Sérgio Luiz SACURAI;Carlos Eduardo da Costa Touzarim;Artur Franz Keppler;Márcio Henrique Zaim;Gilberto De Nucci
发明人:
Sérgio Luiz SACURAI,Márcio Henrique Zaim,Carlos Eduardo da Costa Touzarim,Artur Franz Keppler,Gilberto De Nucci
申请号:
US13196363
公开号:
US20120040988A1
申请日:
2011.08.02
申请国别(地区):
US
年份:
2012
代理人:
摘要:
The present invention describes a series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, the derivative (R)-3-(1,3-benzodioxol-5-yl)-1-(1H-indol-3-yl)-7-methyl-6,7-dihydro[1,3]oxazolo[3,4-a]pyrazine-5,8-dione, its enantiomer (S)-3-(1,3-benzodioxol-5-yl)-1-(1H-indol-3-yl)-7-methyl-6,7-dihydro[1,3]oxazolo[3,4-a]pyrazine-5,8-dione.The present invention describes, additionally, processes for the preparation of said compounds, pharmaceutical compositions containing them, thereof, as well as uses as inhibitors of the enzyme phosphodiesterase type 5 (PDE-5) in the treatment of the erectile dysfunction and PDE-5 inhibitor treatable disorders.