申请人:Farmos-Yhtyma Oy
公开号:EP0058047A1
公开(公告)日:1982-08-18
Compounds of the formula:
wherein each of R1, R2 and R3, wnich can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R4 is hydrogen or alkyl of 1 to 7 carbon atoms; R5 is hydrogen or a straight or branched alkyl group of 1 to 5 carbon atoms or a phenyl group; and R6 is hydrogen or an alkyl group of 1 to 7 carbon atoms or a substituted or unsubstituted benzyl, X is -CH2-, -CHOH-or -CH=CH- and n is 0-4; provided that R5 and R6 are simultaneously hydrogen only when n is 4 and X is -CH=CH-; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antithrombotic agents. Furthermore. some of the compounds have proved to possess anti- hypertensive or β-btocking activity. Antimicrobial and antifungal properties have also been found. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds of their salts.
式中的化合物:
其中R1、R2和R3可以相同或不同,各自为氢、氯、溴、氟、甲基、乙基、甲氧基、氨基、羟基或硝基;R4为氢或1至7个碳原子的烷基;R5 是氢或 1 至 5 个碳原子的直链或支链烷基或苯基;R6 是氢或 1 至 7 个碳原子的烷基或取代或未取代的苄基,X 是-CH2-、-CHOH-或-CH=CH-,n 是 0-4;但只有当 n 为 4 且 X 为-CH=CH-时,R5 和 R6 才同时为氢;它们的无毒药学上可接受的酸加成盐及其混合物具有宝贵的药理活性,可用于哺乳动物的治疗,特别是作为抗血栓药物。此外,其中一些化合物已被证明具有抗高血压或β-阻滞活性。此外,还发现了抗菌和抗真菌特性。本文介绍了这些化合物的制备过程,以及包含至少一种化合物及其盐类的新型药物组合物。