Compound A Suppressing Retinal Vascular Permeability

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Solution Overview

Problem

Existing treatments for eye diseases such as age-related macular degeneration, diabetic retinopathy, and retinal vein occlusion do not effectively inhibit the functions of vascular endothelial growth factor (VEGF), which contributes to increased retinal vascular permeability and neovascularization.

Innovation Solution

The use of Compound A, a specific chemical compound, or its pharmaceutically acceptable salt, which suppresses the increase of retinal vascular permeability induced by VEGF, thereby providing therapeutic or preventive benefits for various eye diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for eye diseases, then treatment is provided, but VEGF functions are not effectively inhibited, resulting in increased retinal vascular permeability and neovascularization

Engineering Contradiction:
Improveeffectiveness of VEGF inhibitionVSAvoidretinal vascular permeability control
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces a novel compound A with a specific chemical structure that represents a parameter change in the therapeutic agent class. This compound achieves effective VEGF inhibition through its unique molecular configuration, resolving the contradiction by providing a new chemical parameter (compound structure) that delivers reliable VEGF inhibition while controlling retinal vascular permeability.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If VEGF functions are inhibited to suppress retinal vascular permeability and neovascularization, then treatment effectiveness improves, but new therapeutic agents are required

Engineering Contradiction:
ImproveVEGF inhibition effectivenessVSAvoidavailability of therapeutic agents
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent segments the therapeutic approach by introducing compound A as a distinct chemical entity with specific structural features (3-[(3S,4R)-3-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile). This segmentation creates a new, manufacturable therapeutic agent that achieves VEGF inhibition, resolving the contradiction between treatment effectiveness and agent availability.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS20250152589A1Therapeutic or preventive agent for eye diseases
Publication Date: 2025.05.15 SHIONOGI & CO LTD
  • US20250152589A1 patent drawing
  • US20250152589A1 patent drawing
  • US20250152589A1 patent drawing

AI summary

3-[(3S,4R)-3-Methyl-6-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile suppresses an increase of the retinal vascular permeability induced by VEGF, it can be used as an active ingredient of a therapeutic or preventive agent for various eye diseases involving VEGF, such as age-related macular degeneration, diabetic retinopathy, macular edema, neovascular maculopathy, retinal vein occlusion and neovascular glaucoma.