Thioether-Piperidinyl Orexin Antagonists for Sleep Disorders

The patent applies parameter changes by modifying the chemical structure of piperidine compounds to include thioether groups and specific substituents (R1a, R1b, R1c, R3, R5, R6, R7) to optimize binding affinity and selectivity for orexin receptors. This structural parameter optimization enables the compounds to effectively antagonize orexin receptor activity, thereby resolving the lack of effective antagonist treatments for neurological and psychiatric disorders

The patent applies segmentation by dividing the complex thioether-piperidinyl compound structure into distinct modular components: the core piperidine ring, thioether linkages, and variable substituent groups (R1a, R1b, R1c, R3, R5, R6, R7). This modular segmentation allows for systematic synthesis and optimization of individual components while maintaining overall therapeutic efficacy, thereby managing the complexity of compound development