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    • 3. 发明授权
    • Piperazinylalkyl-3(2H)-pyridazinones and the use thereof as agents
lowering blood pressure
    • 哌嗪基烷基-3(2H) - 哒嗪酮及其作为降低血压的试剂的用途
    • US5034391A
    • 1991-07-23
    • US443166
    • 1989-11-30
    • Heinz BlaschkeHeimo StroissnigHarald FellierRita Enzenhofer
    • Heinz BlaschkeHeimo StroissnigHarald FellierRita Enzenhofer
    • A61K31/50A61K31/501A61P9/00A61P9/12C07D237/14C07D237/22C07D401/12C07D403/12
    • C07D401/12C07D237/22C07D403/12
    • The invention relates to new piperazinylalkyl-3(2H)-pyridazinones of the formula ##STR1## in which the radicals R.sub.1 represents hydrogen, phenyl, benzyl, or (C.sub.1 -C.sub.6)-alkyl which is unsubstituted or substituted one or more times by hydroxyl, piperidine, morpholine or by a group NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 can be identical or different and which represent hydrogen, methyl or ethyl,R.sub.2 and R.sub.3 represent hydrogen, halogen, (C.sub.1 -C.sub.6)-alkoxy or (C.sub.1 -C.sub.6)-alkyl, where at least one of the radicals R.sub.2 or R.sub.3 denotes hydrogen,R.sub.6 represents hydrogen, (C.sub.1 -C.sub.4)-alkyl, phenyl, benzyl or phenylethyl,B represents (C.sub.1 -C.sub.7)-alkylene which is unsubstituted or substituted one or more times by hydroxyl, (C.sub.1 -C.sub.4)-alkyl or by the group NR.sub.4 R.sub.5 and which can optionally be closed to form an alicyclic 4- to 7-membered ring,R.sub.8 and R.sub.9, which can be identical or different, represent hydrogen or (C.sub.1 -C.sub.6)-alkyl andZ represents phenyl, naphthyl, pyridyl or thiazolyl, each of which can be unsubstituted or substituted one or more times by (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.6)-alkoxy, benzyloxy, trifluoromethyl, halogen, nitro, (C.sub.3 -C.sub.7)-cycloalkoxy, (C.sub.1 -C.sub.4)-alkylthio, trifluoromethylthio or by the group NR.sub.4 R.sub.5, the pharmaceutically utilizable salts thereof, a process for the preparation thereof and the use thereof as medicament for the treatment of hypertension, cardiac insufficiency and disturbances of peripheral circulation.
    • 本发明涉及式Ⅰ的新的哌嗪基烷基-3(2H) - 哒嗪酮,其中基团R 1表示氢,苯基,苄基或(C 1 -C 6) - 烷基,其未被取代或被一个或多个 羟基,哌啶,吗啉或NR4R5基团,其中R4和R5可以相同或不同,代表氢,甲基或乙基,R2和R3代表氢,卤素,(C1-C6) - 烷氧基或(C1-C6) - 烷基,其中基团R 2或R 3中的至少一个表示氢,R 6表示氢,(C 1 -C 4) - 烷基,苯基,苄基或苯乙基,B表示未取代或取代的 羟基,(C 1 -C 4) - 烷基或NR 4 R 5基团更多次,并且其可任选地被封闭以形成脂环族4-至7-元环,可以相同或不同的R 8和R 9表示氢或( C 1 -C 6) - 烷基,Z表示苯基,萘基,吡啶基或噻唑基,其各自可以是未取代的或取代的一个或多个t (C 1 -C 6) - 烷基,(C 1 -C 6) - 烷氧基,苄氧基,三氟甲基,卤素,硝基,(C 3 -C 7) - 环烷氧基,(C 1 -C 4) - 烷硫基,三氟甲硫基或NR 4 R 5基团 其药学上可用的盐,其制备方法及其作为治疗高血压,心脏功能不全和外周循环紊乱的药物的用途。