CRTH2 and DP Receptor Modulators for Asthma Treatment
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Solution Overview
Problem
Current therapies are inadequate for effectively treating or preventing inflammatory and immune-related diseases such as asthma, allergic diseases, and cancer, as they often fail to adequately address the underlying inflammatory processes mediated by prostaglandin D2 receptors like CRTH2 and DP.
Innovation Solution
Development of novel compounds that modulate CRTH2 and DP receptors, specifically targeting the inflammatory pathways to reduce inflammation and immune responses, thereby treating or preventing conditions associated with these diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used for treating inflammatory and immune-related diseases, then treatment is provided, but they fail to adequately address the underlying inflammatory processes mediated by prostaglandin D2 receptors
Solution Approach 1:
The patent segments the inflammatory pathway targeting by developing compounds that specifically modulate CRTH2 and DP receptors rather than using broad-spectrum anti-inflammatory agents. This selective receptor modulation allows the therapy to address the specific prostaglandin D2-mediated inflammatory processes while potentially reducing off-target effects.
Solution Approach 2:
The patent introduces small molecule compounds as intermediaries that bind to and modulate CRTH2 and DP receptors. These compounds act as mediators between the prostaglandin D2 signaling pathway and the therapeutic effect, enabling selective intervention in the inflammatory cascade at the receptor level.
2Reliability
If novel compounds targeting CRTH2 and DP receptors are developed, then therapeutic benefits are achieved, but the complexity of the treatment approach increases
Solution Approach 1:
The patent develops compounds that can modulate both CRTH2 and DP receptors, providing multi-functional activity against multiple targets in the prostaglandin D2 pathway. This universal approach allows a single compound to address multiple aspects of the inflammatory response mediated by these receptors.
Solution Approach 2:
The patent employs structure-activity relationship analysis to optimize compound parameters including molecular weight, logP, hydrogen bond donors and acceptors, and aromatic rings. By systematically adjusting these physicochemical parameters, the patent achieves compounds with improved potency, selectivity, and pharmacological properties while maintaining manageable complexity.
Data Source
Figure 1
AI summary
The present invention is directed to compounds, compositions and methods useful for treating inflammatory and immune-related diseases and conditions. The compounds are modulators of prostaglandin D2 (PGD2) receptors including CRTH2 and DP receptors. The subject compounds are carboxylic acid derivatives of formulae (II) and (III): Formula (II), (III), wherein, X represents a divalent linkage selected from -O-, -S(O)k-., -CRaRb-, -C(O)-, -NR8- and -C(NR9)- Y represents a divalent linkage selected from a single bond, -S(O)kNR10-, -C(O)NR10-, (C1-C4)alkylene, hetero(C2-C4)alkyIene, -N(R11)C(O)NR10- -N(R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- and -S(O)k-. Z represents -CO2R12, -C(O)NR12R13 or heteroaryl. L represents a divalent linkage selected from a single bond, (C1-C6)alkylene, (C2-C6)alkenylene, (C2-C6)alkynylene and (C2-C4)heteroalkylene.