Hubert KOESTER,Lisa VON KLEIST,Simon MICHAELIS,Kathrin BARTHO,Marén SCHLIEF,Mathias DREGER,Anna K. SCHREY,Michael SEFKOW,Friedrich KROLL,Daniel OHLENDORF,Yan LUO
申请号:
US16063297
公开号:
US20180370906A1
申请日:
2016.12.19
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R1 is —OH, R2 is —NO2 and R3 is H, R4 and R5 are H, one of R6 and R7 is selected from H, —CONH2, and —CONR92, and the other one is selected from —CONR92 and —CONR11R9, wherein R9 and R11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off-target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinsons disease.