A crystalline anhydrous form of cabazitaxel, process for the preparation and pharmaceutical compositions thereof
AssigneeIndena S.p.A.
InventorsWalter Cabri, Daniele Ciceri, Luca Domenighini, Andrea Gambini, Federico Peterlongo
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Abstract
The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present invention is a processes for the preparation of the above mentioned form H by recrystallization of Cabazitaxel from a mixture of decanoyl- and octanoyl triglycerides or from glycerol trioctanoate. Form H of Cabazitaxel is useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof. It is also particularly useful as a medicament, especially for the treatment of cancers.
Claims4
An anhydrous crystalline form, referred to as form H, of Cabazitaxel of formula (I)
- wherein the anhydrous crystalline form has one or more of the following:
- an X-RPD pattern obtained using the copper wavelengths λ1 and λ2 of 1.54056 Å and 1.54439 Å, respectively, comprising distinctive reflections, expressed as 2-theta degrees values, at 5.8, 6.5, 8.1, 9.5, 10.9, 11.5, 12.2, 13.0, 14.1, 14.8, 16.8, 17.2, 19.0, 19.4, 20.1, 21.9 and 24.0±0.2;
- an X-RPD pattern obtained using the copper wavelengths λ1 and λ2 of 1.54056 Å and 1.54439 Å, respectively, essentially as depicted in FIG. 1;
- TG and DTA profiles obtained with a linear heating rate of 10° C./min essentially as depicted in FIG. 3;
- a DSC profile obtained with a linear heating rate of 10° C./min essentially as depicted in FIG. 4;
Dependencies are inferred from the claim text.