SOLID FORMS OF ORTATAXEL Russian patent published in 2013 - IPC C07D493/04 A61K31/357 A61P35/00 

Abstract RU 2488586 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to solid forms of 1,14-carbonate 13-(N-Boc-β-isobutylserinyl)-14-b-hydroxybaccatineIII (Ortataxel) of formula

.

There are presented an amorphous form A, a crystalline form B, a mixture thereof and a method for preparing them. The amorphous form A is prepared by rapid deposition of ortataxel from the mixture of acetone and water. The form A is transformed into the form B when suspending and mixing in the mixture of ethanol and water for 4-8 hours. The suspension mixed for at least 4 hours is used to prepared the mixture of the form B and the form A. The form B or the mixtures of the forms A and B can be also produced by dissolving ortataxel in a proton organic solvent with water added thereafter; this compounds possess anticancer activity.

EFFECT: invention refers to the pharmaceutical composition on the basis of the crystalline form A and B or the mixture thereof for treating cancer.

26 cl, 4 ex, 13 dwg

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RU 2 488 586 C2

Authors

Chicheri Daniehle

Sardone Nikola

Gabetta Bruno

Rikotti Mauritsio

Dates

2013-07-27Published

2009-01-12Filed