ALDH2 Modulator Crystalline Forms for Stability and Processability
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Solution Overview
Problem
There is a need for improved forms of ALDH2 modulating compounds, such as those represented by Formulae I, III, and IV, with enhanced stability and processability, as well as improved processes for preparing these compounds.
Innovation Solution
The development of novel crystalline forms of ALDH2 modulating compounds, both with and without coformers, which exhibit improved stability and processability, and can be used in pharmaceutical formulations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If crystalline forms of ALDH2 modulating compounds are developed, then stability and processability are improved, but the complexity of the patent document increases
Solution Approach 1:
The patent segments the compound into different crystalline forms (Form I, Form II, Form III, etc.) with distinct properties. Each crystalline form is characterized by specific X-ray diffraction patterns, making it easier to identify and work with stable forms in pharmaceutical applications.
Solution Approach 2:
The patent utilizes changes in physical parameters (crystalline structure, melting point, solubility) to create distinct forms of the same compound. By controlling crystallization conditions, the patent achieves improved stability and processability through selecting appropriate crystalline forms.
2Ease of manufacture
If co-crystalline forms with coformers are used, then processability is improved, but the number of components increases
Solution Approach 1:
The patent introduces coformers (such as organic acids, bases, or neutral molecules) as intermediary substances that facilitate the formation of stable crystalline structures. These coformers act as mediators between the active compound and the crystallization process, improving processability while maintaining a limited set of suitable coformer options.
Solution Approach 2:
The patent creates composite crystalline structures by combining the active ALDH2 modulating compound with coformers in specific ratios and configurations. These composite crystalline forms exhibit improved processability characteristics while the number of coformer types is controlled to a manageable set.
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 novel crystalline forms provide enhanced stability and processability, making them suitable for pharmaceutical applications and potentially effective in treating alcohol-related disorders.
Implementation Method 1
The present disclosure provides novel crystalline forms of a compound of any one of the Formulae, as described or provided for herein, such as Formula I, Formula III, and Formula IV with or without coformer
Data Source
AI summary
The present disclosure provides novel crystalline forms of a compound that acts as an ALDH2 effector, processes for preparing the crystalline forms of the compound with or without coformer, and uses thereof.