C4-Carboxylic Acid Tryptamine Derivatives Receptor Specificity

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Solution Overview

Problem

Tryptamine-based drugs often exhibit suboptimal pharmacological effects due to poor targeting of specific receptors, leading to inadequate therapeutic outcomes and undesirable side effects, along with rapid drug clearance requiring frequent dosing, which complicates patient compliance and increases toxicity.

Innovation Solution

Development of C4-carboxylic acid-substituted tryptamine derivatives that specifically interact with target receptors, such as 5-HT receptors, to enhance pharmacological effects while minimizing off-target interactions and improving pharmacokinetic properties through specific chemical formulations and administration methods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If tryptamine-based drugs are administered to achieve therapeutic effects, then they can interact with receptors to produce pharmacological effects, but they exhibit poor targeting of specific receptors leading to suboptimal pharmacological effects and undesirable side effects

Engineering Contradiction:
Improvereceptor targeting specificityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces specific substituents at defined positions (C4-carboxylic acid, C3-alkyl/aryl groups) on the tryptamine core structure to create localized chemical modifications that enhance selective binding to 5-HT receptors while minimizing off-target interactions, thereby improving therapeutic specificity and reducing side effects

Inventive Principle:
Principle #3Local quality

2Reliability

If tryptamine-based drugs are administered to achieve therapeutic effects, then they can interact with receptors, but rapid drug clearance requires frequent dosing which complicates patient compliance

Engineering Contradiction:
Improvetherapeutic effectVSAvoiddrug action duration
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies pharmacokinetic parameters by introducing specific chemical groups (C4-carboxylic acid, C3-substituents) that alter the drug's metabolic stability, plasma half-life, and clearance rate, thereby extending the duration of action and reducing dosing frequency while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

3Reliability

If tryptamine-based drugs are administered to achieve therapeutic effects, then they can interact with receptors, but suboptimal molecular interaction results in inadequate therapeutic outcomes

Engineering Contradiction:
Improvetherapeutic outcomeVSAvoidinadequate therapeutic effect
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent optimizes local molecular interactions by introducing specific substituents (C4-carboxylic acid, C3-alkyl/aryl groups) that enhance binding affinity and selectivity for 5-HT receptors, thereby improving the intensity and specificity of the drug-receptor interaction to achieve adequate therapeutic outcomes

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS12077498B2C4-carboxylic acid-substituted tryptamine derivatives and methods of using
Publication Date: 2024.09.03 BERKSHIRE GREY OPERATING CO INC
  • US12077498B2 patent drawing
  • US12077498B2 patent drawing
  • US12077498B2 patent drawing

AI summary

Disclosed are novel C4-carboxylic acid-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders.