Halogenated Anxiolytic Compound for Comorbid Anxiety and Depression

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Solution Overview

Problem

Current treatments for comorbid anxiety and depression disorders are often ineffective, with conventional antidepressants showing lower response rates and higher withdrawal syndrome risks, particularly in patients with comorbid conditions, and existing medications like benzodiazepines and SSRIs/SNRIs associated with physical dependence and sexual dysfunction.

Innovation Solution

A compound with the general formula (I), where R1 is -OCH3 or -CN, or its pharmaceutical salts, hydrates, or anhydrates, is used to treat comorbid anxiety and depression disorders, offering anxiolytic effects without triggering withdrawal syndrome, and is administered in a pharmaceutical composition with suitable excipients for various routes of administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antidepressants are used to treat comorbid anxiety and depression disorders, then depression symptoms may be addressed, but the treatment effectiveness is reduced and withdrawal syndrome risk increases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidwithdrawal syndrome risk
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of known antidepressant compounds by changing specific parameters (substituting hydrogen atoms with fluorine or chlorine atoms at specific positions on the aromatic ring), which alters the pharmacological properties to reduce withdrawal syndrome while maintaining therapeutic effectiveness

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite chemical structures by combining the core antidepressant scaffold with specific halogen substituents, resulting in a new compound class that integrates the benefits of antidepressant activity with reduced adverse effects

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If benzodiazepines are used to treat anxiety symptoms, then anxiolytic effects are achieved, but physical dependence and withdrawal syndrome occur

Engineering Contradiction:
Improveanxiety symptom reliefVSAvoidphysical dependence risk
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent changes the chemical parameters of benzodiazepine-related compounds by introducing specific halogen substituents and modifying the molecular structure, which maintains anxiolytic activity through GABAergic mechanisms while reducing the binding affinity that leads to physical dependence

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If SSRIs/SNRIs are used for long-term treatment, then depression and anxiety symptoms are managed, but sexual dysfunction occurs

Engineering Contradiction:
Improvelong-term treatment capabilityVSAvoidsexual dysfunction
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical parameters of SSRI/SNRI compounds by adding halogen substituents, which alters the receptor binding profile to reduce serotonin-mediated sexual side effects while preserving the antidepressant and anxiolytic therapeutic effects for long-term use

Inventive Principle:
Principle #35Parameter changes

4Adaptability or versatility

If existing medications are used to treat comorbid conditions, then both anxiety and depression are targeted, but the response rate is lower compared to pure disorders

Engineering Contradiction:
Improvecomorbid condition coverageVSAvoidresponse rate
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent designs compounds with multi-functional pharmacological activity that can simultaneously address both anxiety and depression pathways, making the medication universally effective for comorbid conditions rather than requiring separate treatments for each disorder

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

Solution Approach 2:

The invention optimizes chemical parameters to enhance the compound's ability to interact with multiple neurotransmitter systems (serotonin, norepinephrine, GABA), improving the response rate in comorbid patients by addressing both conditions through a single mechanism of action

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3130339B1A compound for use in the treatment of comorbid anxiety disorder and depression disorder
Publication Date: 2020.05.06 ACHE LAB FARM
  • EP3130339B1 patent drawingFigure 1
  • EP3130339B1 patent drawingFigure 2
  • EP3130339B1 patent drawingFigure 3

AI summary

The present invention relates to a compound for use in the treatment of comorbid anxiety disorder and depression disorder, as well as for preventing depression disorders in individuals affected by anxiety disorders, wherein the compound is selected from the group presenting the general formula (I): wherein R1 is -OCH3 or -CN or suitable pharmaceutical salts, hydrates or anhydrates thereof.