Indole derivatives

Abstract

The present invention provides eletriptan hydrobromide monohydrate of the formula (I): together with processes for preparing, uses of, and compositions containing, said monohydrate.

1 . Eletriptan hydrobromide monohydrate of the formula (I):  
       
         
           
           
               
               
           
         
       
     
     
         2 . A pharmaceutical composition including eletriptan hydrobromide monohydrate as claimed in  claim 1  together with a pharmaceutically acceptable excipient, diluent or carrier.  
     
     
         3 . Eletriptan hydrobromide monohydrate as claimed in  claim 1  for use as a medicament.  
     
     
         4 . The use of eletriptan hydrobromide monohydrate as claimed in  claim 1  for the manufacture of a medicament for the treatment of a disease or condition for which a selective agonist of a 5-HT 1B/1D  receptor is indicated.  
     
     
         5 . Use as claimed in  claim 4  for the treatment of a disease or condition for which a selective agonist of a 5-HT 1B/1D  receptor is indicated.  
     
     
         6 . The use of eletriptan hydrobromide monohydrate as claimed in  claim 1  for the manufacture of a medicament for the treatment of a disease or condition selected from migraine, recurrent migraine, hypertension, depression, emesis, anxiety, an eating disorder, obesity, drug abuse, cluster headache, pain, chronic paroxysmal hemicrania and headache associated with a vascular disorder.  
     
     
         7 . Use as claimed in  claim 6  for the treatment of migraine or recurrent migraine.  
     
     
         8 . A method of treatment of a mammal to treat a disease or condition for which a selective agonist of a 5-HT 1  receptor is indicated which includes treating said mammal with an effective amount of eletriptan hydrobromide monohydrate as claimed in  claim 1 .  
     
     
         9 . A method as claimed in  claim 8  to treat a disease or condition for which a selective agonist of a 5-HT 1B/1D  receptor is indicated.  
     
     
         10 . A method of treatment of a mammal to treat a disease or condition selected from migraine, recurrent migraine, hypertension, depression, emesis, anxiety, an eating disorder, obesity, drug abuse, cluster headache, pain, chronic paroxysmal hemicrania and headache associated with a vascular disorder which includes treating said mammal with an effective amount of eletriptan hydrobromide monohydrate as claimed in  claim 1 .  
     
     
         11 . A method as claimed in  claim 10  to treat migraine or recurrent migraine.  
     
     
         12 . A process for the preparation of eletriptan hydrobromide monohydrate as claimed in  claim 1  which comprises treatment of a solution of eletriptan in water, or in an organic solvent containing a sufficient amount of water to facilitate formation of the required monohydrate, with hydrogen bromide or a source thereof.  
     
     
         13 . A process as claimed in  claim 12  wherein the organic solvent is tetrahydrofuran or acetone.  
     
     
         14 . A process as claimed in  claim 12  or  13  wherein hydrogen bromide is used in the form of an aqueous solution.  
     
     
         15 . A process for the preparation of eletriptan hydrobromide monohydrate as claimed in  claim 1  which comprises crystallisation of any other form of eletriptan hydrobromide, or a mixture thereof, from water, or from an organic solvent containing a sufficient amount of water to facilitate formation of the required monohydrate.  
     
     
         16 . A process as claimed in  claim 15  wherein the organic solvent is acetone.  
     
     
         17 . A process for the preparation of anhydrous eletriptan hydrobromide which comprises dehydration of any hydrated form of eletriptan hydrobromide, preferably eletriptan hydrobromide monohydrate as claimed in  claim 1 , or a mixture thereof.