DASATINIB SALTS IN CRYSTALLINE FORM Russian patent published in 2018 - IPC C07D417/12 A61K31/506 C07D275/06 

Abstract RU 2662805 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a crystalline dasatinib salt containing a cation of a compound of formula 1, also known as dasatinib, and an anion of saccharin. Crystalline salt of the invention is obtained by carrying out the following steps: a) providing a compound of formula 1, also known as dasatinib, in a suitable solvent or mixture of solvents selected from the group consisting of C1-C4 alcohols, water or mixtures thereof; b) adding saccharin to the mixture from step a); d) crystallisation; f) isolation of the obtained precipitate. Process further comprises step c) of evaporating the composition obtained in step b), and step e) of evaporating to dryness or balancing the suspension obtained in step d). Crystalline salt of dasatinib with saccharin is used in a process for purifying dasatinib, which is a compound of formula 1.

.

EFFECT: crystalline salt of dasatinib with saccharin is intended to be used as an active substance for the manufacture of a pharmaceutical composition having properties of a tyrosine kinase inhibitor of the BCR/ABL and Src family, and cancer treatment, the cancer being chronic myelogenous leukemia and/or acute lymphoblastic leukemia complicated by the Philadelphia chromosome.

17 cl, 5 dwg, 4 tbl, 5 ex

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RU 2 662 805 C2

Authors

Khafner Andreas

Blatter Fritts

Shelagevich Martin

Zibenkhaar Bernd

Chiodo Titsiana

Khintermann Tobias

Salvador Beate

Fossen Markus

Dates

2018-07-31Published

2014-07-22Filed