Crystalline Spinogenesis Promoter Forms for Single-Polymorph Selection

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Solution Overview

Problem

There is a need for high purity single polymorph forms of compounds that promote spinogenesis with improved pharmacokinetic and/or pharmacodynamic profiles for the treatment of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease.

Innovation Solution

The development of crystalline forms of 2-(2-(2-(4-(benzo[d]thiazol-2-yl)phenoxy)ethoxy)ethoxy)ethan-1-ol (Compound I) characterized by specific X-ray powder diffractogram peaks, including Forms I, II, III, IV, V, and amorphous forms, which are used in pharmaceutical compositions to promote spinogenesis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If multiple polymorph forms of Compound I are synthesized, then the availability of different crystalline forms for pharmaceutical development is improved, but the complexity of characterizing and selecting the optimal single polymorph form worsens

Engineering Contradiction:

Improveavailability of different crystalline formsVSAvoidcomplexity of characterizing and selecting optimal polymorph

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying synthesis conditions (solvents, temperatures, pH levels, reaction times) to generate different polymorph forms of Compound I. Each polymorph is characterized by specific X-ray diffraction patterns and dissolution profiles, allowing selection of the optimal form for pharmaceutical applications based on desired properties such as solubility, stability, and bioavailability.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If high purity single polymorph forms are developed, then the pharmacokinetic and pharmacodynamic profiles are improved, but the manufacturing process complexity increases

Engineering Contradiction:

Improvepharmacokinetic and pharmacodynamic profilesVSAvoidmanufacturing process complexity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs preliminary action by pre-characterizing multiple polymorph forms and establishing their distinct properties before production. This includes determining X-ray diffraction patterns, dissolution rates, and stability profiles of each polymorph in advance, which guides the selection and optimization of manufacturing parameters to produce the desired single polymorph form with high purity and consistency.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent uses parameter changes to control polymorph formation during manufacturing by adjusting synthesis conditions such as solvent selection, temperature profiles, pH control, and crystallization rates. These parameter optimizations enable selective formation of the desired polymorph while minimizing the formation of other crystalline forms, thereby simplifying the purification process and improving manufacturing efficiency.

Inventive Principle:

Principle #35Parameter changes

3Measurement precision

If crystalline forms with specific X-ray powder diffractogram peaks are produced, then the structural characterization and identification are improved, but the time and resources required for comprehensive characterization increase

Engineering Contradiction:

Improvestructural characterization and identificationVSAvoidtime and resources for comprehensive characterization

Core Design Contradiction:

Measurement precisionVSLoss of time

Solution Approach 1:

The patent applies the principle of using distinctive physical characteristics (analogous to color changes) by establishing unique X-ray powder diffractogram peak patterns as fingerprint identifiers for each polymorph form of Compound I. Each polymorph is characterized by specific peak positions and intensities that enable rapid and unambiguous identification without requiring comprehensive structural analysis, thereby reducing characterization time and resources.

Inventive Principle:

Principle #32Color changes

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 crystalline forms of Compound I effectively enhance spinogenesis, providing therapeutic benefits for neurodegenerative diseases like Alzheimer's and Parkinson's disease, with improved stability and efficacy.

Implementation Method 1

crystalline 2-(2-(2-(2-(4-(benzo[d]thiazol-2-yl)phenoxy)ethoxy)ethoxy)ethoxy)ethan-1-ol (Compound I Form I) characterized by an X-ray powder diffractogram comprising the following peaks: about 4.6, about 20.8, and about 23.7°2θ±0.2°2θ, as determined on a diffractometer using Cu-Kα radiation

Methodology Applied

Scientific EffectX-ray diffraction: X-Ray

Data Source

PatentUS12486287B2Solid forms of a promoter of spinogenesis

Publication Date: 2025.12.02 SPINOGENIX INC

AI summary

Provided herein are crystalline forms of 2-(2-(2-(2-(4-(benzo[d]thiazol-2-yl)phenoxy)ethoxy)ethoxy)ethoxy)ethan-1-ol (Compound I): Also provided are processes of manufacture and methods of using the crystalline forms.