different paramyxoviruses while preserving reliable treatment effectiveness

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If no effective antibiotics or over-the-counter medications are available, then treatment options are limited, but developing new antiviral compounds requires significant research resources

Engineering Contradiction:
Improveavailability of treatment optionsVSAvoidresearch and development complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent segments the complex antiviral therapy development into manageable components by focusing on a specific molecular framework (Formula I) with defined substitutable positions. This segmentation allows systematic optimization of individual substituents while maintaining the core antiviral mechanism, reducing overall R&D complexity

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent utilizes systematic parameter changes in the molecular structure (substituents R1-R6) to generate multiple derivatives from a single core structure. This approach efficiently expands treatment options by creating a series of related compounds with potentially different pharmacokinetic profiles while sharing the same mechanism of action, reducing the need for entirely separate R&D programs

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS10358453B2Antiviral compounds
Publication Date: 2019.07.23 ALIOS BIOPHARMA INC
  • US10358453B2 patent drawing
  • US10358453B2 patent drawing
  • US10358453B2 patent drawing

AI summary

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).