Uridine Nucleoside Derivatives P2Y6 Receptor Modulation
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Solution Overview
Problem
There is a need for new ligands, such as agonists, that can effectively modulate P2Y6 receptor activity to treat neuronal disorders like neurodegeneration, traumatic brain injury, and pain, as existing treatments are inadequate.
Innovation Solution
Development of compounds of formulae I and II, which are P2Y6 receptor-modulating compounds that can activate the P2Y6 receptor, used in pharmaceutical compositions to treat various conditions including neurodegenerative disorders, traumatic CNS injury, pain, and inflammatory conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for neuronal disorders, then current therapeutic options are limited, but treatment effectiveness is inadequate
Solution Approach 1:
The patent segments the therapeutic approach by developing a series of compounds with different structural modifications (formulae I and II with various substituents), allowing selective targeting of P2Y6 receptor subtypes and different neuronal disorder manifestations, thereby providing both effective treatment and therapeutic versatility
Solution Approach 2:
The patent applies parameter changes by systematically varying chemical parameters (substituents R1-R8, ring structures A, linkers Y) in the compound molecules to optimize P2Y6 receptor binding affinity and selectivity, improving treatment effectiveness while maintaining structural adaptability for different clinical applications
2Reliability
If new P2Y6 receptor agonists are developed, then therapeutic benefits are improved, but compound complexity increases
Solution Approach 1:
The patent creates universal P2Y6 receptor agonists with core structural motifs that can be systematically modified to address different neuronal disorders (Alzheimer's, Parkinson's, traumatic brain injury, pain), achieving multi-functionality that improves therapeutic benefits without proportionally increasing complexity
Solution Approach 2:
The patent uses the P2Y6 receptor itself as an intermediary target, developing compounds that bind to this specific receptor to mediate therapeutic effects indirectly through receptor activation, which simplifies the approach compared to targeting multiple downstream pathways directly
Data Source
AI summary
This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.