STROBEL, HARTMUT,史哈特,WOHLFART, PAULUS,沃佩斯,ZOLLER, GERHARD,洛葛德,WILL, DAVID WILLIAM,魏威廉
申请号：
TW095122876
公开号：
TWI378095B
申请日:
2006.06.26
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R 1 , R 2 and R 3 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.本發明係有關式I之N－烷基醯胺類；I；其中A、Het、X、R1、R2與R3如申請專利範圍中之定義，其可調控內皮氧化氮(NO)合成酶之轉錄作用，且為有價值之醫藥活性化合物。明確言之，式I化合物向上調節內皮NO合成酶酵素之表現，且可用於需要提高該酵素表現或提高NO濃度或使下降之NO濃度正常化之病症。本發明進一步係有關製備式I化合物之方法，含其之醫藥組合物、及以式I化合物於製造刺激內皮NO合成酶表現之醫藥或於治療多種不同疾病上之用途，包括例如：心血管病變，如：動脈粥樣硬化、血栓形成、冠狀動脈疾病、高血壓與心功能不全。
