申请人:Hoffmann-La Roche Inc.
公开号:US04971982A1
公开(公告)日:1990-11-20
Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R.sup.2 is hydrogen, lower alkyl or phenyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 and R.sup.5 each is hydrogen or R.sup.4 is hydroxy and R.sup.5 is hydrogen or R.sup.4 and R.sup.5 together are a carbon-carbon bond and R.sup.6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position, and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.
公式的化合物##STR1##,其中R.sup.1是氢、卤素、三氟甲基、硝基、腈、低级烷基、低级烷氧基羰基、低级烷基硫醚、低级烷基亚磺酰基、低级烷氧基、芳酰基、氨基甲酰基、单(低级烷基)氨基甲酰基或二(低级烷基)氨基甲酰基,R.sup.2是氢、低级烷基或苯基,R.sup.3是氢或低级烷基,R.sup.4和R.sup.5各自是氢或R.sup.4是羟基且R.sup.5是氢或R.sup.4和R.sup.5一起是碳-碳键,R.sup.6是一个在2-位带有羟基的芳香族或N-杂芳族基团,或者在N-杂芳族基团的情况下,还在2-位带有N-氧化物基团,以及这些公式I的化合物的药用可接受的酸加成盐,它们是碱性的,具有显著地激活钾通道的活性,可以用作药物,特别是在控制或预防高血压、充血性心力衰竭、心绞痛、外周和脑血管疾病以及平滑肌障碍中。