Therapeutic Cyclopentanes for Glaucoma

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Solution Overview

Problem

Current treatments for glaucoma and ocular hypertension lack effective solutions, and prostaglandin EP2 selective agonists have various medical uses but require more targeted and efficient compounds for these conditions.

Innovation Solution

Development of specific compounds, including their pharmaceutically acceptable salts and prodrugs, which act as selective EP2 agonists to treat glaucoma and ocular hypertension, with structures that can be administered topically or systemically, potentially combined with other drugs for enhanced efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If prostaglandin EP2 selective agonists are used to treat glaucoma and ocular hypertension, then therapeutic effectiveness is improved, but current treatments lack targeted efficiency

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtargeted efficiency
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies local quality by designing compounds with specific structural modifications at particular positions of the prostaglandin molecule. The cyclopentane ring with specific substituents at defined positions creates localized structural features that enhance EP2 receptor selectivity, thereby improving targeted efficiency while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying chemical parameters such as substituent types, positions, and stereochemistry of the cyclopentane ring structure. These parameter modifications optimize the compound's affinity and selectivity for the EP2 receptor, resolving the contradiction between general effectiveness and targeted efficiency.

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If selective EP2 agonist compounds are developed with specific structures, then targeted treatment capability is improved, but compound complexity increases

Engineering Contradiction:
Improvetargeted treatment capabilityVSAvoidcompound complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the prostaglandin molecule into distinct functional segments: the cyclopentane ring core, specific substituents at defined positions, and stereochemical configurations. This segmented approach allows each component to contribute specifically to EP2 selectivity, improving targeted treatment capability while managing overall molecular complexity through modular design.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent utilizes universality by designing a core cyclopentane structure that serves multiple functions: providing structural stability, enabling specific receptor binding, and allowing for various substituent variations. This multi-functional core structure achieves high targeted treatment capability without proportionally increasing complexity, as the same basic framework supports multiple therapeutic optimizations.

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

Data Source

PatentUS7585895B2Therapeutic substituted cyclopentanes
Publication Date: 2009.09.08 ALLERGAN INC
  • US7585895B2 patent drawing
  • US7585895B2 patent drawing
  • US7585895B2 patent drawing

AI summary

Therapeutic prostaglandin compounds are disclosed herein.