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    • 3. 发明授权
    • Pyrazolopyridazine antihypertensives
    • 吡唑并嗪抗高血压药
    • US4399136A
    • 1983-08-16
    • US272351
    • 1981-06-10
    • Cedric H. HassallGeoffrey LawtonChristopher J. Moody
    • Cedric H. HassallGeoffrey LawtonChristopher J. Moody
    • C07D237/04C07D487/04C07D491/14A61K31/50C07D487/14
    • C07D487/04C07D237/04C07D491/14
    • Compounds of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, B is carbonyl or methylene, R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, hydroxyaminocarbonyl, mercapto, lower alkanoylthio or aryl(lower alkylthio)--, R.sup.2 is hydroxy, lower alkoxy or amino, R.sup.3 is hydrogen, lower alkyl, aryl or aryl(lower alkyl)--, R.sup.4 is hydrogen, lower alkyl, aryl, aryl-(lower alkyl)-- or a group of the formula --A-R.sup.1 wherein A and R.sup.1 are as described above and the broken line denotes an optional carbon-carbon bond which can be present only when B is carbonyl,and salts of the acids of formula I with pharmaceutically acceptable bases, a process for the manufacture thereof and pharmaceutical preparations containing same, are described. The compounds of formula I and their salts are useful as antihypertensive agents.
    • 式Ⅰ化合物其中A是可被低级烷基取代的亚甲基,亚乙基或丙烯,B是羰基或亚甲基,R 1是卤素,羧基,低级烷氧基羰基,羟基氨基羰基,巯基,低级烷酰硫基或芳基(低级烷硫基 ) - ,R2是羟基,低级烷氧基或氨基,R3是氢,低级烷基,芳基或芳基(低级烷基) - ,R4是氢,低级烷基,芳基,芳基 - (低级烷基) - 或式 -A-R1其中A和R1如上所述,虚线表示只有当B是羰基时才能存在的任选的碳 - 碳键,以及式I的酸与药学上可接受的碱的盐, 描述其制备方法和含有它们的药物制剂。 式I化合物及其盐可用作抗高血压药。