Oxadiazole Compounds for Refractory Epilepsy Treatment

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Solution Overview

Problem

Current epilepsy therapeutic agents have limitations in efficacy, with a significant proportion of patients experiencing refractory seizures despite treatment with established drugs like levetiracetam.

Innovation Solution

Development of a novel compound represented by Chemical Formula 1, or its optical isomers, stereoisomers, or pharmaceutically acceptable salts, which are used to create a pharmaceutical composition for the prevention or treatment of epilepsy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing epilepsy therapeutic agents (levetiracetam, topiramate, lamotrigine) are used, then treatment coverage is achieved, but efficacy for refractory patients is insufficient (30-40% of patients remain untreated)

Engineering Contradiction:
Improvetreatment efficacyVSAvoid适用范围
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of existing epilepsy medications by introducing oxadiazole rings and various substituents (halo, alkyl, alkoxy, carbamoyl groups) at different positions. This structural parameter change creates a series of novel compounds with potentially improved pharmacological properties and broader applicability to refractory epilepsy cases.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent combines the oxadiazole core structure with various functional groups and substituents to create composite molecular structures. These composite compounds integrate multiple pharmacophores that may work synergistically to enhance anticonvulsant activity and broaden the range of epilepsy types treated.

Inventive Principle:
Principle #40Composite materials

2Reliability

If novel compounds with improved efficacy are developed, then treatment effectiveness increases, but drug development complexity and time increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoiddrug development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically divides the molecular structure into a core oxadiazole unit and various substitutable positions (R1-R6 groups). This segmentation allows independent optimization of different molecular regions, enabling methodical development and testing of multiple derivatives without completely redesigning the entire molecule each time.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The oxadiazole core structure serves as a universal scaffold that can accommodate multiple different substituent groups while maintaining the fundamental anticonvulsant mechanism. This multi-functionality allows a single core structure to generate multiple candidate drugs with potentially different profiles for various epilepsy types.

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

Data Source

PatentUS20250034101A1Compound having oxadiazole and pharmaceutical composition containing the same
Publication Date: 2025.01.30 SK BIOPHARMACEUTICALS CO LTD
  • US20250034101A1 patent drawing
  • US20250034101A1 patent drawing
  • US20250034101A1 patent drawing

AI summary

Disclosed are oxadiazole compounds and pharmaceutically acceptable salts thereof. The compounds and pharmaceutically acceptable salts thereof are specifically suitable for the treatment of neurological diseases such as epilepsy.