Sulfamate Derivative Compounds for Epilepsy Treatment

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current antiepileptic drugs suffer from significant side effects and are ineffective for a substantial percentage of epilepsy patients, leaving about 30% untreated despite advancements since 1989.

Innovation Solution

Development of a pharmaceutical composition containing sulfamate derivative compounds, which provide enhanced anti-epileptic activity with reduced side effects, as represented by specific chemical formulas and structures, for treating or preventing epilepsy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If older established antiepileptic drugs (phenytoin, carbamazepine, clonazepam, ethosuximide, valproic acid, barbiturates) are prescribed, then epilepsy treatment coverage is achieved, but significant side effects occur

Engineering Contradiction:
Improveantiepileptic efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention modifies the chemical structure of existing sulfamate derivative compounds by changing parameters such as substituent groups (R1-R6) on the core molecular structure. This structural optimization allows the compound to maintain antiepileptic efficacy while reducing harmful side effects through improved selectivity and metabolic profile

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent develops composite pharmaceutical compositions containing sulfamate derivative compounds combined with pharmaceutically acceptable excipients and carriers. This composite approach enhances therapeutic effectiveness while minimizing adverse reactions through optimized formulation and delivery systems

Inventive Principle:
Principle #40Composite materials

2Reliability

If currently available therapeutic agents are used, then some epilepsy patients are treated, but 20-30% of patients remain resistant

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpatient population coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention optimizes key pharmacological parameters including potency, selectivity, and pharmacokinetic properties of sulfamate derivative compounds. These parameter improvements enable the drug to effectively treat previously resistant patient populations by targeting different seizure mechanisms or overcoming metabolic resistance

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces specific substituent patterns (R1-R6 groups) that create localized functional properties in different regions of the molecule. This local optimization allows the compound to interact with specific neuronal targets while avoiding off-target effects that cause resistance, thereby expanding applicability to resistant patient groups

Inventive Principle:
Principle #3Local quality

3Reliability

If new AEDs (felbamate, gabapentin, lamotrigine, oxcarbazepine, tiagabine, topiramate, vigabartrin, zonisamide, levetiracetam) are launched, then improved efficacy and side-effect profiles are achieved, but about 30% of patients remain untreated

Engineering Contradiction:
Improveefficacy and side-effect profileVSAvoiduntreated patient population
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention further refines pharmacological parameters of sulfamate derivatives by optimizing the balance between potency and safety margin. This continued parameter optimization addresses the remaining untreated population by creating a drug with superior therapeutic index that can effectively treat cases resistant to previously launched new AEDs

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9937145B2Sulfamate derivative compound for use in preventing or treating epilepsy
Publication Date: 2018.04.10 BIO PHARM SOLUTIONS
  • US9937145B2 patent drawing
  • US9937145B2 patent drawing
  • US9937145B2 patent drawing

AI summary

The present invention relates to a pharmaceutical composition for treating or preventing epilepsy containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention epilepsy comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of epilepsy.