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deuterium-enriched catecholamine derivatives in asymmetric specific position and medicaments comprising said compounds
专利权人:
IMPHAR AKTIENGESELLSCHAFT
发明人:
FRANK SCHNEIDER,RUDOLF-GIESBERT ALKEN
申请号:
BR112015016889
公开号:
BR112015016889A2
申请日:
2014.02.05
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
Patent Specification: "Asymmetrically specific deuterium enriched catecholamine derivatives and medicaments comprising said compounds". The present invention relates to 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 an enrichment of. deuterium in the range 0.02 mol% to 100 mol% deuterium, and wherein the deuterium enrichment of r2 and r3 is different from each other and wherein 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, c1 to c6-alkyl or c5 to c6-cycloalkyl deuterated, or a group that is readily 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 be easily prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds have anti-parkinson effect at lower doses and have lower side effects.resumo patente de invenção: "derivados de catecolamina enriquecidos com deutério em posição específica assimétrica e medicamentos compreendendo os referidos compostos". a presente invenção refere-se a derivados de catecolamina deuterados da fórmula geral (i), em que r1 é deutério, r2 e r3 são selecionados independentemente a partir de hidrogênio e deutério e em que pelo menos um de r2 e r3 tem um enriquecimento de deutério na gama de 0,02% em mol a 100% em mol de deutério, e em que o enriquecimento de deutério de r2 e r3 é diferente um do outro e em que a diferença entre o enriquecimento de deutério de r2 e r3 é de pelo menos 5 pontos percentuais, r4 é hidrogênio, deutério, c1 a c6-alquila ou c5 a c6-cicloalquila, c1 a c6-alquila ou c5 a c6-cicloalquila deuterado, ou um grupo que é facilmente hidroliticamente ou enzimaticament
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