CRYSTAL OF 2-AMINO-6-(4-METHOXYPHENYLTHIO)-9-(2-(PHOSPHONOMETHOXY)ETHYL) PURINE BIS(2,2,2-TRIFLUOROETHYL) ESTER

PURPOSE: Crystals of a 2-amino-6-(4-methoxyphenylthio)-9-(2-(phosphonomethoxy)ethyl) purine bis(2,2,2-trifluoroethyl) ester, the ester in an amorphous state, and a medicinal composition containing the same as an active ingredient are provided, which compounds have improved antiviral activity and are...

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Hauptverfasser: SEKIYA KOICHI, SHIROSAKA TADASHI, YOSHIZAWA KATSUYOSHI, MASUNAGA TOSHIO, INOKAWA HARUKI, UBASAWA KEN, YAMADA HIROYUKI
Format: Patent
Sprache:eng ; kor
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Zusammenfassung:PURPOSE: Crystals of a 2-amino-6-(4-methoxyphenylthio)-9-(2-(phosphonomethoxy)ethyl) purine bis(2,2,2-trifluoroethyl) ester, the ester in an amorphous state, and a medicinal composition containing the same as an active ingredient are provided, which compounds have improved antiviral activity and are useful for an orally available and highly safe antiviral agent. CONSTITUTION: The crystals of a 2-amino-6-(4-methoxyphenylthio)-9-(2-(phosphonomethoxy) ethyl) purine bis(2,2,2-trifluoroethyl) ester have the physicochemical properties of: (1) having a diffraction peak(2theta) at 27.9 degree +- 0.2 degree in powder X-ray diffraction pattern; (2) having an endothermic peak at about 93 deg.C in DSC(Differential Scanning Calorimetry); (3) having a chemical shift peak of 24.0 ppm in solid 31P-NMR spectrum; and (4) having a diffraction peak at 3192 +- 2 cm¬-1 in infrared absorption spectrum.