Orexin Receptor Agonist Scaffolds for Non-Invasive CNS Delivery
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Solution Overview
Problem
Current treatments for neurological and psychiatric disorders related to orexin receptors are inadequate, and there is a need for more effective orexin receptor agonists to address a wide range of associated conditions.
Innovation Solution
Development of cyclopentapyrrole, furopyrrole, and azabicycloheptane compounds that act as agonists for orexin receptors, potentially treating or preventing neurological and psychiatric disorders by modulating orexin receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional methods (microinjection, electroporation, viral vectors) are used to deliver orexin receptor agonists into the CNS, then the agonists can reach the target, but the procedures are invasive, complex, and carry risks of infection and immune response
Solution Approach 1:
The patent extracts the agonist delivery from invasive procedures by using intranasal administration, which delivers the agonist through the nasal cavity to reach the CNS via the olfactory nerve pathway, eliminating the need for surgical intervention
Solution Approach 2:
The patent uses intranasal administration as an intermediary pathway, allowing the agonist to travel from the nasal cavity through the olfactory nerve to reach the CNS, serving as a non-invasive mediator between external administration and central target delivery
2Reliability
If conventional delivery methods are used, then agonists can reach the CNS, but the procedures are painful and require specialized facilities and trained personnel
Solution Approach 1:
The patent removes the painful invasive elements from the delivery process by extracting the agonist administration from surgical procedures and delivering it through the non-invasive intranasal route
Solution Approach 2:
The intranasal administration method enables self-service delivery, where patients can administer the agonist themselves without requiring specialized facilities or trained personnel, making the treatment accessible and convenient
3Ease of operation
If peripherally acting drugs are used, then administration is simple, but the drugs cannot effectively cross the blood-brain barrier to reach central targets
Solution Approach 1:
The patent uses the olfactory nerve pathway as an intermediary route that bypasses the blood-brain barrier, allowing peripherally acting drugs to reach central targets through direct neural transport from the nasal cavity
Solution Approach 2:
The patent segments the delivery pathway into two distinct routes: the systemic circulation route (blocked by BBB) and the olfactory nerve route (direct CNS access), utilizing the latter to overcome the barrier limitation
4Reliability
If invasive procedures are used to deliver agonists, then CNS delivery is achieved, but patient compliance and quality of life are reduced
Solution Approach 1:
The patent extracts the agonist delivery from invasive surgical procedures and implements it through simple intranasal administration, dramatically improving patient compliance and quality of life
Solution Approach 2:
The intranasal administration enables patients to self-administer the treatment at home without requiring hospital visits or surgical intervention, significantly enhancing patient compliance and overall quality of life
Data Source
AI summary
The present invention is directed to cyclopentapyrrole, furopyrrole and azabicycloheptane compounds which are agonists 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 compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.