Position-Specific Asymmetric Deuterium Enriched Catecholamine Derivatives And Medicaments Comprising Said Compounds

Abstract

Herein described are deuterated catecholamine derivatives of the general Formula I wherein, R 1 is deuterium, R 2 , and R 3 are independently selected from hydrogen and deuterium and wherein at least one of R 2 and R 3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R 2 and R 3 is different from each other and that the difference between the deuterium enrichment of R 2 and R 3 is at least 5 percentage points, R 4 is hydrogen, deuterium, C 1 to C 6 -alkyl or C 5 to C 6 -cycloalkyl, deuterated C 1 to C 6 -alkyl or C 5 to C 6 -cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomers or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.

What is claimed: 
     
         1 . A pharmaceutical composition comprising
 L-2-amino-2,3,3-trideutero-3-(3,4-dihydroxyphenyl) propionic acid, or a physiologically acceptable salt thereof, having a deuterium enrichment above the natural abundance of deuterium; and   L-2-amino-2,3-dideutero-3-(3,4-dihydroxyphenyl) propionic acid, or a physiologically acceptable salt thereof, having a deuterium enrichment above the natural abundance of deuterium.