OXE Receptor Antagonist Compounds for Inflammatory Treatment

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Solution Overview

Problem

Current treatments for inflammatory and allergic conditions, such as asthma and prostate cancer, are limited in effectively targeting the biological effects of 5-oxo-ETE, a potent chemoattractant that mediates eosinophil and neutrophil infiltration and proliferation, due to the lack of specific antagonists for the OXE receptor.

Innovation Solution

Development of novel heterocyclic and aromatic compounds that act as antagonists of the 5-oxo-ETE receptor, inhibiting its biological responses and blocking the action of 5-oxo-ETE, thereby providing therapeutic and prophylactic agents for inflammatory and allergic conditions, including asthma and cancer.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for inflammatory and allergic conditions are used, then existing therapeutic options are available, but they fail to effectively target the biological effects of 5-oxo-ETE due to lack of specific antagonists

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidspecificity to OXE receptor
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically modifying molecular structures (changing chemical parameters) to develop compounds with optimal binding affinity and selectivity for the OXE receptor. This involves varying substituent groups, molecular weight, and structural features to achieve the desired therapeutic effectiveness while maintaining receptor specificity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by introducing specific functional groups and substituent patterns at particular positions on the molecular scaffold. These localized structural modifications enhance the compound's ability to interact specifically with the OXE receptor binding site, thereby improving both effectiveness and receptor specificity simultaneously.

Inventive Principle:
Principle #3Local quality

2Object-affected harmful factors

If novel heterocyclic and aromatic compounds are developed as OXE receptor antagonists, then specific blocking of 5-oxo-ETE action is achieved, but the complexity of compound structure increases

Engineering Contradiction:
Improveblocking of 5-oxo-ETE actionVSAvoidcompound structure complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the molecular structure into distinct functional modules: a core heterocyclic or aromatic scaffold, substituent groups at specific positions, and side chains. This modular approach allows systematic optimization of blocking activity while managing structural complexity through organized variation of discrete components.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention applies universality by designing a core molecular scaffold that can accommodate multiple different substituent groups and side chains. This universal framework allows a single base structure to generate multiple analogs with varying degrees of blocking activity, simplifying the overall development process despite the diversity of specific compounds.

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

Data Source

PatentUS9464048B25-oxo-ETE receptor antagonist compounds
Publication Date: 2016.10.11 FLORIDA INST OF TECH
  • US9464048B2 patent drawing
  • US9464048B2 patent drawing
  • US9464048B2 patent drawing

AI summary

The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.