DP2 Receptor Antagonists for Asthma Treatment

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Solution Overview

Problem

Current treatments for allergic and inflammatory conditions associated with Prostaglandin D2 (PGD2) lack effective antagonists to mitigate adverse symptoms and disorders, particularly in asthma, rhinitis, and other inflammatory diseases.

Innovation Solution

Development of compounds, such as those represented by Formulas (I) to (VIII), which act as antagonists of the DP2 receptor, selectively inhibiting PGD2-mediated effects to treat PGD2-dependent conditions by modulating the activity of enzymes and proteins involved in the PGD2 pathway.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for allergic and inflammatory conditions are used, then existing therapeutic options are available, but effective antagonists to mitigate adverse symptoms are lacking

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidavailability of antagonists

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent segments the broad category of inflammatory conditions into specific subtypes mediated by PGD2 and its receptors (DP1, DP2/CRTH2), allowing for targeted antagonist development that addresses specific pathological pathways while maintaining overall therapeutic effectiveness

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies parameter changes by developing compounds with specific molecular structures (Formulas I-VIII) that exhibit selective binding affinity to PGD2 receptors, thereby changing the pharmacological parameters of available treatments to include effective antagonists with tailored specificity and potency

Inventive Principle:

Principle #35Parameter changes

2Productivity

If PGD2 binds to DP2 receptor, then chemotaxis and activation of immune cells is promoted, but adverse inflammatory responses are exacerbated

Engineering Contradiction:

Improveimmune cell activationVSAvoidinflammatory responses

Core Design Contradiction:

ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary anti-action by administering PGD2 receptor antagonists before or during the inflammatory response to block the binding of PGD2 to DP2/CRTH2 receptors, thereby preventing the downstream chemotaxis and activation of immune cells that would otherwise lead to harmful inflammatory responses

Inventive Principle:

Principle #9Preliminary anti-action

Solution Approach 2:

The patent converts the harmful inflammatory response into a benefit by selectively blocking the PGD2-DP2/CRTH2 interaction, thereby reducing pathological inflammation while preserving necessary immune functions mediated through other pathways

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentEP2257524B1N,n-disubstituted aminoalkylbiphenyl antagonists of prostaglandin d2 receptors

Publication Date: 2016.01.06 FRESH TRACKS THERAPEUTICS INC

AI summary

Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.