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Publication Number
US-12290515-B2
Publication Date
2025-05-06
Expiration Date
Abstract
Co-crystals of itanapraced; methods of preparation of the co-crystals; uses of the co-crystals as APIs; formulations containing the co-crystals; uses of the co-crystals and formulations for prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries; and methods of prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries are described.
Core Innovation
The invention relates to a method of treating Alzheimer's disease in a human in need thereof by administering a therapeutically effective dosage regimen of a co-crystal comprising itanapraced and nicotinamide. The co-crystal is characterized by an X-ray Powder Diffraction Pattern (XRPD) with specific peaks at about 14.63°, 14.90°, 15.56°, 16.71°, 18.24°, 18.46°, 20.03°, 20.27°, 22.01°, 22.27°, 24.17°, 24.47°, 26.14°, 26.47°, 27.83°, 28.85°, 29.97°, 30.64°, 32.42°, 34.07°, and 39.14°, all ±0.2 degrees 2θ, produced from a Cu radiation source (λ=1.54 Å after Ni filtering).
The co-crystal is described as being associated in a nonionic/noncovalent crystal-lattice manner and as having improved physicochemical properties compared with parent components. The patent emphasizes improved water solubility, reduced hygroscopicity, improved stability, and improved rate of dissolution and bioavailability-related metrics including Cmax, Tmax, and AUC.
The document also frames the co-crystal as functioning as an APP/AICD intracellular domain modulator and as a microglia modulator for preventing or treating neurodegeneration, inflammation, and related disorders. In the provided description content, aqueous solubility screening for coformers and CSP-1103 is used to consolidate solubility results for selecting suitable coformers/solvents for co-crystal formation, with XRPD confirmation used to verify outcomes.
Claims Coverage
Across the independent and dependent claims, the core inventive concept is treating Alzheimer's disease by dosing a specifically defined itanapraced–nicotinamide co-crystal, where identity is established by a defined XRPD peak set under Cu radiation with Ni filtering. The claims further narrow administration by specifying oral dosing, a 1 to 4 times per day regimen, and a daily dose range of about 3 mg/day to about 3000 mg/day, with additional refinement by stoichiometric ratio and substantial similarity to FIG. 3A.
Treating Alzheimer's disease with an itanapraced-nicotinamide co-crystal dosage regimen
Administering a therapeutically effective dosage regimen of a co-crystal comprising itanapraced and nicotinamide to a human in need thereof for treating Alzheimer's disease.
Co-crystal defined by an XRPD peak set under Cu radiation (Ni filtered)
The co-crystal has an X-ray Powder Diffraction Pattern (XRPD) with specified peaks expressed in 2θ produced from a Cu radiation source (λ=1.54 Å after Ni filtering) at about 14.63°; 14.90°; 15.56°; 16.71°; 18.24°; 18.46°; 20.03°; 20.27°; 22.01°; 22.27°; 24.17°; 24.47°; 26.14°; 26.47°; 27.83°; 28.85°; 29.97°; 30.64°; 32.42°; 34.07°; and 39.14°, all ±0.2 degrees 2θ.
Compositional stoichiometric ratio constraint for itanapraced and nicotinamide
The stoichiometric ratio of itanapraced to nicotinamide is within a defined range.
XRPD substantially the same as the XRPD shown in FIG. 3A
The X-ray Powder Diffraction Pattern (XRPD) is substantially the same as the XRPD shown in FIG. 3A.
Oral administration of the co-crystal
Administering the co-crystal orally.
Dosing frequency of 1 to 4 times per day
Administering the co-crystal 1 to 4 times per day.
Daily dose range of about 3 mg/day to about 3000 mg/day
Administering the co-crystal at a dose ranging from about 3 mg/day to about 3000 mg/day.
The claims center on an Alzheimer's treatment method using a therapeutically effective dosage regimen of an XRPD-defined itanapraced and nicotinamide co-crystal. The inventive features are the co-crystal identity defined by the specified XRPD peak set, plus dependent refinements for stoichiometric ratio, XRPD similarity to FIG. 3A, oral administration, dosing frequency, and daily dose range.
Stated Advantages
Improved physicochemical properties, including higher water solubility.
Reduced hygroscopicity.
Improved stability.
Improved rate of dissolution and bioavailability-related performance metrics (Cmax, Tmax, and AUC).
Low hygroscopicity/non-hygroscopic behavior at 95% RH and no solid-state form change upon cycling.
Documented Applications
Treating Alzheimer's disease in a human in need thereof.
Preventing or treating neurodegeneration through modulation of APP/AICD intracellular domain and microglia modulation.
Microglia modulation and neuroinflammation-related prevention or treatment contexts described in connection with the co-crystal approach.
Solubility assessment for selecting suitable coformers/solvents for co-crystal formation with CSP-1103, followed by XRPD confirmation of outcomes.
Treating Alzheimer's disease in a human in need thereof by administering a therapeutically effective dosage regimen of an itanapraced–nicotinamide co-crystal.
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