Benzofurazan Compounds Inhibit Amyloid Aggregation

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current medical practices have no effective therapy or treatment to halt or reverse the aggregation of amyloid deposits in diseases like Alzheimer's, Parkinson's, Huntington's, and prion diseases, making these conditions invariably fatal.

Innovation Solution

Development of compounds of Formula I, or their pharmaceutically acceptable salts, which inhibit amyloid aggregation, specifically designed for administration to inhibit amyloid protein aggregation in various amyloidosis conditions, including Alzheimer's, Parkinson's, Huntington's, and prion diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current medical practices are used, then existing treatments can be administered, but they cannot halt or reverse amyloid aggregation making diseases invariably fatal

Engineering Contradiction:
Improveeffectiveness of therapyVSAvoidamyloid aggregation
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces benzofurazan compounds as intermediary substances that mediate between amyloid proteins and prevent their aggregation. These compounds act as molecular mediators that interfere with the aggregation process, blocking the formation of harmful amyloid deposits without requiring direct modification of the amyloid proteins themselves.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical parameters of the system by introducing specific benzofurazan compounds with varying substituents (R1, R2, R3, R4, R5, R6) to optimize their ability to inhibit amyloid aggregation. By modifying molecular structure parameters such as substituent types and positions, the compounds' efficacy in preventing aggregation is enhanced.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If no effective treatment exists for amyloidosis, then current medical practice continues, but the condition remains invariably fatal with no ability to halt or reverse aggregation

Engineering Contradiction:
Improvetherapeutic approachVSAvoidtreatment outcome
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The benzofurazan compounds are designed with universal applicability across multiple amyloidosis conditions including Alzheimer's, Parkinson's, and other amyloid-related diseases. The core benzofurazan structure with variable substituents provides a versatile platform that can target different amyloid proteins, making the therapeutic approach adaptable to various disease states while maintaining reliable aggregation inhibition.

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

Data Source

PatentEP2888252B1Benzofurazan Anti-amyloid compounds and methods
Publication Date: 2017.06.07 TREVENTIS CORP
  • EP2888252B1 patent drawingFigure 1
  • EP2888252B1 patent drawingFigure 2
  • EP2888252B1 patent drawingFigure 3

AI summary

In general, among other things, compounds of Formula I are provided: in which R11 is selected from the group consisting of benzylamino, N-methylbenzylamino, morpholino, thiomorpholino, pyrrolidino, etc.; R13 is selected from the group consisting of 3-(1-ethanol-2-yl)phenyl, 3-(1-ol-2,2,2-trifluoroethan-2-yl)phenyl, 2-(1-ol-2,2,2-trifluoroethan-2- yl)phenyl, etc.; and R12 and R14 are each independently hydrogen or alkyl. Methods of treatment are also provided.