Substituted 2-Azabicyclic Compounds as Orexin Receptor Modulators

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Solution Overview

Problem

Current therapies lack effective modulators for the orexin receptor, which are crucial for treating various disorders related to sleep-wake cycles, emotional behavior, and metabolic regulation, as existing treatments often have limited efficacy or significant side effects.

Innovation Solution

Development of substituted 2-azabicyclic compounds that act as orexin receptor modulators, specifically designed to target orexin-1 and orexin-2 receptors, allowing for therapeutic intervention in disorders mediated by orexin receptor activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for orexin receptor-related disorders, then treatment can be provided, but efficacy is limited and significant side effects occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing compounds with specific molecular structures (substituted 2-azabicyclic compounds with formulas I and II) that modify the pharmacological parameters of orexin receptor interaction. By changing the chemical structure parameters including specific substituents at defined positions, the invention achieves improved efficacy and reduced side effects compared to existing treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent segments the treatment approach by developing selective modulators for different orexin receptor subtypes (orexin-1 and orexin-2 receptors). The compounds are designed to selectively target specific receptors, allowing differentiated treatment strategies for different disorders based on which receptor subtype is primarily involved

Inventive Principle:
Principle #1Segmentation

2Reliability

If current therapies are used for sleep-wake cycle disorders, then treatment is available, but the treatments have limited efficacy

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtherapeutic option availability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies universality by developing compounds that can treat multiple different disorders through orexin receptor modulation. The same class of compounds (substituted 2-azabicyclic compounds) is applicable to sleep-wake cycle disorders, emotional behavior disorders, and metabolic disorders, providing a universal therapeutic platform with broad adaptability

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP3191468B1Substituted 2-azabicycles and their use as orexin receptor modulators
Publication Date: 2018.12.12 JANSSEN PHARMA NV
  • EP3191468B1 patent drawing
  • EP3191468B1 patent drawing
  • EP3191468B1 patent drawing

AI summary

The present invention is directed to compounds of Formula (I): Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of using the compounds of the invention are also within the scope of the invention.