Naphthylurea Eye Drops for Corneal Neovascularization Inhibition

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Solution Overview

Problem

Existing medicaments for treating ophthalmic diseases related to corneal neovascularization have gaps in efficacy due to varying administration methods, absorption, metabolism, and environmental factors, necessitating a targeted approach.

Innovation Solution

The use of a naphthylurea compound in the form of eye drops, which can include pharmaceutically acceptable salts, solvates, or crystal forms, to treat corneal neovascular diseases, administered at a concentration of 10-30 mg/mL, providing a direct application method.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing medicaments are used to treat corneal neovascularization, then some therapeutic effect is achieved, but efficacy is insufficient due to varying administration methods and absorption issues

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidadministration method complexity
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the physical-chemical parameters of the medicament by providing multiple crystal forms (polymorphs) of the naphthylurea compound. Different crystal forms have different solubility, stability, and dissolution rates, which directly affect absorption and therapeutic efficacy. This allows optimization of the medicament's performance parameters to overcome insufficient efficacy while maintaining simple eye drop administration.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If different administration methods are used, then various therapeutic effects are achieved, but consistency and reliability of treatment are reduced

Engineering Contradiction:
Improveadministration flexibilityVSAvoidtreatment consistency
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent makes the naphthylurea compound applicable to multiple crystal forms and pharmaceutically acceptable salts, creating a universal medicament platform. This universal approach ensures that regardless of which specific crystal form or salt is used, the core therapeutic effect remains consistent, thereby improving treatment reliability while maintaining flexibility in formulation and administration methods.

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

3Adaptability or versatility

If the same medicament is used for different ocular diseases, then broad applicability is achieved, but disease-specific efficacy may be compromised

Engineering Contradiction:
Improvedisease coverageVSAvoiddisease-specific optimization
Core Design Contradiction:
Adaptability or versatilityVSManufacturing precision

Solution Approach 1:

The patent applies local quality by providing specific crystal forms and formulations optimized for corneal neovascularization treatment. While the naphthylurea compound can treat various ocular diseases, the patent specifically optimizes certain crystal forms (e.g., Form I, Form II) and formulations for corneal applications, where local ocular conditions require specific solubility, stability, and penetration characteristics to achieve maximum efficacy.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP4079303B1Naphthylurea compound for treating corneal neovascular disease
Publication Date: 2026.02.04 SUZHOU RAYMON PHARMA CO LTD
  • EP4079303B1 patent drawing
  • EP4079303B1 patent drawing
  • EP4079303B1 patent drawing

AI summary

The present invention provides use of substance A in the preparation of a medicament. The substance A is a naphthylurea compound as shown in formula I, a pharmaceutically acceptable salt thereof, a solvate thereof, a solvate of the pharmaceutically acceptable salt thereof, a crystal form thereof or a tautomer thereof, and the medicament is a medicament for treating a corneal neovascular disease. The naphthylurea compound of the present invention can treat the corneal neovascular disease by means of eye dropping administration.