SOFOSBUVIR CRYSTAL AND PREPARATION METHOD THEREOF

WIPO Patent Application WO/2016/070569

A1

Disclosed are four novel sofosbuvir crystals, namely Crystal H1, Crystal H2, Crystal H3 and Crystal H4, and method for preparing the four crystals. The structures and unit cell parameters of the four novel sofosbuvir crystals are determined by employing a single crystal X-ray diffraction analysis. A diffraction angle 2θ of the Crystal H1 has characteristic peaks at 4.9°, 6.6°, 7.1°, 8.2°, 9.6°, 16.5°, 19.0°, 19.2°, 19.9° and 24.9°; a diffraction angle 2θ of the Crystal H2 has characteristic peaks at 6.7°, 7.0°, 9.7°, 19.1°, 19.3°, 19.8°, 20.3°, 24.9°, 25.1° and 25.6°; a diffraction angle 2θ of the Crystal H3 has characteristic peaks at 5.1°, 6.7°, 7.1°, 9.6°, 15.8°, 17.2°, 19.3°, 19.9°, 20.7° and 24.9°; and a diffraction angle 2θ of the Crystal H4 has characteristic peaks at 5.5°, 5.6°, 10.0°, 10.9°, 10.9°, 16.6°, 19.8°, 20.0°, 20.4° and 25.0°. The four novel sofosbuvir crystals respectively have good physicochemical properties, good stability and good solubility, and are easy to prepare and handle.

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HU YONGBO (CN)

PCT/CN2015/076124

May 12, 2016

April 09, 2015

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CHARM PHARMATECH NANJING CO LTD (CN)

C07H19/10; C07H1/06

CN102858790A	2013-01-02
CN104130302A	2014-11-05

MICHAEL, J.S. ET AL.: "Discovery of a beta-D-2' - Doxy-2'-r-fluoro-2'-beta-C-methyluridine Nucleotide Prodrug (PSI-7977) for the Treatment of Hepatitis C Virus", J. MED. CHEM., vol. 53, no. 19, 19 October 2010 (2010-10-19), pages 7214, XP055004442

NANJING SUGAO PATENT AND TRADEMARK FIRM (ORDINARY PARTNERSHIP) (CN)
南京苏高专利商标事务所(普通合伙） (CN)

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