Crystalline forms of cabazitaxel
First Claim
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1. A crystalline form of cabazitaxel selected from the ethyl acetate solvate, the tetrahydrofuran solvate, the methyl ethyl ketone solvate, the diethyl ketone solvate, the diethyl carbonate solvate, or the dimethyl sulfoxide solvate, wherein said crystalline form is substantially free of other crystalline forms;
- andthe ethyl acetate solvate is characterized by an XRPD pattern that comprises peaks at 7.9, 8.6, and 10.1 (+0.1 degrees 2θ
);
the tetrahydrofuran solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.9, and 10.2 (±
0.1 degrees 2θ
);
the methyl ethyl ketone solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.8, and 10.1 (±
0.1 degrees 2θ
);
the diethyl ketone solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.8, and 10.1 (±
0.1 degrees 2θ
);
the diethyl carbonate solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.6, and 10.1 (±
0.1 degrees 2θ
); and
the dimethyl sulfoxide solvate is characterized by an XRPD pattern that comprises peaks at 7.2, 7.6, and 8.2 (±
0.1 degrees 2θ
).
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Abstract
The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.
12 Citations
8 Claims
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1. A crystalline form of cabazitaxel selected from the ethyl acetate solvate, the tetrahydrofuran solvate, the methyl ethyl ketone solvate, the diethyl ketone solvate, the diethyl carbonate solvate, or the dimethyl sulfoxide solvate, wherein said crystalline form is substantially free of other crystalline forms;
- and
the ethyl acetate solvate is characterized by an XRPD pattern that comprises peaks at 7.9, 8.6, and 10.1 (+0.1 degrees 2θ
);the tetrahydrofuran solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.9, and 10.2 (±
0.1 degrees 2θ
);the methyl ethyl ketone solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.8, and 10.1 (±
0.1 degrees 2θ
);the diethyl ketone solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.8, and 10.1 (±
0.1 degrees 2θ
);the diethyl carbonate solvate is characterized by an XRPD pattern that comprises peaks at 7.8, 8.6, and 10.1 (±
0.1 degrees 2θ
); andthe dimethyl sulfoxide solvate is characterized by an XRPD pattern that comprises peaks at 7.2, 7.6, and 8.2 (±
0.1 degrees 2θ
). - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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Specification
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Current AssigneeScinopharm Taiwan Limited
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Original AssigneeScinopharm Taiwan Limited
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InventorsHenschke, Julian Paul, Hsiao, TsungYu, Ho, MengFen, Huang, YuanChang
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Primary Examiner(s)Heyer, Dennis
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Assistant Examiner(s)PODGORSKI, DANIEL MICHAEL
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Application NumberUS13/965,015Publication NumberTime in Patent Office288 DaysField of SearchNoneUS Class Current549/510CPC Class CodesA61K 31/337 having four-membered rings,...A61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...C07D 305/14 condensed with carbocyclic ...
