CRYSTALLINE γ-MODIFICATION OF N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINOLINE AMINE OF BIS (4-METHYLBENZENESULFONATE) MONOHYDRATE, METHOD OF ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION BASED THEREON Russian patent published in 2016 - IPC C07D405/04 A61K31/517 A61P35/00 

Abstract RU 2603943 C1

FIELD: pharmaceutics.

SUBSTANCE: invention relates to novel crystalline anhydrous modification N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinoline amine of bis (4-methylbenzenesulfonate) monohydrate (lapatinib ditosylate monohydrate), in particular γ-modification, characterized by certain set of diffraction maxima (d, Å) and their intensity (Irelative, %) and certain thermal effects and their temperatures on curve of differential scanning calorimetry, as well as to method of its production and use in pharmaceutical compositions as reversible selective inhibitor of intracellular tyrosine kinase receptor of epidermal growth factor for treating advanced and/or metastatic breast cancer.

EFFECT: increased biological activity.

4 cl, 5 dwg, 3 tbl, 4 ex

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RU 2 603 943 C1

Authors

Mikhajlov Oleg Rostislavovich

Uvarov Nikolaj Aleksandrovich

Malin Aleksandr Aleksandrovich

Dates

2016-12-10Published

2016-02-01Filed