N-oxides of n-phenyl-2-pyrimidine-amine derivatives

Abstract

The invention relates to N-phenyl-2-pyrimidine-amine derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.

1 . A pharmaceutical composition comprising: 4-[4-(methyl-1-piperazinyl)-methyl]-N-[4-methyl-3-[[4-(1-oxido-3-pyridinyl)-2-pyrimidinyl]-amino]-phenyl]-benzamide, or a pharmaceutically acceptable salt thereof, made by a process comprising the step of: combining microcrystalline cellulose, cross-linked polyvinylpyrrolidone, silicon dioxide and magnesium stearate and 4-[4-(methyl-1-piperazinyl)-methyl]-N-[4-methyl-3-[[4-(1-oxido-3-pyridinyl)-2-pyrimidinyl]-amino]-phenyl]-benzamide, or a pharmaceutically acceptable salt thereof. 
     
     
         2 . The pharmaceutical composition according to  claim 1  as a solid mixture compressed into a tablet or filled into a capsule. 
     
     
         3 . A pharmaceutical composition comprising: 20-30% by weight of 4-[4-(methyl-1-piperazinyl)-methyl]-N-[4-methyl-3-[[4-(1-oxido-3-pyridinyl)-2-pyrimidinyl]-amino]-phenyl]-benzamide, or a pharmaceutically acceptable salt thereof; 50-55% by weight of a sugar; 15-20% by weight of microcrystalline cellulose; 3-7% by weight of cross-linked polyvinylpyrrolidone; 0.1-0.5% by weight of silicon dioxide; and 0.5-2% by weight of magnesium stearate, based on the weight of the pharmaceutical composition.