Cyclic Peptide Derivatives for Retinal Neovascularization Control

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for ophthalmic diseases such as diabetic retinopathy and age-related macular degeneration are inadequate in effectively preventing or reversing choroidal and retinal neovascularization, retinal edema, and other associated conditions.

Innovation Solution

Development of cyclic peptide derivative compositions, including specific compounds represented by Formula (1) and Formula (A2), which exhibit significant proliferation activity and are used to treat or prevent ophthalmic diseases like diabetic retinopathy and age-related macular degeneration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for ophthalmic diseases are used, then existing therapeutic approaches are maintained, but they are inadequate in effectively preventing or reversing choroidal and retinal neovascularization and retinal edema

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidchoroidal and retinal neovascularization, retinal edema
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of cyclic peptide derivatives through various substituents (R1-R14 groups including hydrocarbon groups, heterocycloalkyl groups, carboxyl groups, alkoxycarbonyl groups, hydroxy groups, alkoxy groups, and alkoxycarbonyloxy groups) to enhance their therapeutic effectiveness. These structural parameter changes enable the compounds to effectively inhibit neovascularization and reduce retinal edema, overcoming the limitations of current treatments.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If cyclic peptide derivative compositions are developed, then proliferation activity is achieved, but the complexity of the chemical structure increases

Engineering Contradiction:
Improveproliferation activityVSAvoidchemical structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the cyclic peptide derivative into distinct functional segments represented by different substituent groups (R1-R14). Each substituent can be independently selected from specific chemical groups, allowing for modular structure optimization. This segmentation enables the maintenance of proliferation activity while managing structural complexity through systematic variation of individual components.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs parameter changes by systematically varying the chemical parameters of the cyclic peptide structure, including the type of substituents (hydrocarbon, heterocycloalkyl, carboxyl, alkoxycarbonyl, hydroxy, alkoxy, alkoxycarbonyloxy groups), their positions, and their configurations. These controlled parameter changes allow optimization of proliferation activity while maintaining manageable structural complexity through defined chemical space exploration.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20260091082A1Cyclic peptide derivative composition for treating or preventing eye disease
Publication Date: 2026.04.02 DKS CO LTD
  • US20260091082A1 patent drawing
  • US20260091082A1 patent drawing
  • US20260091082A1 patent drawing

AI summary

The present disclosure provides a cyclic peptide derivative composition for treating or preventing ophthalmic diseases.The present disclosure relates to a composition comprising a compound for treating or preventing ophthalmic diseases or a pharmaceutically acceptable salt, solvate or prodrug thereof. More specifically, the composition of the present disclosure can treat or prevent diabetic retinopathy, glaucoma or age-related macular degeneration. The technology provided by the present disclosure can be used for a cyclic peptide derivative for modulating nervous system cell activity and a method for producing said cyclic peptide derivative.