Multi-substituent Psilocybin Derivatives for Reduced Side Effects

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Solution Overview

Problem

Current psilocybin compounds are associated with adverse side effects such as panic attacks, paranoia, and psychotic states, commonly referred to as 'a bad trip', which limits their therapeutic potential.

Innovation Solution

Development of multiple-substituent psilocybin derivative compounds with specific substituents such as halogen atoms, hydroxy groups, nitro groups, and prenyl groups, which are designed to modify the pharmacological properties and reduce adverse effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If psilocybin is used for therapeutic treatment, then therapeutic efficacy is improved, but adverse side effects worsen

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

Solution Approach 1:

The patent modifies the chemical structure of psilocybin by changing substituent parameters at specific positions (R2, R4, R5, R6, R7) to alter pharmacological properties. By introducing specific substituents (halogen atoms, hydroxy groups, nitro groups, prenym groups) at defined positions, the compound's binding affinity and receptor interaction are modified to enhance therapeutic efficacy while reducing adverse effects such as panic attacks and paranoia.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local modifications at specific positions in the psilocybin molecular structure. Each position (R2, R4, R5, R6, R7) can be independently substituted with specific groups to achieve localized functional changes. This allows selective enhancement of therapeutic properties at specific binding sites while minimizing harmful effects at other locations, resolving the contradiction between efficacy and safety.

Inventive Principle:
Principle #3Local quality

2Reliability

If multiple substituents are introduced to psilocybin, then therapeutic efficacy is enhanced, but compound complexity worsens

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidcompound complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the modification process into discrete positions (R2, R4, R5, R6, R7) where specific substituents can be independently introduced. This segmentation allows systematic exploration of substituent combinations to achieve optimal therapeutic efficacy while managing synthesis complexity through modular approach. Each position can be optimized separately before final assembly.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates a universal framework where the same base psilocybin structure can accommodate multiple different substituents at defined positions to achieve various therapeutic effects. This multi-functionality allows a single compound class to address different psychiatric conditions by simply changing substituent parameters, reducing overall development complexity compared to creating entirely new compound classes.

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

Data Source

PatentUS20250025483A1Multi-substituent psilocybin derivatives and methods of using
Publication Date: 2025.01.23 ENVERIC BIOSCIENCES CANADA INC
  • US20250025483A1 patent drawing
  • US20250025483A1 patent drawing
  • US20250025483A1 patent drawing

AI summary

Disclosed are novel multi-substituent psilocybin derivative compounds and pharmaceutical and recreational drug formulations containing the same. The compounds may be produced by reacting a reactant psilocybin derivative with a substituent containing compound.