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POLYMORPHIC, CRYSTALLINE AND MESOPHASE FORMS OF SODIUM 2-(5-BROMO-4-(4-CYCLOPROPYLNAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO)ACETATE, AND USES THEREOF
专利权人:
ARDEA BIOSCIENCES; INC.
发明人:
ZAMANSKY, IRINA,GALVIN, GABRIEL,GIRARDET, JEAN-LUC
申请号:
NZ60098411
公开号:
NZ600984A
申请日:
2011.01.05
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Abstract - 600984 Disclosed are crystalline polymorphs of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate including those characterised by peaks at 4.90, 9.83, 25.29, 6.86, 8.41, 10.13, 17.92, and 23.10 °2?±0.1°2?, characterised by an endothermic point onset at about 62°C as determined by differential scanning calorimetry with a heating rate of about 10°C/min. Other crystalline forms are also disclosed such as those characterised by peaks at 4.22, 8.51, 12.80 and 16.95 °2?±0.1°2?, and characterised by an endothermic point onset at about 173°C as determined by differential scanning calorimetry with a heating rate of about 10°C/min; characterized by peaks at 6.9, 10.1, 22.6, 23.3, 23.9, 25.2, 28.3 and 29.0 °2?±0.1°2?; characterized by peaks at 10.3, 17.8 and 25.2 °2?±0.1°2?; and also a form which is characterised by peaks at 10.5, 22.9, 23.2 and 24.6 °2?±0.1°2?. Further disclosed is a method for preparing a crystalline polymorph of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-trizaol-3-ylthio)acetate comprising: a) contacting amorphous sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-trizaol-3-ylthio)acetate with water and ethyl acetate; and b) isolating the solids from the mixture prepared in step a). Crystalline forms as disclosed above are useful for treating or preventing hyperuricemia, or a disease caused by elevated uric acid levels, and / or for treating or preventing gout.
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