申请人:Takeda Chemical Industries, Ltd.
公开号:EP0135316A1
公开(公告)日:1985-03-27
Novel compounds of the formula:
wherein R is an aromatic or heterocyclic group, which may optionally be substituted, R2 is a methyl group, a hydroxymethyl group, a nitroxymethyl group, a formyl group, a nitrogen-containing five-membered ring-menthyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl-or aryl-sulfonyloxymethyl group, an alkyl- or aryl- sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryloxymethyl group, a cyano group, a carbamoyl group which may optionally be substituted, a carbamoyloxymethyl group which may optionally be substituted, a thiocarbamoyloxymethyl group which may optionally be substituted, a carboxyl or an alkoxycarbonyl group, n is an integer of 1 to 20, and
provided that n is an integer of 9 to 20 when (0←)
is
and, at the same time, R2 is a carboxyl group or an alkoxycarbonyl group, or a pharmacologically acceptable salt thereof, have a selective inhibitory action on biosynthesis of thromboxane A, (TXA2) and an effect of enhancing the production of prostaglandin I2(PGI2), and can be used for mammals to prevent and treat arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vaso- spasms in cardiac, cerebral and peripheral circulatory systems (e.g. cardiac infarction, stroke, occlusion of blood vessels in kidney, lung and other organs, peptic ulcer.
式中的新型化合物:
其中 R 是芳香族或杂环基团,可任选被取代,R2 是甲基、羟甲基、硝基、甲酰基、含氮五元环薄荷基、缩醛甲基、三烷基硅氧基甲基、烷基或芳基磺酰氧基甲基、烷基或芳基磺酰氨基羰基氧基甲基、酰氧基甲基、烷氧基羰氧基甲基、卤代甲基、烷氧基甲基、芳氧基甲基、氰基、可任选被取代的氨基甲酰基、可任选被取代的氨基甲酰氧基甲基、可任选被取代的硫代氨基甲酰氧基甲基、羧基或烷氧基羰基,n 为 1 至 20 的整数,且
当 (0←) 时,n 为 9 至 20 的整数
为
同时,R2 是羧基或烷氧基羰基,或其药理学上可接受的盐,对血栓素 A(TXA2)的生物合成具有选择性抑制作用,并具有增强前列腺素 I2(PGI2)生成的作用、可用于哺乳动物预防和治疗由血小板聚集引起的动脉血栓或由心、脑和外周循环系统血管痉挛引起的缺血性疾病(如心肌梗塞、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死、心肌梗死)。如心肌梗塞、中风、肾、肺和其他器官血管闭塞、消化性溃疡等。