Heterocyclic substituted indolinones
    3.
    发明授权
    Heterocyclic substituted indolinones 失效
    杂环取代的二氢吲哚酮

    公开(公告)号:US4870077A

    公开(公告)日:1989-09-26

    申请号:US94871

    申请日:1987-09-10

    摘要: Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.6 independently being hydrogen atoms or alkyl radicals wherein the alkyl groups independently contain 1 to 6 carbon atoms; as well as the tautomers thereof and the physiologically acceptable salt thereof and the physiologically acceptable salts thereof with inorganic and organic acids, are disclosed, such as, for instance, the compound 5-(2,3,4,5-tetrahydro-3-oxopyridazin-6-yl)-3-ethoxycarbonyl-3-methyl-1H-indol n-2-one. The compounds of the invention are useful in the treatment of heart and circulatory diseases, for example, by producing a positive inotropic action in a patient to whom the compounds are administered.

    摘要翻译: 式(I)的杂环取代的二氢吲哚酮:其中R 1是氢原子或烷基或羟烷基,R 2是羧基或烷氧羰基,羟基烷基或烷基羰基氧基烷基或R 1和R 2与碳 它们连接的原子形成具有4,5或6个环原子的内酯,AB是-CH 2 -CH(R 3) - , - CH = CR 3 - , - CH 2 -NH-,-NH-CH 2 - , - CH 2 -O-,-O-CH 2 - , - CH 2 -S-或-S-CH 2 - 基,R 3是氢原子或烷基或羟烷基,或A是价键,B是亚甲基。 或亚氨基基团R4,R5和R6独立地为氢原子或烷基,其中烷基独立地含有1至6个碳原子; 以及其与无机和有机酸的互变异构体及其生理上可接受的盐及其生理上可接受的盐,例如化合物5-(2,3,4,5-四氢-3- 氧基哒嗪-6-基)-3-乙氧基羰基-3-甲基-1H-吲哚-2-酮。 本发明的化合物可用于治疗心脏和循环系统疾病,例如通过在施用化合物的患者中产生正性肌力作用。