Novel salt 628

Abstract

6-M ethyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.

1 . A pharmaceutical composition comprising 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate Form A in admixture with a pharmaceutically acceptable diluent or carrier. 
     
     
         2 . A pharmaceutical composition comprising 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate Form A and dibasic calcium phosphate. 
     
     
         3 . The pharmaceutical composition according to  claim 2  further comprising microcrystalline cellulose. 
     
     
         4 . The pharmaceutical composition according to  claim 3  comprising said Form A, 40% by weight or less dibasic calcium phosphate and microcrystalline cellulose. 
     
     
         5 . A pharmaceutical composition comprising:
 20 a) 0.1 to 40 parts of 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N- {[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate Form A;   b) 2 to 10 parts dibasic calcium phosphate;   c) 60 to 90 parts microcrystalline cellulose;   d) 2 to 10 parts of a disintegrant;   e) 0.1 to 2 parts of a surfactant; and   f) 0.1 to 3 parts of a lubricant;
 wherein all parts are parts by weight of the total composition and the sum of the parts a) to f)=100. 
   
     
     
         6 . The pharmaceutical composition according to  claim 1  or  claim 5 , which is an instant release pharmaceutical composition for oral administration. 
     
     
         7 . The pharmaceutical composition according to  claim 5  further comprising a coating. 
     
     
         8 . The pharmaceutical composition according to  claim 1  wherein said Form A has an X-ray powder diffraction pattern measured using CuK α  radiation with at least one specific peak at 2θ=about 5.1, 7.3, 8.9, 17.0 or 17.8°. 
     
     
         9 . The pharmaceutical composition according to  claim 1  wherein said Form A has an X-ray powder diffraction pattern measured using CuK α  radiation with specific peaks at 2θ=about 5.1, 7.3, 8.9, 17.0 and 17.8°. 
     
     
         10 . The pharmaceutical composition according to  claim 1  wherein said Form A has an X-ray powder diffraction pattern measured using CuK α  radiation substantially the same as that shown in  FIG. 1 .