Crystalline inhibitor of 4-hydroxyphenylpyruvate dioxygenase
AssigneeDipharma S.p.A.
InventorEmanuele Attolino
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Abstract
The present invention relates to an improved synthesis and crystallization process of the 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione, also known as nitisinone or NTBC.
Claims13
A method of inhibiting 4-hydroxyphenylpyruvate dioxygenase enzyme in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of crystalline 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione having a X-ray powder diffraction pattern with at least five specific peaks at about 2-theta=7.4, 14.7, 15.7, 22.9, and 29.7, wherein said peaks may be plus or minus 0.2° 2-theta and have an intensity of at least 30%.
A method of treating oculocutaneous/ocular albinism, microbial infections, restless leg syndrome, alkaptonuria, or hereditary tyrosinemia type 1, the method comprising administering to a patient in need thereof a therapeutically effective amount of crystalline 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione having X-ray powder diffraction pattern with at least five specific peaks at about 2-theta=7.4, 14.7, 15.7, 22.9, and 29.7, wherein said values may be plus or minus 0.2° 2-theta and have an intensity of at least 30%.
A method of treating oculocutaneous/ocular albinism, microbial infections, restless leg syndrome, alkaptonuria, or hereditary tyrosinemia type 1, the method comprising administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical formulation comprising crystalline 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione having X-ray powder diffraction pattern with at least five specific peaks at about 2-theta=7.4, 14.7, 15.7, 22.9, and 29.7, wherein said values may be plus or minus 0.2° 2-theta and have an intensity of at least 30%.
Dependencies are inferred from the claim text.