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    • 1. 发明公开
    • Quinolones having antihypertensive activity.
    • Chinolone mit blutdrucksenkender Wirkung。
    • EP0206616A2
    • 1986-12-30
    • EP86304390
    • 1986-06-09
    • BOOTS CO PLC
    • DAVIES ROY VICTORFRASER JAMESNICHOL KENNETH JOHN
    • C07D209/38A61K31/47A61P9/10A61P9/12C07C67/00C07C301/00C07C303/38C07C303/40C07C311/35C07D215/22C07D215/36C07D215/56
    • C07D215/36
    • Quinolines with antihypertensive activity have the general formula I, … … wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R3 is hydrogen or lower alkyl; R1 and R2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease. … With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel. … Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.
    • 具有抗高血压活性的喹诺酮具有通式I,... ...其中X是任选取代的苯环的残基; R为低级烷基; R3是氢或低级烷基; R 1和R 2可以相同或不同,为氢,低级烷基,或与它们相连的氮原子一起形成任选地含有另外的杂原子的5至7元饱和杂环,所述杂环选自氮, 氧和硫,并任选被1个或多个低级烷基取代; 并且喹诺酮核的位置2和3之间的虚线表示任选的键。 该化合物可用作抗高血压药。 它们也被用于治疗心力衰竭和缺血性心脏病。 ...除了三种化合物1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺,1,N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和 6,7-二甲氧基甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺,式I的喹诺酮是新的。 描述了含有式I化合物的药物组合物。 还描述了制备新型喹诺酮类的方法。