Peptidic Compounds for SARS-CoV-2 Protease Inhibition
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for SARS-CoV-2 infections lack effective alternatives, with existing drugs showing promise in vitro but not in human patients, and there is a need for new therapeutic options to address the ongoing COVID-19 pandemic.
Innovation Solution
Development of specific peptidic compounds, as defined by formula (I), which can be administered alone or in combination with other compounds to treat or prevent infections by enveloped viruses, particularly SARS-CoV-2, utilizing solid phase peptide synthesis and preferred protecting groups for peptide stabilization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing drugs (remdesivir, chloroquine, hydroxychloroquine) are used to treat SARS-CoV-2 infections, then viral inhibition is achieved in vitro, but proven efficiency in human patients is not demonstrated
Solution Approach 1:
The invention segments the treatment approach by developing a library of individual peptidic compounds with specific sequences and structures, rather than relying on a single existing drug. Each peptide is designed to target viral proteases, creating multiple specialized agents that can be selected and optimized for human treatment based on clinical results.
Solution Approach 2:
The invention changes the chemical parameter space by transitioning from small molecule drugs to peptidic compounds with specific amino acid sequences. The peptides incorporate non-natural amino acids and modified backbones that enhance stability and activity, representing a fundamental parameter change in drug chemistry that enables both viral inhibition and clinical efficacy.
2Reliability
If peptidic compounds are designed to inhibit viral proteases, then antiviral activity is enhanced, but compound stability and selectivity challenges arise
Solution Approach 1:
The invention uses disposable-like transient peptidic inhibitors that bind to and inhibit viral proteases during the infection process. These peptides are designed to be effective during their functional lifetime in treating the infection, with their stability optimized for therapeutic use rather than long-term storage, balancing antiviral activity with practical stability requirements.
Solution Approach 2:
The peptides are constructed as composite structures combining natural amino acids with non-natural amino acids and modified backbones. This composite approach enhances both antiviral activity through specific protease binding and stability through chemical modifications that resist degradation, solving the contradiction between activity and stability.
3Adaptability or versatility
If broad-spectrum antiviral compounds are developed, then coverage of different enveloped viruses is improved, but specificity and off-target effects may increase
Solution Approach 1:
The invention creates universally applicable peptidic compounds that can inhibit multiple enveloped viruses by targeting a conserved functional element - the viral protease active site. The peptides are designed with specificity for the protease mechanism rather than virus-specific features, enabling broad-spectrum activity against coronaviruses and other enveloped viruses while maintaining selectivity through precise protease binding.
Solution Approach 2:
The peptidic compounds act as intermediary molecules that bridge the treatment approach between virus-specific therapies and broad-spectrum antivirals. By targeting the conserved protease function rather than virus-specific surface proteins, the peptides provide intermediary-level specificity that achieves broad coverage while minimizing off-target effects through mechanism-based selectivity.
Data Source
AI summary
The present invention relates to a compound of the following formula (I):or a pharmaceutically acceptable salt thereof,for use in a method for preventing or treating an infection by an enveloped virus in an individual.