New Aminopropylphosphinic acids
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)