Therapeutic Compounds for Glaucoma via Aqueous Humor Outflow

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Solution Overview

Problem

Current treatments for glaucoma, particularly those involving ocular hypertensive conditions, often rely on topical β-adrenoreceptor antagonists and eicosanoids, which may not effectively manage intraocular pressure or have limitations in addressing the underlying causes of glaucoma, such as obstruction of aqueous humor outflow.

Innovation Solution

Development of compounds with specific structural features, including organic acid functional groups, amides, esters, and tetrazolyl functional groups, which can reduce intraocular pressure, treat glaucoma, and promote hair growth or improve hair appearance by targeting intraocular pressure, drainage issues, and ocular health.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stress or pressure

If topical β-adrenoreceptor antagonists are used to treat glaucoma, then intraocular pressure can be reduced, but the underlying causes of glaucoma such as obstruction of aqueous humor outflow are not effectively addressed

Engineering Contradiction:
Improveintraocular pressureVSAvoideffectiveness in addressing underlying causes
Core Design Contradiction:
Stress or pressureVSReliability

Solution Approach 1:

The patent extracts and addresses the root cause of glaucoma by designing compounds that specifically target and improve aqueous humor outflow through the trabecular meshwork and canal of Schlemm, rather than merely suppressing symptoms. The compounds are structurally designed to interact with pathways involved in aqueous drainage, thereby extracting the underlying pathological mechanism from the symptom management approach.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

Instead of continuing with the conventional approach of reducing intraocular pressure through β-adrenoreceptor antagonism, the patent inverts the therapeutic strategy by focusing on improving aqueous humor outflow through novel chemical structures that target drainage pathways directly, thereby addressing the problem from the opposite direction.

Inventive Principle:
Principle #13The other way round (Inversion)

2Stress or pressure

If eicosanoids are used for glaucoma management, then intraocular pressure can be reduced, but limitations remain in effectively managing ocular hypertensive conditions

Engineering Contradiction:
Improveintraocular pressureVSAvoideffectiveness across various ocular hypertensive conditions
Core Design Contradiction:
Stress or pressureVSAdaptability or versatility

Solution Approach 1:

The patent creates compounds with universal applicability across different types of ocular hypertensive conditions including open-angle glaucoma, angle-closure glaucoma, and post-surgical hypertensive episodes. The chemical structures are designed to act through multiple mechanisms that can address various underlying causes, making the treatment versatile and adaptable to different clinical scenarios.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent employs parameter changes by modifying chemical structures with specific functional groups (carboxylic acids, amides, esters, tetrazolyl groups) and varying chain lengths and substitutions to optimize activity across different ocular conditions. This systematic variation of molecular parameters enables broad-spectrum effectiveness.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If traditional glaucoma treatments are used, then ocular health can be maintained, but additional benefits such as hair growth promotion are not achieved

Engineering Contradiction:
Improveocular health maintenanceVSAvoidtherapeutic benefits range
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent achieves multi-functionality by designing compounds that simultaneously provide ocular therapeutic effects (intraocular pressure reduction, glaucoma treatment) and extracocular benefits (hair growth promotion, hair appearance improvement). This single agent addresses multiple health concerns, expanding the therapeutic benefits beyond traditional glaucoma treatment.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent merges multiple therapeutic functions into a single compound class, combining glaucoma treatment capabilities with hair growth promotion effects. This consolidation allows one medication to address both ocular and dermatological conditions, reducing the need for multiple separate treatments.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS8278347B2Therapeutic compounds
Publication Date: 2012.10.02 ALLERGAN INC
  • US8278347B2 patent drawing
  • US8278347B2 patent drawing
  • US8278347B2 patent drawing

AI summary

A compound having a structureis disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.