申请人:Japan Tobacco Inc.
公开号:EP0677519A1
公开(公告)日:1995-10-18
A chroman derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and a medicinal use thereof, wherein R¹ is cyano, nitro, trihalomethyl, trihalomethoxy or halogen; R² is lower alkoxyalkyl, aryloxyalkyl or dialkoxyalkyl; R³ is lower alkoxyalkyl or aryloxyalkyl; R⁴ is hydroxy, formyloxy or lower alkanoyloxy; X is N-H which may be substituted by lower alkyl, oxygen, sulfur or a single bond; Y is a residue of an aromatic or heterocyclic ring which may be substituted. The compound and pharmaceutically acceptable salt thereof have a prominent selective coronary vasodilator activity while having a minimized hypotensive effect. Therefore, they can selectively increase the coronary blood flow volume without the fear of causing sudden hypotension causative of tachycardia which adversely affects the heart, and hence are useful as a coronary vasodilator, in particular, as a preventive or remedy for cardiovascular disturbance such as angina pectoris or cardiac failure.
一种由通式(I)代表的色烷衍生物、其药学上可接受的盐及其药用方法,其中 R¹是氰基、硝基、三卤甲基、三卤甲氧基或卤素;R²是低级烷氧基烷基、芳氧基烷基或二烷氧基烷基;R³ 是低级烷氧基烷基或芳氧基烷基;R⁴ 是羟基、甲酰氧基或低级烷酰氧基;X 是可被低级烷基、氧、硫或单键取代的 N-H;Y 是可被取代的芳环或杂环的残基。该化合物及其药学上可接受的盐具有突出的选择性冠状动脉血管扩张活性,同时具有最小的降压作用。因此,它们可以选择性地增加冠状动脉血流量,而不必担心引起突发性低血压导致心动过速,从而对心脏产生不利影响,因此可用作冠状动脉血管扩张剂,特别是作为心绞痛或心力衰竭等心血管疾病的预防或治疗药物。