6-Alkyl Naphthamide Compounds for Ocular Hypertension

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Solution Overview

Problem

Current treatments for glaucoma, particularly primary and secondary forms, face challenges in effectively reducing intraocular pressure due to obstruction of aqueous humor outflow, with existing ocular hypotensive agents having limitations in efficacy and comfort for patients.

Innovation Solution

Development of well-defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds, which can be administered topically as ophthalmically acceptable pharmaceutical compositions to treat glaucoma and ocular hypertension, facilitating the reduction of intraocular pressure.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional ocular hypotensive agents are used to treat glaucoma, then intraocular pressure reduction is achieved, but patient comfort and efficacy are limited

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidpatient comfort
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the chemical structure of naphthamide and quinoline compounds by changing parameters such as adding alkyl groups at specific positions (6-alkyl or hydroxyalkyl), adjusting molecular weight, and modifying functional groups. These parameter changes optimize the compounds for both efficacy in reducing intraocular pressure and improved patient comfort, resolving the contradiction between therapeutic reliability and ease of operation.

Inventive Principle:
Principle #35Parameter changes

2Stress or pressure

If aqueous humor outflow is obstructed, then glaucoma condition develops, but current drugs fail to effectively reduce pressure

Engineering Contradiction:
Improveintraocular pressureVSAvoidpressure reduction efficacy
Core Design Contradiction:
Stress or pressureVSReliability

Solution Approach 1:

The patent extracts and targets specific molecular interactions responsible for aqueous humor outflow obstruction. By designing compounds that specifically interfere with the obstruction mechanism at the cellular or molecular level (rather than using general pressure-reducing agents), the invention achieves more reliable and effective intraocular pressure reduction, directly addressing the root cause of the glaucoma condition.

Inventive Principle:
Principle #2Taking out (Extraction)

Data Source

PatentUS8633220B2Therapeutic agents for ocular hypertension
Publication Date: 2014.01.21 ALLERGAN INC
  • US8633220B2 patent drawing
  • US8633220B2 patent drawing
  • US8633220B2 patent drawing

AI summary

This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.