HCV Inhibitor Compounds Oral Protease Inhibition

Solution Overview

Problem

Current treatments for hepatitis C virus (HCV) infections, such as those using interferon and pegylated interferon, induce severe side effects and there is a need for a safe, oral drug alternative.

Innovation Solution

Development of compounds of Formula (I), which inhibit HCV replication, and their use in pharmaceutical compositions for treating HCV infections, including processes for preparing these compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If interferon or pegylated interferon is used to treat HCV infection, then HCV replication is inhibited, but severe side effects occur

Engineering Contradiction:

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical structure parameters by developing novel compounds with a specific molecular framework (Formula I) that differs fundamentally from interferon proteins. This structural parameter change allows the compound to inhibit HCV replication through a different mechanism while avoiding the side effects associated with interferon therapy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent replaces the protein-based interferon mechanism with a small molecule compound mechanism. The compounds of Formula (I) act as protease inhibitors with a different mode of action compared to interferon, substituting the biological protein system with a chemically synthesized molecule system that achieves similar antiviral effects without the same toxicity profile

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Reliability

If injectable interferon is used to treat HCV infection, then HCV replication is inhibited, but treatment convenience is reduced

Engineering Contradiction:

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the administration route parameter by designing compounds suitable for oral administration rather than injection. The compounds of Formula (I) are developed with pharmacokinetic properties that enable oral bioavailability, transforming the administration method from parenteral (injectable) to enteral (oral), thereby significantly improving treatment convenience

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compounds effectively inhibit HCV replication, providing a safer and more effective treatment option for hepatitis C without the severe side effects associated with existing therapies.

Implementation Method 1

WO 2005/035525 describes compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease

Methodology Applied

Scientific EffectProtease inhibition: Enzyme

Data Source

PatentEP1906945B1HCV inhibitors

Publication Date: 2015.08.05

AI summary

The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.