3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one; antagonistic action against AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor and/or inhibitory action against kainate receptor prophylactic agent for neurodegenerative diseases
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Publication Number
US-7803818-B2
Publication Date
2010-09-28
Expiration Date
Abstract
An amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one.
Core Innovation
The invention relates to an amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one. The amorphous form is defined by absence of X-ray powder diffraction peaks and is characterized as distinct from a reference crystalline form.
The amorphous form is described for therapeutic and prophylactic use as an agent for neurodegenerative diseases. The disclosed neurodegenerative diseases include Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea, amyotrophic lateral sclerosis, spinocerebellar degeneration, epilepsy, and demyelinating disease, and the description frames these uses as central nervous system disorders.
The document further describes preparation and characterization of the amorphous form, including spray-drying, XRD, and solubility testing. Solubility in JP2 fluid (2nd fluid, pH 6.8) is reported relative to a reference crystalline form, and the amorphous form is linked to enhanced solubility behavior. The disclosure also includes pharmaceutical composition content involving inert carriers.
Claims Coverage
The independent claims cover a specific amorphous form of a dihydropyridine-2-one compound and a pharmaceutical composition comprising that amorphous form with an inert carrier. Across the claim set, three inventive features are defined.
Amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one
An amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one.
X-ray powder diffraction criterion defining the amorphous form
The amorphous form has absence of diffraction peaks in an X-ray powder diffraction pattern.
Pharmaceutical composition with an inert carrier
A pharmaceutical composition comprising the amorphous form and an inert carrier.
Overall, the claim coverage centers on a specific amorphous dihydropyridine-2-one, its definition by absence of X-ray powder diffraction peaks, and incorporation into a pharmaceutical composition using an inert carrier.
Stated Advantages
Improved solubility in JP2 fluid.
Documented Applications
Therapeutic and prophylactic agent for neurodegenerative diseases, including Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea, amyotrophic lateral sclerosis, spinocerebellar degeneration, epilepsy, and demyelinating disease.
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