Quinazoline-2,4-dione Derivative for Neuroprotection

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Solution Overview

Problem

Current treatments for neurological brain diseases, such as stroke and neurodegenerative disorders, face challenges in efficacy and toxicity, and there is a need for effective compounds that can protect nerve cells and improve brain function.

Innovation Solution

A novel quinazoline-2,4-dione derivative compound, specifically formulated as a pharmaceutical composition, is developed to protect nerve cells and treat neurological brain diseases by addressing mechanisms of nerve cell death, including excitotoxicity and oxidative stress.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for neurological brain diseases are used, then some therapeutic effect is achieved, but efficacy and toxicity problems persist

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing a new chemical compound (quinazoline-2,4-dione derivative) with modified molecular structure and properties. The compound features specific substituents (R1-R8 groups) and structural parameters (n, l, m, p values) that are optimized to achieve selective neuroprotection with reduced toxicity compared to existing treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite therapeutic approach by combining the quinazoline-2,4-dione core structure with various functional groups and substituents to produce a series of derivative compounds with tailored properties for specific neurological conditions

Inventive Principle:
Principle #40Composite materials

2Reliability

If thrombolytic agents are administered within 3 hours after cerebral infarction, then functional status is improved, but the treatment window is very limited

Engineering Contradiction:
Improvefunctional status improvementVSAvoidtreatment time window
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The compound acts by suppressing excitotoxicity and oxidative stress that occur early in the ischemic cascade, providing neuroprotection before irreversible cell death occurs. This mechanism allows for a potentially extended treatment window compared to thrombolytics

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The quinazoline derivative pre-empts the harmful effects of excessive glutamate release and free radical generation by blocking their toxic actions on neurons, thereby preventing cell death before it becomes irreversible

Inventive Principle:
Principle #9Preliminary anti-action

3Reliability

If NMDA glutamate receptor antagonist is used to suppress nerve cell death by ischemic stroke, then cell death is suppressed, but development of new drugs is delayed due to efficacy and toxicity problems

Engineering Contradiction:
Improvenerve cell protectionVSAvoiddrug development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The compound achieves selective action by targeting specific receptors and pathways involved in excitotoxicity and oxidative stress in the nervous system, while minimizing effects on other physiological systems, thereby reducing systemic toxicity

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS9290480B2Quinazoline-2,4-dione derivative, and medical compositions for the prophylaxis and treatment of cranial nerve disease containing the same
Publication Date: 2016.03.22 SHIN POONG PHARMA CO LTD
  • US9290480B2 patent drawing
  • US9290480B2 patent drawing
  • US9290480B2 patent drawing

AI summary

The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease.