Polymorphic forms of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide
Inventors
Mollard, Paul • Giannousis, Peter • Suchit, Shazad • Mirmehrabi, Mahmoud • Cornell, Christopher R. • Wesson, Kieron E.
Assignees
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Publication Number
US-11938101-B2
Publication Date
2024-03-26
Expiration Date
Abstract
Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.
Core Innovation
The invention relates to a composition comprising polymorphs of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide. The composition is defined for an anhydrate, a hydrate, or a solvate, and it comprises polymorph Form I together with at least one additional polymorph selected from Form II, Form III, Form IV, Form V, and Form VI.
The solid forms are characterized by powder X-ray diffraction patterns with specified characteristic peak angular positions. The disclosed work includes XRPD characterization and form identification for polymorph Form I, Form II, Form III, Form IV, Form V, and polymorph Form VI, with an allowed variation of ±0.2°.
The disclosure includes XRPD pattern descriptions and tables reporting peak positions for each form, together with DSC/TGA/KF/solvent content/microscopy descriptors for the polymorph set. The compositions are linked to therapeutic use for treating or suppressing oxidative stress disorders, and the document states modulation, normalization, and/or enhancement of one or more energy biomarkers in that context.
Claims Coverage
The document includes one independent claim. The independent claim contains two inventive features: a defined polymorph combination requirement and form-specific powder X-ray diffraction peak requirements for the named polymorphs.
Polymorph Form I with at least one of Forms II–VI
A composition comprising a polymorph of an anhydrate, a hydrate, or a solvate of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide, wherein the composition comprises a polymorph Form I and at least one polymorph selected from Form II, Form III, Form IV, Form V, and Form VI.
Form-specific XRPD characteristic peaks with ±0.2 variation
A powder X-ray diffraction pattern requirement that ties polymorph Form I, and polymorphs Form II, Form III, Form IV, Form V, and Form VI, to characteristic peaks at specified angular positions, with the angular positions allowed to vary by ±0.2.
Overall, claim coverage centers on compositions containing a specific polymorph combination and on identification of each included polymorph via powder X-ray diffraction characteristic peaks with ±0.2° angular variation.
Stated Advantages
Documented Applications
No documented applications found
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