Solid state crystalline forms of a selective potassium channel modulator
Inventors
BICHLER, Paul Robert • CADIEUX, Jean-Jacques Alexandre • Tandy, Matthew David • Beatch, Gregory N.
Assignees
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Publication Number
US-12319657-B1
Publication Date
2025-06-03
Expiration Date
Abstract
The present disclosure provides solid state forms of a selective potassium channel modulator and pharmaceutical compositions comprising the solid state crystalline forms and pharmaceutically acceptable excipients, and methods for preparing and using the solid state forms and the pharmaceutical compositions thereof.
Core Innovation
The disclosure relates to solid-state crystalline forms of Compound A, identified as N-(4-(6-fluoro-3,4-dihydroisoquinolin-2(1H)-yl)-2,6-dimethylphenyl)-3,3-dimethylbutanamide. The crystalline forms are characterized by XRPD patterns with specified 2θ peak positions and peak counts, enabling form designation by XRPD fingerprints and form-specific characterization figures. The crystalline forms are also described in the context of polymorphism, mixtures of crystalline forms, and the possibility that the crystalline forms may be substantially free of other forms.
The disclosure further describes pharmaceutical compositions that include the crystalline form of Compound A with a pharmaceutically acceptable excipient. It also describes controlled, delayed, or quick release systems, including dissolutional polymer matrices, osmotic pump systems, polymer-coated reservoirs, and controlled particle dispersion systems, as well as pharmaceutical solid forms for use in formulations.
Analytical characterization of the crystalline forms is described using XRPD and form identification via XRPD figures, DSC, NMR fingerprints, TG/DTA, PLM, FTIR, Karl Fischer (KF), gravimetric vapor sorption (GVS), variable temperature XRPD (VT-XRPD), HPLC-UV, gas chromatography (GC), and particle size distribution (PSD). The disclosure connects the crystalline forms of Compound A to therapeutic use by describing administration concepts for treating seizure disorders in mammals and humans, including focal onset (partial onset) seizures.
Claims Coverage
The independent claims cover crystalline forms of Compound A defined by XRPD peak characterization, and corresponding pharmaceutical composition and therapeutic use. Across the independent claims, the inventive features primarily differ by the XRPD peak sets and peak-count requirements that define the crystalline forms, together with a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a method of treating seizure disorder in a human.
Crystalline form characterized by selected XRPD peaks
A crystalline form of Compound A characterized by three or more peaks in an XRPD pattern selected from 13.62, 14.16, 14.61, 18.44, 19.92, and 22.97 degrees 2θ ± 0.3 degrees 2θ.
Crystalline form characterized by XRPD peaks at 14.61, 18.44, and 22.97
A crystalline form of Compound A characterized by at least three peaks in an XRPD pattern at 14.61, 18.44, and 22.97 degrees 2θ ± 0.3 degrees 2θ.
Crystalline form characterized by XRPD peaks at 13.62, 14.16, and 19.92
A crystalline form of Compound A characterized by peaks in an XRPD pattern at 13.62, 14.16, and 19.92 degrees 2θ ± 0.2 degrees 2θ.
Pharmaceutical composition with a pharmaceutically acceptable excipient and crystalline form
A pharmaceutical composition that includes a pharmaceutically acceptable excipient and a therapeutically effective amount of a crystalline form of Compound A.
Method of treating a seizure disorder in a human by administering the crystalline form
A method for treating a seizure disorder in a human by administering a therapeutically effective amount of the crystalline form of Compound A.
Overall, the claim coverage is centered on crystalline forms of the specified Compound A defined by XRPD peak-position requirements, with claim pathways into pharmaceutical composition and methods for treating seizure disorders in humans by administering the defined crystalline form.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Pharmaceutical compositions comprising the crystalline form of Compound A are described for multiple administration routes, including rectal suppository, intramuscular and intrathecal, intravenous, intranasal delivery, intravaginal shell or core devices, and aerosol dosage units.
A method for treating a seizure disorder in a human by administering a therapeutically effective amount of the crystalline form of Compound A is described.
The disclosure describes administration concepts for treating seizure disorders in mammals and humans, including focal onset (partial onset) seizures.
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