Novel Crystalline Forms Of An Antiviral Benzimidazole Compound

Abstract

The invention relates to crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1H benzimidazole, pharmaceutical compositions comprising the same, processes for preparing the same, and their use in medical therapy.

1 - 15 . (canceled) 
   
   
       16 . A pharmaceutical composition comprising a crystalline form of Form I 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 1 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Ka X-radiation, and at least one pharmaceutically acceptable carrier therefor. 
   
   
       17 . The pharmaceutical composition according to  claim 16 , wherein the pharmaceutical composition is in the form of a capsule, cachet, sachet of granules or tablets. 
   
   
       18 . A method for the treatment of a herpes viral infection in a human which comprises administering to the human host, and effective antiviral amount of a crystalline form of Form I 5,6-dichloro-2-(isopropylamino)-1-R-L-ribofuranosyl-1H-benzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 1 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Ka X-radiation. 
   
   
       19 . The method according to  claim 18 , wherein the crystalline form of Form I is administered orally, topically or parenterally. 
   
   
       20 . The method according to  claim 18 , wherein the herpes viral infection is cytomegalovirus (CMV). 
   
   
       21 . The method according to  claim 18 , wherein the effective antiviral amount of a crystalline form of Form I 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1H-benzimidazole ranges from about 0.01 to about 250 mg per kilogram of body weight of recipient per day. 
   
   
       22 . A crystalline form of Form I 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 1 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Kα X-radiation, and at least one pharmaceutically acceptable carrier therefor. 
   
   
       23 . A pharmaceutical composition comprising a crystalline form of Form IV 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 4 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Ka X-radiation, and at least one pharmaceutically acceptable carrier therefor. 
   
   
       24 . The pharmaceutical composition according to  claim 23 , wherein the pharmaceutical composition is in the form of a capsule, cachet, sachet of granules or tablets. 
   
   
       25 . A method for the treatment of a herpes viral infection in a human which comprises administering to the human host, and effective antiviral amount of a crystalline form of Form IV 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 4 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Ka X-radiation. 
   
   
       26 . The method according to  claim 25 , wherein the crystalline form of Form I is administered orally, topically or parenterally. 
   
   
       27 . The method according to  claim 25 , wherein the herpes viral infection is cytomegalovirus (CMV). 
   
   
       28 . The method according to  claim 25 , wherein the effective antiviral amount of a crystalline form of Form I 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1H-benzimidazole ranges from about 0.01 to about 250 mg per kilogram of body weight of recipient per day. 
   
   
       29 . A crystalline form of Form IV 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole having substantially the same X-ray powder diffraction pattern as  FIG. 4 , wherein said X-ray diffraction pattern is obtained with a diffractometer equipped with a diffracted beam curved graphite monochromator using copper Ka X-radiation, and at least one pharmaceutically acceptable carrier therefor.