Teva Pharmaceuticals International Gmbh

Ratiopharm Gmbh

Birds Pharma Gmbh Berolina Innovative

Rudolf-Giesbert Alken

Frank Schneider

The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.

Deuterated catecholamine derivatives and medicaments compromising said compounds

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.

Position-specific asymmetric deuterium enriched catecholamine derivatives and medicaments comprising said compounds

The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.

Deuterated catecholamine derivatives and medicaments comprising said compounds

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, enantiomeres 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.

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Svedala, Sweden

Rudolf-Giesbert Alken