Diaryl Thioether Piperazine Compounds for Sustained Release
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Solution Overview
Problem
Current treatments for major depressive disorder, such as vortioxetine, require daily administration and have limitations in sustained release, leading to inconvenient dosing frequencies for patients.
Innovation Solution
Development of diaryl thioether piperazine compounds, specifically represented by Formulas (I) and (II), which exhibit good pharmacokinetic properties and low solubility, allowing for slow release and prolonged efficacy, potentially reducing administration frequency.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If vortioxetine is used for treatment, then antidepressant efficacy is achieved, but administration frequency must be daily which reduces convenience
Solution Approach 1:
The patent modifies the chemical structure of vortioxetine by introducing a piperazine ring with specific substituents (Formula I) to change the pharmacokinetic parameters of the drug. This structural modification extends the half-life and duration of action, enabling less frequent dosing while maintaining antidepressant efficacy
Solution Approach 2:
The patent creates a composite molecular structure combining vortioxetine's core pharmacophore with a piperazine moiety and various substituents. This composite structure achieves both the desired antidepressant activity and improved sustained-release properties through the synergistic effects of different molecular components
2Duration of action of moving object
If drug is designed for slow release, then sustained release effect is improved, but solubility decreases which may affect absorption
Solution Approach 1:
The patent introduces different functional groups at specific positions of the piperazine ring to create local variations in molecular properties. The hydrophobic substituents (aryl groups, alkyl chains) at certain positions provide slow-release characteristics, while other positions maintain polarity for adequate solubility and absorption
Solution Approach 2:
The patent creates multiple analogues (Formula I compounds with different substituents) that copy the core pharmacophore structure of vortioxetine while modifying peripheral groups. These analogues maintain the essential drug-receptor interaction capabilities while achieving improved pharmacokinetic profiles including sustained release and adequate solubility
Data Source
AI summary
The invention relates to a diaryl thioether piperazine compound, a preparation method and use thereof. Specifically, the compound is a compound of Formula (I), wherein HX is C10-20 fatty acid or pamoic acid.