Substituted Piperidyl-Propane-Thiols for CCR3 Modulation
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Solution Overview
Problem
Current agents for modulating chemokine receptor CCR-3 have significant side effects, limiting their effectiveness in treating inflammatory, infectious, and autoimmune diseases such as asthma and rheumatoid arthritis.
Innovation Solution
Development of novel substituted piperidyl-propane-thiols that act as CCR-3 modulators with reduced side effects, specifically designed to target and regulate chemokine receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current chemokine receptor CCR-3 modulating agents are used, then CCR-3 receptor activity is modulated, but significant side effects occur that limit treatment effectiveness
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of CCR-3 modulating agents through specific substitution patterns on the piperidyl-propane-thiol core. By changing parameters such as substituent types (R1-R6 groups), positions, and configurations, the invention achieves improved therapeutic profiles with reduced side effects while maintaining CCR-3 modulating activity. This is evident in the detailed structural variations presented in the patent that optimize both efficacy and safety parameters.
2Object-affected harmful factors
If novel substituted piperidyl-propane-thiols are developed to reduce side effects, then treatment safety improves, but compound complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the molecule into distinct functional modules: a core piperidyl-propane-thiol structure with separately defined substituent groups (R1-R6) at specific positions. This modular approach allows systematic optimization of each segment's properties to reduce side effects while maintaining overall tractability for synthesis and characterization. The segmented structure enables independent optimization of pharmacokinetic and pharmacodynamic properties.
Solution Approach 2:
The patent systematically varies structural parameters including substituent types, positions, and stereochemical configurations to optimize the balance between safety and complexity. By controlling which parameters are modified and which are held constant, the invention manages compound complexity while achieving the desired reduction in side effects through precise structural optimization.
3Adaptability or versatility
If CCR-3 modulators are used for treating inflammatory and autoimmune diseases, then therapeutic benefits are achieved, but the scope of application requires broad specificity
Solution Approach 1:
The patent applies universality by designing CCR-3 modulators with a core structure and substituent pattern that can address multiple inflammatory and autoimmune conditions (asthma, rheumatoid arthritis, atherosclerosis, etc.). The molecular architecture is optimized to provide broad therapeutic applicability while maintaining reliable CCR-3 receptor specificity through careful selection of substituents that preserve key binding interactions across different disease contexts.
Data Source
AI summary
One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and R4 are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.