Paulus Wohlfart;Heinz-Werner Kleemann;Gerhard Zoller;David William Will;Hartmut Strobel
发明人:
Hartmut Strobel,Paulus Wohlfart,Heinz-Werner Kleemann,Gerhard Zoller,David William Will
申请号：
US12486117
公开号：
US08304438B2
申请日:
2009.06.17
申请国别(地区):
US
年份:
2012
代理人:
摘要：
The present invention relates to heteroarylacrylamides of the formula I,in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
