XINAFOATE SALT OF N4-[(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ON)-6-YL]-5-FLUORO-N2-[3-(METHYLAMINOCARBONYL METHYLENEOXY)PHENYL]-2,4-PYRIMIDINE DIAMINE Russian patent published in 2012 - IPC C07D413/12 A61K31/538 A61P11/06 

Abstract RU 2458925 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-on)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonyl methyleneoxy)phenyl]-2,4-pyrimidine diamine, having the structural formula given below. The invention also relates to a method of producing a salt, use of the latter, a pharmaceutical composition and a treatment method. The method of producing a xinafoate salt involves dissolving N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-on)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonyl methyleneoxy)phenyl]-2,4-pyrimidine diamine and 1-1.1 molar equivalents of 1-hydroxy-2-naphthoic acid in a minimum amount of a suitable organic solvent such as acetone, acetonitrile or methyl ethyl ketone, each optionally containing a small amount of water, and subsequent slow cooling of the solution with optional stirring until precipitation of the salt from the solution.

EFFECT: obtained salt has Syk-kinase inhibiting properties and can be used in treating an inflammatory condition such as asthma (I).

12 cl, 6 tbl, 1 ex

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RU 2 458 925 C2

Authors

Tehjlor Stefan Kolin Dzhon

Dates

2012-08-20Published

2008-08-27Filed