Formula I Compounds Inhibiting Norovirus and Coronavirus Replication

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Solution Overview

Problem

Current treatments lack effective inhibitors for norovirus and coronavirus replication, necessitating the development of compounds that can safely and effectively inhibit these viruses in biological samples and patients.

Innovation Solution

Compounds of Formula (I) and their pharmaceutically acceptable salts are administered to patients, which are designed to inhibit the replication of noroviruses and coronaviruses, reducing their viral load and treating infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for norovirus and coronavirus infections, then patient safety is maintained with existing therapies, but effective inhibition of viral replication is not achieved

Engineering Contradiction:
Improveeffectiveness of viral replication inhibitionVSAvoidviral load in patients
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs parameter changes by modifying chemical structures (Formula I with various substituents R1-R7, n-m-o parameters) to optimize antiviral activity. The compounds systematically vary structural parameters to enhance inhibition of viral replication while maintaining safety, directly addressing the contradiction between effectiveness and viral load reduction.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new compounds are developed to inhibit viral replication, then effectiveness against norovirus and coronavirus is improved, but development complexity and time increase

Engineering Contradiction:
Improveantiviral efficacyVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent achieves universality by designing compounds of Formula I that can inhibit multiple viruses (norovirus, coronavirus, and potentially other RNA viruses) through a common mechanism. The core structure with variable substituents provides broad-spectrum antiviral activity, reducing the need for separate treatments for different viruses and simplifying therapeutic approaches.

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

Solution Approach 2:

The compound structure is segmented into a core framework (Formula I) with interchangeable substituent groups (R1-R7). This modular design allows systematic optimization of antiviral activity while maintaining a consistent base structure, facilitating drug development and reducing overall complexity compared to creating entirely new compounds for each virus.

Inventive Principle:
Principle #1Segmentation

3Reliability

If high concentrations of antiviral compounds are administered, then viral replication inhibition is enhanced, but potential side effects and toxicity increase

Engineering Contradiction:
Improveviral load reductionVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by introducing specific substituent groups (R1-R7) at particular positions on the core molecular structure to enhance antiviral activity at the viral replication site while minimizing systemic toxicity. The localized structural modifications allow optimization of therapeutic index by targeting viral enzymes specifically without affecting host cell functions.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20230159453A1Inhibitors of norovirus and coronavirus replication
Publication Date: 2023.05.25 COCRYSTAL PHARMA INC
  • US20230159453A1 patent drawing
  • US20230159453A1 patent drawing
  • US20230159453A1 patent drawing

AI summary

Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a vims infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.