Antiviral Compounds Targeting HCV Genotypes

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Solution Overview

Problem

Current hepatitis C virus (HCV) therapeutic agents have limited effectiveness due to toxicity and side effects, and there is a need for broad-spectrum agents that are less susceptible to viral resistance, particularly against HCV genotypes 1a, 1b, 2a, 3a, and 4a.

Innovation Solution

A compound of formula (I) is developed, comprising specific structural elements such as E1a-V1a—C(═O)—P1a—W1a—P1b—C(═O)—V1b-E1b, where various substituents and functional groups are defined, forming a molecular structure designed to target HCV effectively while minimizing resistance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current HCV therapeutic agents are used, then liver disease treatment is achieved, but toxicity and side effects occur that limit usefulness

Engineering Contradiction:
ImproveeffectivenessVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies chemical parameters of HCV inhibitors by introducing specific substituent groups (E1a, E1b, V1a, V1b, P1a, P1b, W1a) at defined positions in the molecular structure, changing the chemical composition to achieve broad-spectrum activity against multiple HCV genotypes while reducing toxicity and side effects

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite molecular structures combining multiple functional groups and substituent patterns in a single inhibitor molecule, designed to target conserved regions across different HCV genotypes (1a, 1b, 2a, 3a, 4a) simultaneously, achieving broad-spectrum efficacy with improved safety profile

Inventive Principle:
Principle #40Composite materials

2Reliability

If HCV inhibitors are used, then establishment and progression of infection is limited, but viral resistance develops

Engineering Contradiction:
Improveinfection controlVSAvoidviral resistance susceptibility
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent designs inhibitors with multiple substituent configurations (E1a, E1b, V1a, V1b, P1a, P1b, W1a) that can bind to conserved regions across diverse HCV genotypes, creating multi-functional agents that prevent viral replication while reducing the likelihood of resistance mutations emerging

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

Data Source

PatentUS10344019B2Antiviral compounds
Publication Date: 2019.07.09 GILEAD SCIENCES INC
  • US10344019B2 patent drawing
  • US10344019B2 patent drawing
  • US10344019B2 patent drawing

AI summary

The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.