Ethylene Diamine FAAH Modulators for Anxiety and Pain

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Solution Overview

Problem

Current FAAH modulators lack potency and suitable pharmaceutical properties for effective treatment of various diseases and disorders mediated by fatty acid amide hydrolase (FAAH) activity.

Innovation Solution

Development of ethylene diamine derivatives that act as FAAH modulators, specifically compounds of Formula (I), which include various substituents and moieties that enhance their pharmacological efficacy and safety profile.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional cannabinoid treatments are used, then therapeutic effects are achieved, but side effects increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and isolates the specific ethylene diamine derivative compounds that modulate FAAH activity, separating the therapeutic mechanism from the broader cannabinoid system. This allows selective FAAH inhibition without activating CB1/CB2 receptors, thereby achieving therapeutic effects while avoiding cannabinoid-related side effects.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The ethylene diamine derivatives act as intermediary substances that specifically target and modulate FAAH enzyme activity. These compounds serve as a mediator between the therapeutic goal (FAAH inhibition) and the desired outcome (elevated endocannabinoid levels) without requiring direct cannabinoid receptor activation, thus avoiding associated side effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If FAAH modulator potency is increased, then therapeutic effectiveness improves, but pharmaceutical properties deteriorate

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidpharmaceutical properties

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent systematically varies chemical parameters of the ethylene diamine derivatives, including substituents on aromatic rings, chain lengths, and functional groups. These parameter changes optimize the balance between FAAH inhibition potency and pharmaceutical properties such as solubility, stability, and bioavailability, enabling effective therapeutic agents with suitable manufacturing characteristics.

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The ethylene diamine derivatives effectively modulate FAAH activity, providing therapeutic benefits for conditions such as anxiety, pain, multiple sclerosis, and other disorders with potentially fewer side effects compared to traditional cannabinoid treatments.

Implementation Method 1

ethylene diamine compounds... FAAH-modulating activity... modulate FAAH activity

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS8906914B2Ethylene diamine modulators of fatty acid hydrolase

Publication Date: 2014.12.09 JANSSEN PHARMA NV

AI summary

Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.