Amyloid-Targeting Compounds With Improved GI Tolerability

Solution Overview

Problem

There is a lack of effective pharmaceutical agents that can disaggregate and/or prevent the formation of amyloid aggregates associated with diseases such as Alzheimer's disease and other amyloid-related conditions.

Innovation Solution

The use of specific compounds of structural formulas I, II, III, and IV, or their pharmaceutically acceptable salts, to treat diseases characterized by amyloid aggregates, including Alzheimer's disease, by administering these compounds to a subject in need thereof.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional pharmaceutical agents are used, then other therapeutic functions may be provided, but they cannot disaggregate and/or prevent formation of amyloid aggregates

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidability to treat amyloid aggregates

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of tramiprosate to create ALZ-801, specifically changing the amino acid side chain from beta-alanine to dimethyl-beta-alanine. This structural parameter change results in improved plasma exposure consistency and reduced gastrointestinal toxicity while maintaining amyloid aggregate disaggregation and prevention capabilities

Inventive Principle:

Principle #35Parameter changes

2Reliability

If tramiprosate is used to treat Alzheimer's disease, then amyloid aggregate disaggregation is achieved, but inconsistent plasma exposures and gastrointestinal toxicity occur

Engineering Contradiction:

Improveamyloid aggregate disaggregationVSAvoidGI tolerability

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of tramiprosate to create ALZ-801, specifically changing the amino acid side chain from beta-alanine to dimethyl-beta-alanine. This structural parameter change results in improved plasma exposure consistency and reduced gastrointestinal toxicity while maintaining amyloid aggregate disaggregation and prevention capabilities

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP3585373B1Compounds for use in methods for treating alzheimer's disease

Publication Date: 2026.02.11 ALZHEON INC

AI summary

Methods of treating a disease characterized by amyloid aggregates are provided herein.