Nitric Oxide Donating Carnosine Analogues for Glaucoma
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Solution Overview
Problem
Current treatments for glaucoma and ocular hypertension, such as beta-blockers, alpha-agonists, and prostaglandin analogs, exhibit undesirable side effects and lack potency and duration of action, with no nitric oxide donor drugs approved for these conditions.
Innovation Solution
Development of nitric oxide donating carnosine analogues, specifically compounds of formula (I), which reduce intraocular pressure through topical, periocular, or intraocular administration, potentially combined with other active ingredients like alpha adrenergic agonists or carbonic anhydrase inhibitors.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for glaucoma and ocular hypertension (beta-blockers, alpha-agonists, prostaglandin analogs) are used, then intraocular pressure is reduced, but undesirable side effects occur
Solution Approach 1:
The patent introduces a novel chemical compound class (carnosine analogues with nitric oxide donating groups) that changes the pharmacological parameters of treatment. These compounds provide a different mechanism of action through nitric oxide donation, achieving intraocular pressure reduction without the side effects associated with conventional drug classes.
Solution Approach 2:
The invention combines carnosine structure with nitric oxide donating groups to create a composite molecular structure. This composite approach integrates the beneficial properties of carnosine (antioxidant, protective effects on ocular tissues) with the vasodilatory and pressure-reducing properties of nitric oxide donors, achieving both efficacy and safety.
2Reliability
If current treatments for glaucoma and ocular hypertension are used, then intraocular pressure is reduced, but potency and duration of action are insufficient
Solution Approach 1:
The patent modifies the pharmacokinetic and pharmacodynamic parameters by introducing carnosine analogues with extended duration of action. The compounds demonstrate prolonged intraocular pressure reduction effects, addressing the insufficient duration of action of current treatments through optimized molecular structure and sustained nitric oxide release.
3Adaptability or versatility
If no nitric oxide donor drugs are approved for glaucoma and ocular hypertension, then existing treatments are limited, but new therapeutic options are needed
Solution Approach 1:
The patent segments the therapeutic approach by introducing a completely new drug class (nitric oxide donating carnosine analogues) distinct from existing glaucoma medications. This segmentation provides diversified treatment options while maintaining proven effectiveness through the novel mechanism of nitric oxide donation and carnosine-based protective actions.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The nitric oxide donating carnosine analogues demonstrate a potent and prolonged ocular hypotensive effect, offering a more effective treatment for glaucoma and ocular hypertension with improved pharmacological properties compared to existing therapies.
Implementation Method 1
nitric oxide donating carnosine analogues of formula (I) for the use in the treatment and/or prophylaxis of glaucoma and ocular hypertension
Data Source
AI summary
The present invention relates to nitric oxide donor carnosine derivatives having a great efficacy in reducing elevated intraocular pressure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.