Formula I Compounds for Hepatitis C Viral Elimination

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Solution Overview

Problem

Current treatments for hepatitis C virus (HCV) infection are limited by the lack of effective vaccines and therapies, with genotype 1 being particularly difficult to treat and existing treatments having poor efficacy and severe side effects.

Innovation Solution

Development of novel compounds of formula I, which are effective against HCV, including pharmaceutically acceptable salts, that target specific mechanisms of action, inhibition efficacy, and safety profiles, potentially used in combination with other antiviral agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If pegylated alpha-interferon and ribavirin combination therapy is used to treat HCV, then viral elimination is achieved for approximately 50% of genotype 1 patients, but severe side effects occur and treatment response is poor

Engineering Contradiction:
Improveviral elimination rateVSAvoidsevere side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing compounds with modified chemical structures (formula I with various substituents R1-R7) that alter the pharmacological properties compared to existing interferon and ribavirin therapies. This structural modification aims to achieve comparable or improved antiviral efficacy while reducing the severe side effects associated with conventional treatment parameters

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating complex molecular structures that combine multiple functional groups and substituents in a single compound framework. These composite chemical structures are designed to achieve multi-target antiviral activity against HCV while improving the safety profile compared to simple monotherapies

Inventive Principle:
Principle #40Composite materials

2Reliability

If genotype 1 HCV is treated with current therapies, then some viral elimination is achieved, but treatment difficulty remains high with only 50% sustained virologic response

Engineering Contradiction:
Improvesustained virologic responseVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts the essential antiviral activity from complex combination therapies by developing single compounds (formula I) that can target multiple viral mechanisms simultaneously. This extraction approach simplifies the treatment regimen while maintaining or improving efficacy against difficult-to-treat genotype 1 HCV

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent applies universality by designing compounds with multiple substituents and functional groups that enable a single agent to perform multiple antiviral functions. These multi-functional compounds aim to address various stages of the HCV lifecycle, providing broad-spectrum activity against genotype 1 and potentially other genotypes

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

Data Source

PatentUS9422311B2Compounds for the treatment of hepatitis C
Publication Date: 2016.08.23 BRISTOL MYERS SQUIBB CO
  • US9422311B2 patent drawing
  • US9422311B2 patent drawing
  • US9422311B2 patent drawing

AI summary

The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.