Diarylhydantoin Compounds for Receptor Modulation
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Solution Overview
Problem
Current therapies for Parkinson's disease, Alzheimer's disease, and prostate cancer lack effective treatments, with a need for new therapies that can target these conditions specifically and improve treatment outcomes.
Innovation Solution
Development of diarylhydantoin and diarylthiohydantoin compounds, including their metabolites, which act as receptor modulators to effectively treat these diseases by modulating the norepinephrine transporter, progesterone receptor, and sigma receptor, among others, and are administered in pharmaceutical compositions to achieve therapeutic effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used for Parkinson's disease, Alzheimer's disease, and prostate cancer, then treatment is provided, but effective treatment outcomes are not achieved
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of hydantoin compounds through specific substitutions at positions R1, R2, R3, R4, R5, and R6 with various functional groups (halogens, alkyl groups, aryl groups, heteroaryl groups, etc.). These structural parameter changes create compounds with enhanced binding affinity and selectivity for target receptors, thereby improving treatment effectiveness for Parkinson's disease, Alzheimer's disease, and prostate cancer compared to existing therapies.
2Reliability
If new therapies are developed to target specific diseases, then treatment effectiveness is improved, but device complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the complex medicinal chemistry problem into systematic components: (1) core hydantoin structure, (2) six substitutable positions (R1-R6), (3) five categories of acceptable groups for each position, and (4) specific metabolite patterns. This segmented approach allows for rational drug design where each position can be independently optimized for specific therapeutic targets while maintaining overall molecular stability and drug-like properties.
Solution Approach 2:
The patent applies universality by creating a platform compound structure that can target multiple disease indications through selective substitution patterns. The same core hydantoin scaffold with systematic variations can address Parkinson's disease (dopamine pathway), Alzheimer's disease (acetylcholine pathway), and prostate cancer (hormonal pathway), making the compound class multi-functional across different therapeutic areas.
Data Source
AI summary
Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.