Hiv Inhibiting 2-(4-Cyanophenyl)-6-Hydroxylaminopyrimidines

Abstract

HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R 1 is halo; R 2 and R 3 each independently are C 1-6 alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

1 . A compound of formula 
       
         
           
           
               
               
           
         
         a pharmaceutically acceptable addition salt; or a stereochemically isomeric form thereof, wherein 
         R 1  is halo; 
         R 2  and R 3  each independently are C 1-6 alkyl. 
       
     
     
         2 . A compound as claimed in  claim 1  wherein R 1  is chloro or bromo. 
     
     
         3 . A compound as claimed in  claim 1  wherein R 1  is bromo. 
     
     
         4 . A compound as claimed in  claim 1  wherein R 2  and R 3  are methyl. 
     
     
         5 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredient a therapeutically effective amount of a compound as claimed in  claim 1 . 
     
     
         6 . A compound as claimed in  claim 1  for use as a medicine. 
     
     
         7 . A process for preparing a composition according to  claim 5 , the process comprising intimately mixing the active ingredient and the carrier. 
     
     
         8 . A process for preparing a compound as claimed in  claim 1 , characterized by reacting an intermediate (II) with a protected hydroxylamine, thus obtaining an intermediate (II); and subsequently deprotecting the intermediate (II) thus obtaining the end products (I): 
       
         
           
           
               
               
           
         
       
       and if desired preparing a pharmaceutically acceptable acid-addition salt form of the compounds of formula (I) by treating them with a pharmaceutically acceptable acid. 
     
     
         9 . A chemical compound of formula 
       
         
           
           
               
               
           
         
       
       or an acid-addition salt thereof; or a stereochemically isomeric form thereof, wherein R 1 , R 2  and R 3  are as defined in  claim 1  and P is a hydroxy-protecting group, in particular P is tetrahydro-2H-pyran-2-yl.