Substituted CNS Compounds for Aggression and Mood Symptoms
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Solution Overview
Problem
There is a need for effective treatments for central nervous system (CNS) diseases and disorders such as depression, schizophrenia, and aggressive behavior in patients with Alzheimer's disease.
Innovation Solution
Development of substituted compounds and their pharmaceutically acceptable salts, which can be administered to treat CNS disorders, including compounds of Formula I, II, III, IV, IVf, and IVl, with specific structural variations in R1, R2, R3, R4, R5, R6, R7, and ring D, and their enantiomerically pure forms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments for CNS disorders are used, then some therapeutic effect may be achieved, but they fail to effectively reduce aggressive behavior and improve social interactions in patients with Alzheimer's disease and other CNS disorders
Solution Approach 1:
The patent employs parameter changes by systematically varying molecular parameters (substituents R1-R7, ring structures A-D, linkers) to optimize the therapeutic compound's effectiveness. This allows the same compound structure to be adapted for treating multiple CNS disorders including Alzheimer's disease, depression, and schizophrenia, thereby resolving the contradiction between reliable therapeutic effect and adaptability across different disorders
2Reliability
If new compound structures are developed to improve therapeutic effects, then efficacy in animal models is enhanced, but the complexity of compound synthesis and characterization increases
Solution Approach 1:
The patent applies segmentation by dividing the complex molecule into distinct functional modules (core structure with rings A-D, substituents R1-R7, and linkers). This modular approach allows systematic optimization of therapeutic efficacy while managing synthesis complexity through standardized building blocks that can be independently characterized and assembled
Solution Approach 2:
The patent uses parameter changes by systematically varying specific molecular parameters (types of substituents at R1-R7 positions, saturation of rings, linker length) to achieve desired therapeutic effects. This structured parameter variation enables methodical optimization without exponentially increasing overall complexity, as changes are made to discrete parameters rather than the entire molecular structure
Data Source
AI summary
Disclosed herein are substituted compounds, salts, and pharmaceutical formulations thereof, for the treatment of a central nervous system disease or disorder.