申请人:The Boots Company PLC
公开号:EP0206616A2
公开(公告)日:1986-12-30
Quinolines with antihypertensive activity have the general formula 1,
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-dimeth- oxyl-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啉类化合物具有通式 1、
其中,X 是任选取代的苯环的残基;R 是低级烷基;R3 是氢或低级烷基;R1 和 R2(可以相同或不同)是氢、低级烷基,或与它们连接的氮原子一起形成 5 至 7 个成员的饱和杂环,其中任选含有一个选自氮、氧和硫的杂原子,并任选被 1 个或多个低级烷基取代;喹诺酮核的位置 2 和 3 之间的虚线代表任选键。这些化合物可用作降压药。它们还可用于治疗心力衰竭和缺血性心脏病。
除了 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 6,7-二甲基-氧代-4-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺这三种化合物外,式 I 中的喹诺酮类化合物均为新型化合物。
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药物的工艺。