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Publication Number
US-11717516-B2
Publication Date
2023-08-08
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 co-crystal comprising itanapraced and a coformer, wherein the coformer is nicotinamide. It defines the co-crystal identity by an X-ray Powder Diffraction Pattern (XRPD) having specific peak positions expressed as 2θ values measured from a Cu radiation source after Ni filtering. The patent characterizes the solid-state behavior of the co-crystal using XRPD and thermal characterization.
The disclosure addresses the need for an AICD inhibitor/binder targeting amyloid precursor protein (APP) intracellular domain (AICD) for neurodegeneration and neuroinflammation, including infections and dementia disorders, while improving physical properties relevant to solid-state pharmaceutical performance. The approach is framed as co-crystal formation with nicotinamide as a coformer to obtain a distinct solid form associated with improved properties.
The disclosed co-crystal is intended for in vivo coformer dissociation and is associated with improved physical properties. These include reduced hygroscopicity and improved water solubility, dissolution, and bioavailability concepts, with intended pharmacokinetic outcome described in terms of reduced time to Cmax and altered exposure metrics such as Cmax, Tmax, and AUC.
Claims Coverage
The document provides one independent claim defining the co-crystal by its XRPD peaks and Cu radiation conditions, and dependent claims that further specify comparative physical and thermal properties, as well as formulation into solid dosage forms and pharmaceutical compositions. Across the independent claim set, the inventive features center on an XRPD-defined co-crystal identity using nicotinamide as the coformer with specified peak positions.
Nicotinamide coformer co-crystal of itanapraced
A co-crystal comprising itanapraced and a coformer, wherein the coformer is nicotinamide.
Xrpd peak-defined co-crystal identity with cu radiation after ni filtering
The co-crystal has an X-ray Powder Diffraction Pattern (XRPD) with specific peaks expressed in 2θ from a Cu radiation source 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.
Overall claim coverage centers on a nicotinamide coformer co-crystal of itanapraced, uniquely defined by a specified XRPD pattern under Cu radiation after Ni filtering, with dependent claims additionally specifying comparative hygroscopicity, comparative water solubility, DSC thermal parameters, and solid dosage forms and pharmaceutical compositions with pharmaceutically acceptable excipients.
Stated Advantages
Less hygroscopic than itanapraced.
More water soluble than itanapraced.
Documented Applications
Use as an AICD inhibitor/binder to amyloid precursor protein (APP) intracellular domain (AICD) targeting neurodegeneration and neuroinflammation.
Use in infections, including COVID-19-related neuroinfection and acute respiratory stress syndrome (ARDS).
Use in dementias.
Use in injury.
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