CRYSTALLINE ANHYDROUS γ-MODIFICATION OF 4-(3'-CHLOR-4'-FLUORANILINO)-7-METHOXY-6-(3-MORPHOLINOPROPOXY)QUINAZOLINE, METHOD FOR PRODUCING IT AND BASED PHARMACEUTICAL COMPOSITION Russian patent published in 2016 - IPC C07D239/94 A61K31/5377 A61P35/00 

Abstract RU 2577518 C2

FIELD: medicine.

SUBSTANCE: invention concerns the new crystalline anhydrous γ-modification of 4-(3'-chlor-4'-fluoranilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline (international nonproprietary name is Gefinitib), which is characterised by the definite set of diffraction peaks (d, Å) and their intensity (Irelative, %) specified in cl.1 of the patent claim. The invention also refers to a method for producing and using it for preparing the pharmaceutical composition which is applicable in the pharmaceutical industry and medicine as a selective tyrosine kinase inhibitor for treating oncology diseases. The produced crystalline γ-modification of Gefinitib represents a white or off-white powder, odour-free, soluble in dimethyl sulphoxide, poorly soluble in ethanol and methanol, practically insoluble in water.

EFFECT: higher biological activity.

4 cl, 7 dwg, 3 tbl, 5 ex

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RU 2 577 518 C2

Authors

Malin Aleksandr Aleksandrovich

Mikhajlov Oleg Rostislavovich

Uvarov Nikolaj Aleksandrovich

Dates

2016-03-20Published

2014-06-02Filed