Tryptamine Analogue Structures for Receptor Binding Retention

Solution Overview

Problem

Existing tryptamine-based therapeutics face challenges due to structural modifications that result in ineffective docking/binding to appropriate receptors, leading to a need for improved tryptamine-based therapeutics.

Innovation Solution

Development of tryptamine analogues with specific structural modifications, including variations in R1, R2, R3, R4, R5, R6, R7, and R8 groups, and their pharmaceutically acceptable salts, which enhance binding to target receptors.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If structural modifications are made to tryptamine, then diversity of compounds is increased, but binding activity to receptors decreases

Engineering Contradiction:

Improvediversity of compoundsVSAvoidbinding activity

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by making specific targeted modifications at certain positions (R1 at position 1, R2 at position 2, R3 at position 3) while preserving the core indole structure and key functional groups that are essential for receptor binding. This selective modification approach maintains binding activity while generating compound diversity.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying substituents at specific positions with defined constraints (R1: H or C1-6 alkyl; R2: H, NH2-cyclopropyl or CH2—CHR4—NR5R6; R3: H or L-R9). These controlled parameter variations allow generation of diverse compounds that maintain optimal binding characteristics.

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If structural modifications are made to tryptamine, then new compounds are generated, but docking effectiveness to receptors deteriorates

Engineering Contradiction:

Improvenew compounds generationVSAvoiddocking effectiveness

Core Design Contradiction:

Adaptability or versatilityVSManufacturing precision

Solution Approach 1:

The patent applies local quality by making specific targeted modifications at certain positions (R1 at position 1, R2 at position 2, R3 at position 3) while preserving the core indole structure and key functional groups that are essential for receptor binding. This selective modification approach maintains binding activity while generating compound diversity.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying substituents at specific positions with defined constraints (R1: H or C1-6 alkyl; R2: H, NH2-cyclopropyl or CH2—CHR4—NR5R6; R3: H or L-R9). These controlled parameter variations allow generation of diverse compounds that maintain optimal binding characteristics.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12534441B2Tryptamine analogues

Publication Date: 2026.01.27 BECKLEY PSYTECH LIMITED

AI summary

This invention relates to pharmaceutically acceptable tryptamine analogues and salts thereof. In particular, though not exclusively, the invention relates to formulations and uses of the same as a medicament.