Hepatitis C Compound Formula I Targeting Viral Proteases

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for Hepatitis C virus (HCV) infection, particularly with combinations of pegylated alpha-interferon and ribavirin, do not achieve sustained viral load reduction in a significant fraction of patients, highlighting a need for more effective therapeutic options.

Innovation Solution

Development of specific compounds of formula I, which include various substituents and functional groups, potentially targeting viral proteases or replication processes of HCV, offering a new approach to inhibit viral replication or processing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If combination therapy with pegylated alpha-interferon and ribavirin is used, then treatment coverage is improved, but sustained viral load reduction is not achieved in substantial fraction of patients

Engineering Contradiction:
Improvetreatment efficacyVSAvoidviral load reduction
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines pegylated alpha-interferon and ribavirin into a single tablet formulation, merging two separate therapeutic agents into one integrated product that delivers both drugs simultaneously with controlled release mechanisms

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent introduces a novel excipient or delivery system that acts as an intermediary to enhance the interaction between interferon and ribavirin, improving their synergistic effect and sustained release profile

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If current standard therapy is administered, then treatment is provided to patients, but a substantial fraction do not achieve sustained reduction in viral load

Engineering Contradiction:
Improvetreatment accessibilityVSAvoidviral load reduction
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent segments the treatment regimen into controlled-release phases, with the tablet delivering interferon and ribavirin at different rates or at different times to maintain optimal therapeutic levels throughout the treatment cycle

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent modifies the physical or chemical parameters of the drug delivery system, such as using pH-sensitive or enzyme-sensitive linkers that change release characteristics based on physiological conditions, thereby improving sustained viral load reduction

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS8143243B2Compounds for the treatment of hepatitis C
Publication Date: 2012.03.27 BRISTOL MYERS SQUIBB CO
  • US8143243B2 patent drawing
  • US8143243B2 patent drawing
  • US8143243B2 patent drawing

AI summary

The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.