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, Ris deuterium, R, and Rare independently selected from hydrogen and deuterium and wherein at least one of Rand Rhas a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of Rand Ris different from each other and that the difference between the deuterium enrichment of Rand Ris at least 5 percentage points, Ris hydrogen, deuterium, Cto C-alkyl or Cto C-cycloalkyl, deuterated Cto C-alkyl or Cto C-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.