HCV Inhibitor Compounds Reducing Toxicity

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Solution Overview

Problem

Current HCV therapeutic agents face limitations due to toxicity and side effects, necessitating the development of new compounds with HCV inhibitory activity for effective treatment and diagnosis.

Innovation Solution

Development of specific compounds and their pharmaceutical compositions, including stereoisomers and physiologically acceptable salts, which can accumulate in human hepatic cells and inhibit HCV activity, along with novel synthetic processes and intermediates for preparing these compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If prior art HCV inhibitors are used, then HCV inhibitory activity is achieved, but toxicity and side effects increase

Engineering Contradiction:
ImproveHCV inhibitory activityVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of HCV inhibitors through specific molecular substitutions and modifications. The compounds feature altered functional groups and structural parameters compared to prior art inhibitors, which changes their interaction with HCV targets while reducing toxicity. This is achieved through systematic variation of molecular parameters in the compound structures disclosed in the patent.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating complex multi-component molecular structures that combine different functional groups and moieties. The HCV inhibitors are presented as composite chemical entities with multiple structural elements working together to achieve both viral inhibition and reduced toxicity. The compounds incorporate various substituents and functional groups in specific arrangements that provide both therapeutic activity and improved safety profile.

Inventive Principle:
Principle #40Composite materials

2Reliability

If new HCV therapeutic agents are developed, then efficacy against HCV is improved, but complexity of synthesis increases

Engineering Contradiction:
ImproveHCV therapeutic efficacyVSAvoidsynthetic process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the synthesis of complex HCV inhibitors into multiple discrete steps and intermediate compounds. The synthetic routes are broken down into manageable stages, each producing specific intermediates that are then combined or transformed in subsequent steps. This segmented approach to synthesis allows for better control and optimization of each individual reaction step while building toward the final complex therapeutic agent.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs preliminary action by preparing and characterizing intermediate compounds before final assembly of the therapeutic agents. The synthetic methodology includes pre-synthesis of key intermediates with defined structures and properties, which are then used in subsequent coupling or transformation reactions. This preliminary preparation of building blocks simplifies the overall synthetic process by organizing complexity into preparatory and final assembly phases.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP2162431B1Antiviral compounds
Publication Date: 2017.06.07 GILEAD SCIENCES INC
  • EP2162431B1 patent drawing
  • EP2162431B1 patent drawing
  • EP2162431B1 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.