6-Chloro Phenoxychroman Carboxylic Acid Derivative as DP2 Antagonist

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Solution Overview

Problem

Current treatments for allergic diseases such as asthma and atopic dermatitis are inadequate in targeting the DP2 receptor, which plays a critical role in allergic inflammation, as existing therapies do not effectively modulate this receptor to alleviate symptoms.

Innovation Solution

Development of a novel compound, 6-chloro-7-(4-(4-chloro-2-methoxyphenethylcarbamoyl)phenoxy)chroman-4-carboxylic acid, or its pharmaceutically acceptable salts, which acts as a DP2 antagonist, providing a specific mechanism to inhibit the receptor's activity and reduce allergic responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing therapies are used for allergic diseases, then general anti-inflammatory effects are achieved, but specific modulation of the DP2 receptor is insufficient

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidtargeting capability of DP2 receptor
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies molecular parameters by introducing specific substituents at defined positions on the chroman core structure. The 6-chloro substitution and 7-phenoxy group with 4-position amide linkage create a molecule with optimized binding characteristics for the DP2 receptor, transforming a general anti-inflammatory approach into a targeted therapy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by placing specific functional groups at precise locations on the molecule. The 4-position amide-linked group on the phenoxy moiety and the 6-chloro substitution on the chroman ring provide localized interactions with specific amino acid residues in the DP2 receptor binding pocket, enabling selective antagonism

Inventive Principle:
Principle #3Local quality

2Measurement precision

If DP2 receptor antagonists are developed to specifically target allergic inflammation, then treatment precision is improved, but compound complexity increases

Engineering Contradiction:
Improvereceptor targeting precisionVSAvoidmolecular structure complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The molecule is segmented into distinct functional modules: a chroman core providing structural stability, a 6-chloro substituent for specific binding interaction, a 7-phenoxy group for aromatic stacking, and a 4-position amide-linked group for hydrogen bonding. This segmentation allows each part to contribute specifically to DP2 receptor binding while maintaining overall molecular manageability

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The compound combines multiple chemical moieties (chroman ring, phenoxy group, amide linkage, aromatic substituents) into a composite molecular structure. Each component brings specific properties that collectively enable high-affinity, selective binding to the DP2 receptor while maintaining pharmacological stability

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3144303B16-substituted phenoxychroman carboxylic acid derivatives
Publication Date: 2018.09.26 ARRAY BIOPHARMA INC

AI summary

A compound which is 6-chloro-7-(4-(4-chloro-2-methoxyphenethylcarbamoyl)-phenoxy)chroman-4-carboxylic acid, or a pharmaceutically acceptable salt thereof. Said compound is either a racemic mixture or a single enantiomer, preferably Enantiomer 2 of 6-chloro-7-(4-(4-chloro-2-methoxyphenethylcarbamoyl)phenoxy)chroman-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, in particular its sodium salt. Said compound for use in treating an immunologic disorder in a mammal.