DP Receptor Antagonist Compounds for Sleep-Wake Disorders
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Solution Overview
Problem
Current compounds with DP receptor antagonistic activity lack sufficient central transferability, making them ineffective as therapeutic agents for sleep-wake disorders.
Innovation Solution
A compound represented by general formula (I), which includes specific structural elements such as various alkyl, halogen, and heterocyclic groups, exhibits strong DP receptor antagonistic activity and good central transferability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If compounds with DP receptor antagonistic activity are used, then DP receptor antagonism is achieved, but central transferability is insufficient
Solution Approach 1:
The patent applies parameter changes by systematically modifying molecular parameters including the aromatic ring substituents (R1-R6), linker characteristics (J, L), and heterocyclic group variations (R5, R51) to optimize the balance between DP receptor binding affinity and central nervous system penetration. Specific parameter ranges are defined: R1 as hydrogen or C1-4 alkyl, R2-R4 as halogen or C1-4 alkyl/alkoxy groups, J as bond or —O—, L as C1-6 alkylene or unsaturated variants, and R5 as C3-10 carbocycles or heterocycles, creating a structured approach to improving both antagonistic activity and central transferability simultaneously
2Reliability
If compounds are designed for strong DP receptor binding, then antagonistic activity increases, but selectivity and safety may be compromised
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns at different positions on the aromatic ring system. The R1-R6 substituents are strategically positioned with specific requirements: R1 as hydrogen or C1-4 alkyl, R2-R4 independently as halogen atoms or C1-4 alkyl/alkoxy groups (with options for multiple substitutions), and R5 as C3-10 carbocycles or heterocycles. This localized functional differentiation enhances DP receptor selectivity while maintaining antagonistic activity, thereby improving safety through selective action on the target receptor
Data Source
AI summary
An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I):(wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.