Chromen-2-one derivatives for balanced monoamine reuptake inhibition
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Solution Overview
Problem
Current Serotonin Selective Reuptake Inhibitors (SSRIs) for treating CNS disorders like depression and panic disorder have undesirable features, such as an unoptimized pharmacological profile for monoamine neurotransmitter reuptake, particularly the serotonin, dopamine, and noradrenaline reuptake ratio.
Innovation Solution
Development of chromen-2-one derivatives and their pharmaceutical compositions that act as monoamine neurotransmitter reuptake inhibitors, offering a balanced activity profile for serotonin, dopamine, and noradrenaline reuptake inhibition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If SSRIs are used to treat CNS disorders, then serotonin reuptake inhibition is achieved, but the ratio of serotonin to noradrenaline and dopamine reuptake activity is unoptimized
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of coumarin derivatives through systematic variation of substituents at different positions (R1-R6, R2'-R6') to optimize the pharmacological profile. This includes changing electronic properties, steric properties, and hydrophobicity to achieve balanced reuptake inhibition across multiple monoamine neurotransmitters while maintaining therapeutic efficacy
2Reliability
If existing SSRIs are used, then depression and panic disorder are treated, but tolerability and side effects are compromised due to unoptimized pharmacological profile
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns at different positions of the coumarin core structure to achieve selective optimization of pharmacological properties. Different substituent combinations (halogens, alkyl groups, alkoxy groups, cyano, nitro, amino) are placed at specific positions to fine-tune the balance between therapeutic efficacy and side effect profile for individual neurotransmitter systems
Data Source
AI summary
This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors.In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.