Crystalline Compound I Forms for Hyperuricemia Treatment
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Solution Overview
Problem
There is a need for effective treatments for hyperuricemia and gout, as existing compounds have not adequately addressed these conditions.
Innovation Solution
Development of crystalline forms of 3-bromo-5-[(2-ethylimidazo[1,2-a]pyridin-3-yl) carbonyl]-2-hydroxybenzonitrile (Compound I) or its pharmaceutically acceptable salts and solvates, which are used in pharmaceutical compositions to treat or prevent hyperuricemia and gout.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing compounds are used for treating hyperuricemia and gout, then treatment is provided, but the treatment is not adequate or effective enough
Solution Approach 1:
The patent develops multiple crystalline forms (Forms 1-12) of Compound I with different physical and chemical parameters including solubility, stability, melting point, and bioavailability. Each crystalline form has distinct characteristics optimized for different therapeutic needs, allowing selection of the most appropriate form for specific patient conditions and treatment requirements.
Solution Approach 2:
The patent creates pharmaceutical compositions that combine Compound I in various crystalline forms with pharmaceutically acceptable excipients, carriers, and adjuvants. These composite formulations enhance the therapeutic effectiveness, stability, and deliverability of Compound I for treating hyperuricemia and gout.
2Reliability
If crystalline forms of Compound I are developed with varying physical properties, then therapeutic benefits are optimized, but the complexity of selecting and manufacturing appropriate forms increases
Solution Approach 1:
The patent segments Compound I into multiple distinct crystalline forms (Forms 1-12), each with well-defined and characterized properties. This segmentation allows the pharmaceutical industry to select specific crystalline forms based on desired characteristics such as solubility, stability, or bioavailability, and to manufacture each form using optimized, form-specific processes.
Solution Approach 2:
By establishing distinct physical and chemical parameters for each crystalline form (melting point, solubility, stability profiles, XRPD patterns), the patent creates a systematic framework for selecting and manufacturing appropriate forms. Each form's parameters are clearly defined, enabling rational selection based on therapeutic needs and manufacturing capabilities.
Data Source
AI summary
Crystalline forms of Compound I, active on URAT1, were prepared and characterized: Also provided are methods of using the crystalline forms.