Crystalline anhydrous form of Cabazitaxel, process for the preparation and pharmaceutical compositions thereof

Patent metadata

Field	Value
Publication number	US-9586919-B2
Application number	US-201415030620-A
Country	US
Kind code	B2
Filing date	Oct 9, 2014
Priority date	Oct 23, 2013
Publication date	Mar 7, 2017
Grant date	Mar 7, 2017

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.

First claim

The invention claimed is:

1. An anhydrous crystalline form, referred to as form H, of Cabazitaxel of formula (I)

wherein the anhydrous crystalline form has
an X-RPD pattern obtained using the copper wavelengths λ 1 and λ 2 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.

2. Pharmaceutical compositions comprising the anhydrous crystalline form H according to claim 1 in admixture with at least one pharmaceutically suitable excipient.

3. A process for the preparation of the anhydrous crystalline form H according to claim 1 , comprising:
dissolving Cabazitaxel in a decanoyl- and octanoyl-triglycerides or glycerol trioctanoate to form a mixture;
adding heptane to said mixture;
filtering said mixture to obtain crystals of said form H.

Assignees

• Indena Spa

Inventors

• Cabri Walter
• Ciceri Daniele
• Domenighini Luca
• Gambini Andrea
• Peterlongo Federico

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D305/14 Primary

  condensed with carbocyclic rings or ring systems · CPC title

• A61K31/337

  having four-membered rings, e.g. taxol · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title