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    • 5. 发明授权
    • Dihydro pyridine compounds, compositions and use
    • 二氢吡啶化合物,组成和用途
    • US4616002A
    • 1986-10-07
    • US816461
    • 1986-01-06
    • Bruno KamberThomas LeutertHans KuhnisKurt Eichenberger
    • Bruno KamberThomas LeutertHans KuhnisKurt Eichenberger
    • C07D211/90C07D401/06C07D405/12C07D417/12C07K5/065A61K31/535A61K37/02C07D413/12C07K5/06
    • C07D401/06C07D211/90C07D405/12C07D417/12C07K5/06078
    • Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.9, independently of one another, each represents hydrogen, unsubstituted or substituted alkyl or a carbocyclic or heterocyclic aryl radical; in which R.sub.1 and R.sub.2 together or R.sub.1 and R.sub.3 together may represent unsubstituted or substituted lower alkylene in which a carbon atom is optionally replaced by a hetero atom, in which R.sub.4 and R.sub.5 together, and likewise R.sub.5 and R.sub.6 together and/or R.sub.8 and R.sub.9 together, independently of one another, may represent unsubstituted or substituted lower alkylene in which a carbon atom may have been replaced by a hetero atom, optical isomers of compounds of the formula I, mixtures of these optical isomers and salts of such compounds that have a salt-forming grouping, are distinguished by cardiovascular, especially blood pressure-reducing, properties. They are manufactured in a manner known per se.
    • 式I的化合物(I)其中n表示1,2或3,Ar表示碳环或杂环芳基,Ac表示酸的酰基,Z表示基团-OR7或-NR8R9,R1 代表氢,未取代或取代的低级烷基,碳环或杂环芳基或游离的醚化或酯化的羟基,R 2和R 3彼此独立地表示氢,未取代或取代的低级烷基,甲酰基或官能改性的甲酰基,羧基或 官能改性的羧基,碳环或杂环芳基或未取代的或单取代或二取代的氨基,R 4表示氢或低级烷基,R 5和R 6彼此独立地表示氢,未取代或取代的低级烷基或碳环或 杂环芳基,R 7,R 8和R 9彼此独立地表示氢,未取代或取代的烷基或碳环或杂环芳基; 其中R 1和R 2一起或R 1和R 3一起可以表示未取代或取代的低级亚烷基,其中碳原子任选被杂原子取代,其中R 4和R 5一起以及R 5和R 6一起和/或R 8和R 9 一起彼此独立地表示未取代或取代的低级亚烷基,其中碳原子可以被杂原子取代,式I化合物的光学异构体,这些光学异构体的混合物和这些化合物的盐,其具有 盐形成分组由心血管特别是降血压特性区分。 它们以本身已知的方式制造。