Selective Muscarinic Modulators for Myopia Eye Growth Control
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Solution Overview
Problem
Current treatments for excessive eye growth, such as myopia, are inadequate as they only correct refractive errors without addressing the underlying cause, and non-selective muscarinic antagonists like atropine cause side effects.
Innovation Solution
Development of azabicyclo derivatives that act as muscarinic modulators to treat or prevent excessive eye growth by administering effective amounts of these compounds, which are formulated into pharmaceutical compositions suitable for ophthalmic or intravitreal administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If non-selective muscarinic antagonists like atropine are used to treat excessive eye growth, then the treatment effectiveness is improved, but side effects such as mydriasis and blurring of near vision worsen
Solution Approach 1:
The patent applies local quality by developing muscarinic modulators with selective activity for specific muscarinic receptor subtypes (M1, M3, M4, or M5) rather than non-selective antagonism. This selectivity allows the drug to act on specific receptors in the eye responsible for controlling eye growth while avoiding activation of other subtypes that cause side effects like mydriasis and cycloplegia, thereby achieving localized therapeutic effect with reduced harmful consequences.
Solution Approach 2:
The patent inverts the traditional approach by using muscarinic modulators that can be agonists, partial agonists, or antagonists depending on the specific subtype, rather than relying solely on non-selective antagonism. This inverted strategy allows for fine-tuned control of receptor activity to achieve therapeutic benefits while minimizing adverse effects.
2Manufacturing precision
If corrective lenses are used to ameliorate refractive errors, then visual clarity is improved, but the underlying cause of excessive eye growth is not treated
Solution Approach 1:
The patent extracts the therapeutic function from the corrective lens approach by introducing a separate pharmacological intervention (muscarinic modulators) that directly addresses the underlying cause of excessive eye growth. This separates the symptomatic treatment (visual correction via lenses) from the etiological treatment (growth control via muscarinic modulation), allowing both needs to be met independently.
3Reliability
If 1% atropine drops are administered to treat myopia, then treatment efficacy is improved, but patient compliance worsens due to numerous side effects
Solution Approach 1:
The patent applies local quality by developing muscarinic modulators with selective activity for specific muscarinic receptor subtypes (M1, M3, M4, or M5) rather than non-selective antagonism. This selectivity allows the drug to act on specific receptors in the eye responsible for controlling eye growth while avoiding activation of other subtypes that cause side effects like mydriasis and cycloplegia, thereby achieving localized therapeutic effect with reduced harmful consequences.
Data Source
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AI summary
The present invention provides in one aspect azabicycio and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulae (I) & (II):