Crystalline bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino]pyrimidin -5-yl] (3R,5S)-3, 5-dihydroxyhept -6-enoic acid]calcium salt

Abstract

The present invention relates to a crystalline form of the compound bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino] pyrimidin-5-yl] (3R, 5S)-3, 5-dihydroxyhept-6-enoic acid]calcium salt, as well as processes for its manufacture and pharmaceutical compositions comprising the crystalline form, which is useful as an agent for treating hyperlipidemia, hypercholesterolemia and atherosclerosis.

1 . A crystalline form of the compound bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt of the formula I  
       
         
           
           
               
               
           
         
       
       or a hydrate thereof having an X-ray powder diffraction pattern with specific peaks at 2-theta (2θ)=4.92, 11.50, 6.93, 9.35, 23.12 and 18.76°.  
     
     
         2 . A crystalline form as claimed in  claim 1  which is a crystalline hydrated form.  
     
     
         3 . A pharmaceutical composition comprising a crystalline form as claimed in  claim 1  or  2 , together with a pharmaceutically acceptable carrier.  
     
     
         4 . A process for the manufacture of a crystalline form or hydrated form as claimed in  claim 1  which comprises forming crystals from a mixture of the compound of formula I, water and one or more organic solvents.  
     
     
         5 . A process as claimed in  claim 4  wherein the organic solvent is selected from acetonitrile, acetone or a mixture of methanol and methyl tert-butyl ester.  
     
     
         6 . A process for the manufacture of a pharmaceutical composition as claimed in  claim 3  which comprises admixing a crystalline form as claimed in  claim 1  together with a pharmaceutically acceptable carrier.  
     
     
         7 . The use of a crystalline form as claimed in  claim 1  in the manufacture of a medicament.  
     
     
         8 . A method of treating a disease condition wherein inhibition of HMG CoA reductase is beneficial which comprises administering to a warm-blooded mammal an effective amount of a crystalline form as claimed in  claim 1.