GAG Derivative Composition for Chemokine Receptor Regulation

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Solution Overview

Problem

Current treatments for age-related macular degeneration (AMD) using CCR3 inhibitors can cause rapid tissue degeneration due to the use of solubilizing agents like DMSO, and existing compositions do not effectively regulate chemokine receptors, leading to inadequate medicinal effects.

Innovation Solution

A composition comprising a glycosaminoglycan (GAG) derivative, such as a hydrophobic group-introduced or crosslinked GAG, combined with a chemokine receptor activity regulator, which forms a covalent complex to inhibit chemokine receptors without using excessive solubilizing agents, thereby reducing tissue degeneration and enhancing medicinal effects for posterior eye diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a CCR3 inhibitor is prepared with a solubilizing agent (such as DMSO) to achieve a concentration sufficient for exhibiting a pharmaceutical effect, then the medicinal effect on AMD is improved, but rapid degeneration of tissues (such as lens) in the vicinity of the vitreous body occurs

Engineering Contradiction:

Improvemedicinal effectVSAvoidtissue degeneration

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses GAG derivatives as intermediary carriers to deliver chemokine receptor activity regulators to the target site. The GAG derivative forms a complex with the regulator, enabling delivery at lower concentrations that avoid tissue toxicity while maintaining therapeutic efficacy through targeted action on chemokine receptors involved in CNV

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the concentration parameter of the chemokine receptor activity regulator from high concentration (requiring solubilizing agents like DMSO) to low concentration when complexed with GAG derivatives. This parameter change eliminates the need for harmful solubilizing agents while maintaining pharmaceutical effect through enhanced target specificity and prolonged action

Inventive Principle:

Principle #35Parameter changes

2Reliability

If heparan sulfate or heparin is administered to suppress CNV in a laser-induced CNV model, then the medicinal effect is improved, but the composition lacks chemokine receptor activity regulation capability

Engineering Contradiction:

Improvemedicinal effectVSAvoidchemokine receptor activity regulation

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent merges the CNV suppression capability of GAG derivatives with the chemokine receptor regulation capability of specific chemokine receptor activity regulators. This combination creates a composition that simultaneously achieves vascular inhibition through multiple mechanisms: GAG-mediated angiogenesis suppression and chemokine receptor-mediated leukocyte recruitment inhibition

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The patent creates a multi-functional composition where the GAG derivative-chemokine receptor activity regulator complex performs multiple functions: (1) suppresses angiogenesis through GAG activity, (2) regulates chemokine receptors to inhibit inflammatory cell recruitment, and (3) provides sustained release and targeted delivery to the vitreous body and choroid

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20240390411A1Composition comprising glycosaminoglycan derivative and chemokine receptor activity regulator

Publication Date: 2024.11.28 SEIKAGAKU KOGYO CO LTD

AI summary

Provided are a composition comprising a GAG derivative and a chemokine receptor activity regulator, and a pharmaceutical composition comprising said composition.