Aryl Substituted Pyrimidines Inhibiting Influenza Replication
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Solution Overview
Problem
Current influenza treatments and vaccines face challenges due to rapid viral evolution, limited effectiveness in certain populations, and the emergence of resistant strains, necessitating a wider range of antiviral options to effectively combat influenza infections.
Innovation Solution
Development of compounds of formula (I), which can inhibit the replication of influenza viruses, are used in pharmaceutical compositions either alone or in combination with other antiviral agents or vaccines to treat and prevent influenza infections.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If neuraminidase inhibitors (oseltamivir or zanamivir) are used as primary antiviral agents, then effectiveness against influenza A and B viruses is improved, but development of resistance occurs during treatment
Solution Approach 1:
The patent employs a novel chemical structure (formula I) with specific molecular parameters including a pyrimidine core, heterocyclic substituent R2, and various functional groups (R1, Y, X) that differ from existing neuraminidase inhibitors. This structural parameter change creates a new class of antiviral agents with potentially different resistance profiles while maintaining effectiveness against both influenza A and B viruses.
2Reliability
If amantadine and rimantadine (amantadanes) are used for antiviral treatment, then activity against influenza A strains is achieved, but resistance increases rapidly worldwide
Solution Approach 1:
The patent introduces a completely different chemical structure (formula I) with a pyrimidine core and heterocyclic substituents, replacing the amantadane structure. This parameter change in molecular structure aims to achieve activity against influenza A strains while avoiding the rapid resistance development associated with amantadine and rimantadine.
3Reliability
If influenza vaccines are used for prevention, then protection against illness is provided, but effectiveness is limited in elderly populations and requires annual updates
Solution Approach 1:
The patent introduces antiviral compounds (formula I) as an intermediary therapeutic approach that can be used in combination with vaccines or as alternative treatment. This intermediary approach may provide broader protection including for elderly populations and does not require annual updates like vaccines, as it targets viral replication directly rather than relying on antigenic matching.
Data Source
AI summary
The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.