New Aminopropylphosphinic acids

Abstract

Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S,3R)-(3-amino-2-hydroxybutyl)phosphinic acid, having affinity to one or more GABA B receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as processes for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

1 . A compound according to formula I 
       
         
           
           
               
               
           
         
       
       wherein
 R 1  represents hydrogen, hydroxyl, lower alkyl, lower alkoxy or halogen; 
 R 2  represents hydroxy, mercapto, halogen, or an oxo group; 
 R 3  represents hydrogen or lower alkyl (optionally substituted with hydrogen, mercapto, lower alkoxy, lower thioalkoxy or aryl); 
 R 4  represents hydrogen, lower alkyl (optionally substituted with aryl) or aryl; 
 and pharmaceutically acceptable salts, solvates and the stereoisomers thereof, 
 with the exceptions of: 
 i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid, and 
 ii) (2R/S,3R)-(3-amino-2-hydroxybutyl)phosphinic acid. 
 
     
     
         2 - 26 . (canceled)