New derivatives of amino acids has - acetylenic, their preparation and their use as inhibitors of the aromatic amino acid decarboxylase

摘要

Pharmaceutically useful compounds have the formula IMAGE wherein R1 is hydrogen, (C1-4alkyl) carbonyl, (C1-4alkoxy) carbonyl or CO-CHNH2-R27 wherein R27 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R is hydroxy, alkoxy of 1 to 8 carbon atoms, -NR7R8 wherein R7 and R8 are the same or different and are each hydrogen or C1-4alkyl, or NH-CHR9-COOH wherein R9 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and R2, R3, R4, R5 and R6 are certain combinations of hydrogen, methyl, ethyl, tert-butyl, chlorine, fluorine and OR10 wherein R10 is hydrogen, alkyl of 1 to 8 carbon atoms, (C1-6alkyl) carbonyl, benzoyl or phenyl (C1-6alkyl) carbonyl or R3 and R4 together are methylene dioxy.