Substituted Phenylalkylamines for Controlled Psychedelic Duration

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Solution Overview

Problem

Current psychedelic compounds for treating mental health disorders have variable duration of action and numerous side effects, limiting their clinical use and accessibility.

Innovation Solution

Development of substituted phenylalkylamine compounds that modulate monoamine neurotransmitter receptors and transporters, such as serotonin receptors, with optimized time course and reduced side effects, including formulations for various administration routes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If known psychedelic compounds are used to treat mental health disorders, then therapeutic efficacy is achieved, but variable duration of action and numerous side effects occur

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidduration of action
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies molecular parameters of psychedelic compounds by introducing deuterium atoms at specific positions (R1 or R2) in the phenylalkylamine structure. This isotopic substitution changes the physical and chemical properties of the compound, resulting in improved duration of action and reduced side effects while maintaining therapeutic efficacy for mental health disorders

Inventive Principle:
Principle #35Parameter changes

2Reliability

If known psychedelic compounds are used to treat mental health disorders, then therapeutic efficacy is achieved, but numerous side effects occur

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

Solution Approach 1:

The patent applies isotopic substitution by replacing hydrogen atoms with deuterium at specific positions in the molecular structure. This parameter change alters the compound's interaction with biological targets, reducing harmful side effects while preserving the therapeutic benefits for treating mental health disorders

Inventive Principle:
Principle #35Parameter changes

3Reliability

If known psychedelic compounds are used to treat mental health disorders, then therapeutic benefits are provided, but treatment accessibility is limited

Engineering Contradiction:
Improvetherapeutic benefitsVSAvoidtreatment accessibility
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the pharmacokinetic parameters of psychedelic compounds through deuterium substitution, which improves duration of action and reduces side effects. These parameter changes make the compounds more suitable for clinical application, thereby increasing treatment accessibility and feasibility

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12465578B2Substituted alpha-ethyl phenylalkylamines
Publication Date: 2025.11.11 ALEXANDER SHULGIN RES INST INC
  • US12465578B2 patent drawing
  • US12465578B2 patent drawing
  • US12465578B2 patent drawing

AI summary

Provided are phenylalkylamines, such as 2,5-disubstituted and 2,4,5-trisubstituted phenylalkylamines. In some embodiments, the phenylalkylamines are asymmetrically substituted. In some embodiments, such compounds modulate the activity of monoamine receptors and/or monoamine transporters. Also provided are methods for the preparation of phenylalkylamines and pharmaceutical compositions thereof. Methods of using the phenylalkylamines, alone or in combination with other therapeutic agents, are provided. In some embodiments, phenylalkylamines are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders, or are used for the improvement of mental health or functioning.