Kappa Opioid Receptor Compounds for Rapid Antidepressant Onset

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Solution Overview

Problem

Current treatments for depression and related mood disorders, schizophrenia, addiction, and Alzheimer's disease often require weeks to show significant clinical relief, have side effects, and do not adequately treat 30% of patients, with a need for faster and more effective mechanisms of action.

Innovation Solution

Development of compounds of formula I, which are selective kappa opioid receptor agonists or antagonists, potentially offering faster onset of action and better toleration, administered as pharmaceutical compositions to treat these conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If traditional antidepressant medications (SSRI, SNRI, TCA) are used, then depression treatment is provided, but it takes several weeks to achieve significant clinical relief

Engineering Contradiction:

Improveonset of actionVSAvoidtime to achieve clinical relief

Core Design Contradiction:

SpeedVSLoss of time

Solution Approach 1:

The patent changes the pharmacological parameter from serotonin/norepinephrine reuptake inhibition to kappa opioid receptor modulation, fundamentally altering the mechanism of action to achieve faster antidepressant effects without the delayed onset characteristic of traditional medications

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent extracts the treatment approach from the conventional serotonin system and isolates the kappa opioid receptor pathway as a separate, independent mechanism that can provide rapid antidepressant effects without relying on the slow adaptive changes of traditional antidepressants

Inventive Principle:

Principle #2Taking out (Extraction)

2Reliability

If traditional antidepressant medications are used, then depression treatment is provided, but approximately 30% of patients do not achieve adequate clinical relief

Engineering Contradiction:

Improvetreatment efficacyVSAvoidresponse rate across patient population

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The kappa opioid receptor modulator is designed to provide universal antidepressant activity that may respond to diverse pathological mechanisms underlying depression, potentially benefiting patients who do not respond to serotonin-based medications through a different neurobiological pathway

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Object-affected harmful factors

If traditional antidepressant medications are used, then depression treatment is provided, but side effects occur including gastrointestinal disturbances, sexual dysfunction, and serotonin syndrome

Engineering Contradiction:

Improveside effectsVSAvoidsafety profile

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent extracts the therapeutic effect from the serotonin system and relocates it to the kappa opioid receptor system, thereby eliminating side effects associated with serotonin manipulation such as gastrointestinal disturbances, sexual dysfunction, and serotonin syndrome while preserving antidepressant benefits

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent converts the previously harmful overactivation of the kappa opioid system (which contributes to depression and anhedonia) into a therapeutic opportunity by using selective modulators to restore normal signaling, thereby transforming a pathological mechanism into a beneficial treatment pathway

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

4Speed

If kappa opioid receptor agonists are used, then faster onset of action is achieved, but selective interaction with kappa subtype must be ensured to avoid off-target effects

Engineering Contradiction:

Improveonset of actionVSAvoidreceptor selectivity requirements

Core Design Contradiction:

SpeedVSDevice complexity

Solution Approach 1:

The patent applies local quality by designing the compound to interact specifically with the kappa opioid receptor subtype through tailored molecular features, ensuring selective binding at the target site while avoiding interactions with other receptor types, thus achieving both rapid action and specificity

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS9284291B2Kappa opioid receptor compounds

Publication Date: 2016.03.15 MEDISYNERGIES

AI summary

The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, Alzheimer's disease, anxiety and addiction, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.