A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid

IL315950BActive Publication Date: 2026-08-01SAGE THERAPEUTICS LLC
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Patent Information

Application Number
IL315950
Authority / Receiving Office
IL · IL
Patent Type
Patents
Current Assignee / Owner
Priority Date
2016-08-23
Filing Date
2017-08-23
Publication Date
2026-08-01
Estimated Expiration
2037-08-23

AI Technical Summary

Technical Problem

Current neuroactive steroids lack effective crystalline forms that can modulate brain excitability and treat CNS-related diseases, necessitating the development of new crystalline steroid forms with improved properties.

Method used

The development of novel crystalline forms of a 19-nor C21-pyrazolyl steroid, specifically characterized by XRPD patterns, thermal stability, and solubility, which are converted through methods like slow evaporation, anti-solvent addition, and slurry conversion, and evaluated using techniques such as XRPD, TGA, and DSC to identify stable and effective forms for pharmaceutical use.

Benefits of technology

These crystalline forms exhibit enhanced stability and solubility, enabling effective modulation of brain excitability and treatment of CNS-related disorders, including sleep disorders, mood disorders, and neurological conditions, by providing a stable and bioavailable pharmaceutical composition.

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Abstract

This invention relates to a 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I) and crystalline solid forms and compositions thereof. Also disclosed herein are methods of making crystalline solid forms of the 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I) and methods of using the 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I) or crystalline solid forms, pharmaceutically acceptable salts, and pharmaceutically acceptable compositions thereof.
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