Benzene Compounds Protecting Retinal Cells

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Solution Overview

Problem

Current treatments for ocular diseases such as age-related macular degeneration (AMD) and other ischemia-linked conditions are inadequate in addressing oxidative stress and hypoxia-induced damage to retinal pigment epithelium cells, leading to vision loss and blindness, particularly in the elderly.

Innovation Solution

Compounds with specific structures (Formulae I to X) are synthesized and used to enhance the viability of retinal pigment epithelium cells under oxidative stress and hypoxia, while minimizing impact on human umbilical vein endothelial cells, and administered to treat ocular diseases through pharmaceutical compositions with pharmaceutically acceptable carriers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for ocular diseases, then current standard therapy is maintained, but oxidative stress and hypoxia-induced damage to RPE cells is not effectively addressed

Engineering Contradiction:
Improveeffectiveness in treating oxidative stress and hypoxia-induced damageVSAvoidoxidative stress and hypoxia-induced damage to RPE cells
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of flavonoid compounds by changing parameters such as introducing specific substituents (e.g., prenyl groups at positions 5 and 8), adjusting molecular weight, and modifying functional groups to enhance the compounds' ability to scavenge reactive oxygen species and protect against hypoxia-induced damage in RPE cells

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite protective effects by combining multiple mechanisms of action within a single compound structure, including antioxidant activity, anti-apoptotic effects, and cytoprotective properties, thereby achieving comprehensive protection against oxidative stress and hypoxia

Inventive Principle:
Principle #40Composite materials

2Reliability

If treatments are developed to protect RPE cells, then cell viability is improved, but the complexity of compound structure increases

Engineering Contradiction:
ImproveRPE cell viability under oxidative stress and hypoxiaVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent designs flavonoid compounds with multi-functional properties that can simultaneously scavenge reactive oxygen species, inhibit apoptosis, protect against hypoxia-induced damage, and promote cell survival, thereby achieving multiple protective effects through a single compound class rather than requiring multiple separate agents

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

Solution Approach 2:

The invention optimizes compound parameters such as molecular weight, substituent types, and structural configurations to balance protective efficacy with pharmacological feasibility, ensuring that the enhanced RPE cell protection is achieved through manageable structural modifications

Inventive Principle:
Principle #35Parameter changes

3Reliability

If new compounds are synthesized to treat ocular diseases, then therapeutic effectiveness is improved, but manufacturing complexity increases

Engineering Contradiction:
Improvetherapeutic effectiveness in ocular disease treatmentVSAvoidcompound synthesis complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent divides the complex flavonoid molecule into modular segments with specific functional groups and substituents that can be independently optimized and synthesized, allowing for systematic development of compounds with enhanced therapeutic properties while maintaining manageable synthesis complexity through stepwise construction

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention adjusts synthesis parameters such as reaction conditions, reagent selection, and purification methods to optimize the manufacturing process of flavonoid compounds, ensuring that the enhanced therapeutic effectiveness is achieved through controlled chemical modifications rather than entirely new synthetic pathways

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3261635B1Benzene compounds for treating ocular diseases
Publication Date: 2021.03.31 NATURE WISE BIOTECH & MEDICALS CORP
  • EP3261635B1 patent drawingFigure 1(A)~1(B)
  • EP3261635B1 patent drawingFigure 2(A)~2(B)
  • EP3261635B1 patent drawingFigure 3(A)~3(B)

AI summary

The present invention provides a method for treating an ocular disease in a subject in need thereof, comprising administering an effective amount of a compound of Formula (A) to the subject. Also provided is a pharmaceutical composition for treating an ocular disease, which comprises compound of Formula (A), and a pharmaceutically acceptable carrier.