Compound I Solid Forms for Stable High-Purity Hemoglobin Modulation
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Solution Overview
Problem
There is a need for high purity solid forms of Compound I that are efficacious for the treatment of diseases modulated by hemoglobin, particularly for conditions like sickle cell disease.
Innovation Solution
The development of various solid forms of Compound I, including crystalline and amorphous forms, as well as salts and solvates, which are characterized by specific X-ray diffraction peaks, melting points, and thermal stability, providing improved therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high purity solid forms of Compound I are developed, then therapeutic efficacy is improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by developing multiple crystalline forms (polymorphs) of Compound I with different physical and chemical parameters. Each polymorph (Forms I-VIII) has distinct X-ray diffraction patterns, melting points, and solubility characteristics. This allows optimization of therapeutic efficacy through selection of appropriate crystal forms while managing manufacturing complexity through systematic characterization of each form's properties.
Solution Approach 2:
The patent utilizes phase transitions by identifying and characterizing different solid-state phases (polymorphs) of Compound I. Each polymorph represents a distinct phase with unique stability and solubility properties. The patent describes methods for preparing and converting between these phases, enabling control over therapeutic performance while establishing standardized manufacturing protocols for each phase.
2Stability of the object's composition
If multiple solid forms (crystalline and amorphous) are developed, then stability and purity are enhanced, but characterization and quality control difficulty increases
Solution Approach 1:
The patent employs characteristic physical properties (analogous to color changes in TRIZ) for identification and characterization of different polymorphs. Each crystalline form has distinct X-ray diffraction patterns, melting points, and spectroscopic signatures that serve as fingerprint identifiers. This systematic characterization approach enables differentiation and quality control of multiple solid forms through measurable physical parameters.
Solution Approach 2:
The patent implements feedback mechanisms through comprehensive characterization data for each polymorph. The detailed XRPD patterns, DSC curves, and other analytical data provide feedback criteria for identifying and controlling the presence of specific polymorphs in pharmaceutical formulations. This enables quality assurance through measurable parameters that confirm the desired solid form is present.
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
These solid forms of Compound I exhibit enhanced stability and purity, offering improved therapeutic potential for treating diseases mediated by abnormal hemoglobin, such as sickle cell disease.
Implementation Method 1
characterized by specific X-ray diffraction peaks
Implementation Method 2
melting points, and thermal stability
Data Source
AI summary
Forms of (S)-2-hydroxy-6-((4-(2-(2-hydroxyethyl)nicotinoyl)morpholin-3-yl)methoxy)benzaldehyde (Compound I), or salts or solvates thereof, were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms of Compound I.