Benzopyran derivatives having anti-hypertensive and vasodilatory activity, their preparation and their therapeutic use
申请人:Sankyo Company Limited
公开号:EP0482931A1
公开(公告)日:1992-04-29
Compounds of formula (I):
in which:
R¹ is perfluoroalkyl; R² is a group of formula (II):
in which R⁴ is hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, cyano, hydroxy or nitro;
or a group of formula (III):
in which R⁵ is hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, cyano or nitro;
α-β is a carbon-carbon single bond or a carbon-carbon double bond; and
where α-β is a carbon-carbon single bond, R³ is hydroxy or nitrooxy or, where α-β is a carbon-carbon double bond, R³ is hydrogen;
and pharmaceutically acceptable salts thereof, have valuable anti-hypertensive activity and can thus be used for the treatment and prophylaxis of cardiovascular diseases. The invention also provides methods and compositions using these compounds as well as processes or their preparation.
式(I)化合物:
其中
R¹ 是全氟烷基;R² 是式 (II) 所示基团:
其中 R⁴ 是氢、烷基、烷氧基、卤素、三氟甲基、氰基、羟基或硝基;
或式 (III) 的基团:
其中 R⁵ 是氢、烷基、烷氧基、卤素、三氟甲基、氰基或硝基;
α-β 是碳碳单键或碳碳双键;以及
其中 α-β 是碳碳单键,R³ 是羟基或硝基氧基,或者,其中 α-β 是碳碳双键,R³ 是氢;
及其药学上可接受的盐类具有重要的抗高血压活性,因此可用于治疗和预防心血管疾病。本发明还提供了使用这些化合物的方法和组合物,以及制备这些化合物的工艺。