Polydeuterated Ambroxol Analogs for Stability and Prolonged Action

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Solution Overview

Problem

Existing ambroxol formulations face challenges in stability and duration of action, limiting their therapeutic efficacy in treating conditions such as Gaucher's disease, Parkinson's disease, and other neurological disorders.

Innovation Solution

Development of polydeuterated analogs of ambroxol and related compounds, which exhibit increased stability and resistance to metabolism, enhancing their pharmacokinetic properties and therapeutic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If polydeuterated analogs of ambroxol are developed, then stability and duration of action are improved, but manufacturing complexity increases

Engineering Contradiction:
ImprovestabilityVSAvoidmanufacturing complexity
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by replacing hydrogen atoms with deuterium atoms in the ambroxol molecular structure. This isotopic substitution modifies the physical and chemical parameters of the compound, specifically enhancing metabolic stability and prolonging duration of action while maintaining the core therapeutic activity of the original molecule.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures by combining the ambroxol core framework with deuterium-labeled substituents. These polydeuterated analogs represent composite materials at the molecular level, integrating stable deuterium-containing groups into the pharmacologically active scaffold to achieve enhanced therapeutic properties.

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If polydeuterated analogs of ambroxol are developed, then duration of action is prolonged, but production cost increases

Engineering Contradiction:
Improveduration of actionVSAvoidproduction cost
Core Design Contradiction:
Duration of action of moving objectVSEase of manufacture

Solution Approach 1:

The patent utilizes parameter changes through isotopic substitution, where deuterium replacement of hydrogen extends the duration of action by protecting against metabolic degradation. This fundamental parameter modification directly addresses the duration of action enhancement while the synthetic routes described provide a framework for managing production costs.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs copying strategies by synthesizing deuterated compounds from non-deuterated precursors using established organic synthesis methodologies. This approach allows replication of the successful ambroxol molecular scaffold with modifications that extend duration of action, leveraging existing synthetic knowledge to control production expenses.

Inventive Principle:
Principle #26Copying

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The polydeuterated ambroxol analogs demonstrate improved stability and prolonged action, effectively treating respiratory diseases, lysosomal storage disorders, and neurological conditions, while potentially extending life expectancy and improving healthspan.

Implementation Method 1

polydeuterated analogs of ambroxol and related compounds... which exhibit increased stability and resistance to metabolism, enhancing their pharmacokinetic properties and therapeutic effects

Methodology Applied
Scientific EffectDeuterium isotope effect:

Data Source

PatentUS20250235413A1Modified forms of ambroxol for therapeutic use
Publication Date: 2025.07.24 ZYWIE LLC
  • US20250235413A1 patent drawing
  • US20250235413A1 patent drawing
  • US20250235413A1 patent drawing

AI summary

The invention relates to polydeuterated analog forms of ambroxol and related compounds (including bromhexine and the ambroxol salt, ambroxol hydrochloride), compositions comprising same, and methods of preventing and/or treating various diseases and medical conditions involving the administration of polydeuterated analogs of ambroxol and related compounds.