Selective OX1 Receptor Antagonists for Orexin Disorder Treatment

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Solution Overview

Problem

Current treatments for a wide range of neurological, psychiatric, and physiological disorders related to the orexin system are inadequate, particularly in addressing substance abuse, anxiety, sleep disorders, and other conditions associated with orexin receptor dysfunction.

Innovation Solution

Development of novel compounds that act as selective antagonists of the orexin receptor OX1 to modulate physiological functions and treat various disorders by inhibiting the orexinergic signaling pathway.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for orexin-related disorders are used, then existing therapeutic options are available, but treatment effectiveness is inadequate for substance abuse, anxiety, and sleep disorders

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidapplicability to multiple disorder types
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops novel compounds with modified molecular structures (formula 1 with specific substituents R1-R7) to achieve selective antagonism at the OX1 receptor. By changing the chemical parameters and structural characteristics of the compounds, the invention achieves both high treatment effectiveness and broad adaptability across multiple orexin-related disorders including substance abuse, anxiety, and sleep disorders

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If selective OX1 receptor antagonists are developed, then treatment specificity is improved, but the complexity of drug development increases

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

Solution Approach 1:

The patent introduces specific local modifications to the molecular structure at key positions (substituents R1-R7 at defined locations in formula 1) to achieve selective binding at the OX1 receptor. This local quality approach allows the compound to maintain high specificity for OX1 while managing overall structural complexity through targeted modifications rather than comprehensive redesign

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20260085056A1Ox1 receptor antagonists
Publication Date: 2026.03.26 NXERA PHARMA UK LTD
  • US20260085056A1 patent drawing
  • US20260085056A1 patent drawing
  • US20260085056A1 patent drawing

AI summary

The disclosures herein relate to novel compounds of formula (I); and salts thereof, wherein W; X; Y; Z; R1; R2; R3 and R4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.