composition based on derivatives of alpha - alogenometilamminoacidi with inhibitory activity of decarboxylase amino acids and process for its production

摘要

Compounds of the formula IMAGE wherein Y is -CH2F, -CHF2, -CF3, -CH2Cl or -CHCl2; R1 is hydroxy, alkoxy of 1 to 8 carbon atoms, -NY1Y2 wherein Y1 and Y2 are the same or different and are each hydrogen or alkyl of 1 to 4 carbon atoms, or -NH-CHR8-COOH wherein R8 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxyphenyl; R2 is hydrogen, (C1-4alkyl)carbonyl, (C1- 4alkoxy)carbonyl or -CO-CHNH2-R9 wherein R9 is hydrogen, alkyl of 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R3 is hydrogen or methyl; and R4, R5, R6 and R7 are certain combinations of hydrogen, methyl, halogen, trifluoromethyl and OR10 wherein R10 is hydrogen, alkyl of 1 to 8 carbon atoms, (C1-6alkyl)carbonyl, benzoyl or phenyl(C1-6alkylene) carbonyl may be prepared by formation of the indole ring. The compounds irreversibly inhibit aromatic amino acid decarboxylase. The compounds may be converted to pharmaceutically active compounds of the formula II. IMAGE