VAP-1 Inhibitor Compounds for Uveitis Treatment

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Solution Overview

Problem

Current medical treatments lack effective compounds for inhibiting vascular adhesion protein-1 (VAP-1) activity, which is involved in various diseases and disorders such as uveitis, where existing solutions are inadequate in modulating VAP-1 activity to treat or prevent these conditions.

Innovation Solution

Development of specific compounds with structural Formula (I) and its variants, including alkene isomers, tautomers, and isotopic variants, or their pharmaceutically acceptable salts, solvates, hydrates, or prodrugs, which inhibit VAP-1 activity and are used in pharmaceutical compositions for treating or preventing VAP-1-mediated diseases like uveitis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing medical treatments are used, then current standard care is provided, but effective inhibition of VAP-1 activity is not achieved

Engineering Contradiction:
Improveeffectiveness of VAP-1 inhibitionVSAvoidavailability of treatment options for VAP-1-mediated diseases
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by systematically varying molecular structures of compounds (Formula I, II, III) to optimize VAP-1 inhibition. Different substituents (R1-R12, L1, X1-X3, Y, W) represent parameter variations in chemical structure that enhance binding affinity and inhibitory potency against VAP-1 enzyme activity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention segments the VAP-1 inhibition problem into distinct compound classes (Formula I, II, III) with specific structural features. Each formula represents a segmented approach to achieving inhibition through different molecular architectures, allowing selection based on specific disease indications and patient needs

Inventive Principle:
Principle #1Segmentation

2Reliability

If no specific VAP-1 inhibitors are available, then existing treatments cannot target VAP-1, but developing new compounds requires significant research investment

Engineering Contradiction:
Improvetargeted inhibition of VAP-1VSAvoiddevelopment complexity of new compounds
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent creates universal VAP-1 inhibitor compounds that can treat multiple VAP-1-mediated diseases (uveitis, psoriasis, atherosclerosis, etc.). The core molecular structures (Formula I, II, III) serve multiple therapeutic indications, reducing development complexity by addressing various conditions with a unified compound platform rather than developing separate inhibitors for each disease

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

Data Source

PatentUS12162871B2Inhibitors of VAP-1
Publication Date: 2024.12.10 ACUCELA INC
  • US12162871B2 patent drawing
  • US12162871B2 patent drawing
  • US12162871B2 patent drawing

AI summary

Provided herein are compounds and methods of use thereof for the modulation of VAP-1 activity.