Prucalopride-n-oxide

Abstract

The present invention is concerned with a novel benzamide derivative and the pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions comprising said novel compound, processes for preparing said compounds and compositions, and the use thereof as a medicine in the treatment of gastrointestinal motility disorders.

1 . A compound of formula (I)  
       
         
           
           
               
               
           
         
       
       and stereochemically isomeric forms and pharmaceutically acceptable acid addition salts thereof.  
     
     
         2 . A compound as claimed in  claim 1  having the cis configuration.  
     
     
         3 . A compound as claimed in  claim 1  having the trans configuration.  
     
     
         4 . A compound as claimed in any of  claims 1  to  3  wherein the compound of formula (I) is the (1:1) hydrate.  
     
     
         5 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically active amount of a compound as claimed in any of  claims 1  to  4 .  
     
     
         6 . A process for preparing a pharmaceutical composition as claimed in  claim 5  wherein a therapeutically active amount of a compound as claimed in any of  claims 1  to  4  is intimately mixed with a pharmaceutically acceptable carrier.  
     
     
         7 . A compound as claimed in any of  claims 1  to  4  for use as a medicine.  
     
     
         8 . A process for preparing a compound of formula (I) by oxidizing a compound of formula (II) with a suitable oxidans in a reaction-inert solvent.