Stilbene Derivatives for Protein Aggregation in CNS Disorders
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Solution Overview
Problem
There are no known effective treatments or cures for neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and prion diseases, and existing treatments for protein aggregation-related diseases are limited.
Innovation Solution
Development of stilbene derivatives and pharmaceutical compositions containing therapeutically effective amounts of these compounds for administering to patients to treat ocular diseases, neurological disorders, and protein aggregation-related diseases, including neurodegenerative disorders like Alzheimer's and Parkinson's disease.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If no treatment is administered, then existing treatments cannot be applied, but protein aggregation and neurodegenerative diseases progress unchecked
Solution Approach 1:
The patent converts the harmful effect of protein aggregation into a beneficial diagnostic and therapeutic opportunity by designing compounds that specifically bind to aggregated proteins (amyloid-beta, alpha-synuclein, prion proteins). The stilbene derivatives and related compounds bind to these aggregated proteins, transforming the harmful aggregation process into a detectable and treatable state, thereby addressing both the harmful factor and treatment effectiveness contradiction
Solution Approach 2:
The patent introduces small molecule compounds (stilbene derivatives, amino-substituted acrylonitrile derivatives, 2-cyano-acrylic acid derivatives) as intermediary substances that mediate between the aggregated proteins and the therapeutic effect. These compounds act as mediators that bind to aggregated proteins, prevent further aggregation, and facilitate clearance, thereby resolving the contradiction between untreated progression and effective treatment
2Ease of operation
If existing treatments are used, then some symptomatic relief may be achieved, but no cure or prevention exists for neurodegenerative diseases
Solution Approach 1:
The patent employs preliminary action by designing compounds that can prevent protein aggregation before it leads to irreversible neurodegenerative damage. The stilbene derivatives and related compounds are formulated to bind to and stabilize proteins in their native state, preventing misfolding and aggregation in the early stages, thereby enabling prevention and potential cure rather than just symptomatic treatment
Solution Approach 2:
The patent applies parameter changes by modifying the chemical structure of the compounds to optimize their binding affinity and specificity for aggregated proteins. The stilbene core structure with various substituents (cyano groups, amino groups, aromatic rings) is systematically modified to change parameters such as binding strength, selectivity, and pharmacokinetic properties, thereby transforming available treatments into curative therapies
Data Source
AI summary
The present application discloses stilbene derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.