Sulfonamide Compounds for Glaucoma Neuroprotection
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Solution Overview
Problem
Current treatments for glaucoma, which focus on lowering intraocular pressure, often fail to prevent progressive damage to the optic nerve, highlighting a need for agents with neuroprotective effects to address microvascular factors contributing to the disease.
Innovation Solution
Development of novel sulfonamide compounds represented by a specific formula, which can be used to lower intraocular pressure and provide neuroprotection, including specific compounds like 7-[[5-Hydroxy-5-(1-propylcyclobutyl)pent-2-enyl]methanesulfonylamino]heptanoic acid ethyl ester and heptanoic acid, suitable for topical ocular use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stress or pressure
If traditional glaucoma treatments focus on lowering intraocular pressure, then intraocular pressure is reduced, but optic nerve damage continues to progress
Solution Approach 1:
The patent combines two functions into a single compound class: IOP lowering and neuroprotection. The sulfonamide compounds simultaneously reduce intraocular pressure and provide optic nerve protection, merging the previously separate functions of pressure control and nerve preservation that were achieved by different drug classes
Solution Approach 2:
The sulfonamide compounds exhibit multi-functionality by acting as both ocular hypotensives and neuroprotective agents. This universal approach allows a single compound class to address multiple aspects of glaucoma pathogenesis rather than requiring separate specialized agents
2Stress or pressure
If maximum intraocular pressure lowering is achieved, then pressure control is optimized, but optic nerve damage still progresses
Solution Approach 1:
The patent identifies microvascular factors as a harmful element in glaucoma pathogenesis and converts this understanding into a beneficial therapeutic approach. By targeting microvascular dysfunction with sulfonamide compounds, the treatment addresses the root cause of nerve damage rather than merely managing the symptom of high pressure
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
These compounds effectively lower intraocular pressure and offer neuroprotection, potentially halting or retarding optic nerve damage associated with glaucoma, as demonstrated by their selective binding to prostaglandin receptors and suitability for pharmaceutical formulations.
Implementation Method 1
as demonstrated by their selective binding to prostaglandin receptors
Data Source
AI summary
The present invention provideswherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5;R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH;R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl;R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl;m is 0 or an integer from 1 to 3 andn is an integer of from 1 to 4.These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.