Benzofurazan Compounds Inhibit Amyloid Aggregation
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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
Engineering 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
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.
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.
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
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.
Data Source
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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.