Hydroxy Orexin Antagonists for Sleep Disorder Treatment

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Solution Overview

Problem

Current treatments for neurological and psychiatric disorders associated with orexin receptors lack effective antagonists, which are essential for managing sleep disorders, insomnia, and other related conditions.

Innovation Solution

Development of hydroxy compounds that act as antagonists to orexin receptors, specifically targeting the OX1R and OX2R receptors, which are designed to inhibit orexin receptor activity and treat various neurological and psychiatric disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for neurological and psychiatric disorders are used, then existing therapeutic options are available, but effective orexin receptor antagonists are lacking

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidavailability of antagonist compounds
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically varying chemical substituents (R1, R2, R3, R4, R5, R6, R7) on the core molecular structure to optimize orexin receptor antagonist activity. Different combinations of hydroxyl groups, alkyl chains, and aromatic rings are explored to achieve desired pharmacological properties while maintaining structural diversity for treating various neurological and psychiatric disorders

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If orexin receptor antagonists are developed, then sleep disorders and insomnia can be treated, but the complexity of targeting specific receptors (OX1R and OX2R) increases

Engineering Contradiction:
Improvetreatment of sleep disordersVSAvoidreceptor targeting specificity
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The patent applies local quality by designing molecules with specific functional groups positioned at particular locations on the core structure to target specific orexin receptors. The strategic placement of hydroxyl groups, alkyl chains, and aromatic substituents creates localized interactions that differentiate OX1R from OX2R binding, enabling selective antagonism while simplifying the overall treatment approach for sleep disorders

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS9725434B2Hydroxy-substituted orexin receptor antagonists
Publication Date: 2017.08.08 MERCK SHARP & DOHME LLC
  • US9725434B2 patent drawing
  • US9725434B2 patent drawing
  • US9725434B2 patent drawing

AI summary

The present invention is directed to hydroxy compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.