SALTS OF 4-METHYL-N-[3-(4-METHYLIMIDAZOLE-1-YL)-5-TRIFLUOROMETHYLPHENYL]-3-(4-PYRIDINE-3-YLPYRIMIDINE-2-YLAMINO)BENZAMIDE Russian patent published in 2016 - IPC C07D401/14 A61K31/506 A61P35/00 

Abstract RU 2605551 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel salts of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide (nilotinib), which have protein kinase inhibitor properties and can be used for treating diseases responding to protein kinase activity inhibition. Salts are selected from hydrochloride, diphosphate, sulphate, methanesulphonate, ethanesulphonate, benzolesulphonate and n-toluene sulphonate. Method involves the stage for reacting 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide in the form of a free base with the corresponding acid of formula HB selected from the said acids in a solvent medium. Invention also relates to a pharmaceutical composition containing: (a) a therapeutically effective amount of the salt and (b) at least one pharmaceutically acceptable carrier, a diluent, an adjuvant or an excipient.

EFFECT: method of treating involves introducing a patient requiring such treatment a therapeutically effective amount of the said salt, or monohydrate of monohydrochloride, or a monophosphate salt of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide.

13 cl, 8 dwg, 17 tbl, 11 ex

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RU 2 605 551 C2

Authors

Manli Pol U.

Shi Venchun

Satton Pol Allen

Karpinski Peter Kh.

Vu Rain

Monne Stefani

Brotsio Jerg

Dates

2016-12-20Published

2013-01-15Filed