申请人:Farmos Group Ltd.
公开号:EP0072615A1
公开(公告)日:1983-02-23
The invention provides novel compounds of the formula:
or
wherein R, is H, an alkyl of 1 to 4 carbon atoms or -CH2OH; R2 is H or CH3; R3 is -CH3, -CH2CH3, -CH2CH2CH3,
R4 is H or OH; or R3 and R4 together represent =CH2, =CH-CH3, =CH-CH2-CH3,
or
X is
or
Rs, R6 and R7, which can be the same or different are H, -CH3, -CN2CH3, halogen, OH or -OCH3 or R5 is hydrogen and R6 and R7 together form an -O-CH2-O-bridge between two adjacent carbon atoms in the phenyl group; -CHR8- is -CH2-, -CH(CH3)-, -CH(-CH2CH3)-, -CH(-CH2CH2CH3)-,
or
or
or
or -CH2CH2CH2CH3; n is 0 to 4; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising at least one of the compounds or their salts. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antihypertensive agents. Furthermore. some of the compounds have proved to possess anthrombotic and diuretic activity. Antimycotic and antifungal properties have also been found.
本发明提供了式如下的新型化合物: 或 其中R,是H、1至4个碳原子的烷基或-CH2OH;R2是H或CH3;R3是-CH3、-CH2CH3、-CH2CH2CH3、
R4是H或OH;或R3和R4一起代表=CH2、=CH-CH3、=CH-CH2-CH3,或X是或Rs、R6和R7(可以相同或不同)是H、-CH3、-CN2CH3、卤素、OH或-OCH3,或R5是氢,R6和R7一起在苯基中两个相邻碳原子之间形成-O-CH2-O桥;-CHR8-是-CH2-、-CH(CH3)-、-CH(-CH2CH3)-、-CH(-CH2CH2CH3)-、
或
或
或
或 -CH2CH2CH2CH3;n 为 0 至 4;以及它们的无毒药学上可接受的酸加成盐及其混合物。本文描述了这些化合物的制备过程,以及包含至少一种化合物或其盐类的新型药物组合物。这些化合物及其无毒盐具有宝贵的药理活性,可用于哺乳动物的治疗,特别是作为抗高血压药物。此外,其中一些化合物还被证明具有蒽醌和利尿活性。还发现了抗霉菌和抗真菌特性。