A3 Adenosine Receptor Antagonists for Glaucoma Neuroprotection
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Solution Overview
Problem
Current medical and surgical therapies for glaucoma are limited in efficacy and associated with significant side effects, and they fail to protect the retina from degeneration, with elevated adenosine levels and upregulated A3 adenosine receptors contributing to elevated intraocular pressure.
Innovation Solution
Development of novel heteroaryl-tetrahydrothiophene-3,4-diol, tetrahydrofuran-3,4-diol, or cyclopentane-1,2-diol compounds as A3 adenosine receptor antagonists to reduce intraocular pressure and provide neuroprotection for retinal ganglion cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stress or pressure
If current medical and surgical therapies are used to lower intraocular pressure, then intraocular pressure is reduced, but significant side effects occur and retinal protection is not achieved
Solution Approach 1:
The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (formula I) that selectively target A3 adenosine receptors. By modifying the chemical parameters of the therapeutic agent, the patent achieves selective receptor binding that lowers intraocular pressure while minimizing systemic side effects through selective action on ocular A3 receptors
Solution Approach 2:
The patent uses A3 adenosine receptor antagonists as intermediary substances that mediate between the therapeutic goal (lowering intraocular pressure) and the desired outcome (retinal protection). These compounds act as intermediaries by blocking A3 receptor-mediated pathways that contribute to elevated intraocular pressure while preventing retinal ganglion cell degeneration
2Stress or pressure
If current therapies are used to treat glaucoma, then intraocular pressure is lowered, but retinal ganglion cells are not protected from degeneration
Solution Approach 1:
The patent employs A3 adenosine receptor antagonists as intermediary substances that mediate between the therapeutic goal (lowering intraocular pressure) and the desired outcome (retinal protection). These compounds act as intermediaries by blocking A3 receptor-mediated pathways that contribute to elevated intraocular pressure while preventing retinal ganglion cell degeneration
Solution Approach 2:
The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (formula I) that selectively target A3 adenosine receptors. By modifying the chemical parameters of the therapeutic agent, the patent achieves selective receptor binding that provides dual benefits of pressure reduction and neuroprotection
Data Source
AI summary
The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.