发明名称 Position-Specific Asymmetric Deuterium Enriched Catecholamine Derivatives And Medicaments Comprising Said Compounds
摘要 Herein described are deuterated catecholamine derivatives of the general Formula I;;wherein, R1 is deuterium, R2, and R3 are independently selected from hydrogen and deuterium and wherein at least one of R2 and R3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R2 and R3 is different from each other and that the difference between the deuterium enrichment of R2 and R3 is at least 5 percentage points, R4 is hydrogen, deuterium, C1 to C6-alkyl or C5 to C6-cycloalkyl, deuterated C1 to C6-alkyl or C5 to C6-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.
申请公布号 US2017119716(A1) 申请公布日期 2017.05.04
申请号 US201715402343 申请日期 2017.01.10
申请人 ratiopharm GmbH 发明人 Alken Rudolf-Giesbert;Schneider Frank
分类号 A61K31/198;A61K9/20;A61K9/28;A61K31/165;A61K31/277 主分类号 A61K31/198
代理机构 代理人
主权项 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.
地址 ULM DE