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    • 10. 发明授权
    • N-Substituted-1-aminoalkyl-1,4-dihydropyridines
    • N-取代的-1-氨基烷基-1,4-二氢吡啶
    • US4472584A
    • 1984-09-18
    • US471959
    • 1983-03-03
    • Bernard LoevHoward JonesJohn T. Suh
    • Bernard LoevHoward JonesJohn T. Suh
    • C07D211/90C07D211/82A61K31/455C07D401/04C07D405/04
    • C07D211/90
    • Compounds of the formula: ##STR1## wherein Ar is heteroaryl, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydro naphthyl, or a radical of the formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 is independently H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and R.sub.5 and R.sub.6 when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R.sub.1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R.sub.1 may be hydrogen; R.sub.2 is lower alkyl; R.sub.3 is hydroxyalkyl containing 2 to 4 carbon atoms and R.sub.4 is H, alkyl, cycloalkyl or hydroxyalkyl containing 2 to 4 carbon atoms; wherein the alkyl, alkoxy, and acyl groups contain up to 10 carbon atoms, and their pharmaceutically-acceptable salts are disclosed. These compounds have anti-hypertensive activity.
    • 下式的化合物:其中Ar是杂芳基,具有3至7个碳原子的环烷基,萘基,茚满基,茚基,四氢萘基或下式的基团其中R 5,R 6和R 7各自独立地是 H,烷基,芳基,卤素,低级烷氧基,硝基,氨基,烷基巯基,氰基,羧基,烷氧基,氨基磺酰基,三氟甲基,羟基,酰氧基,甲磺酰基,烷基氨基或酰基氨基; 并且R 5和R 6一起形成亚甲二氧基; Z是主链中含有1至约5个碳原子的亚烷基; 每个R 1独立地是氢,烷基或烷氧基烷基,条件是只有一个R 1可以是氢; R2是低级烷基; R3是含有2至4个碳原子的羟基烷基,R4是H,含2至4个碳原子的烷基,环烷基或羟基烷基; 其中烷基,烷氧基和酰基含有至多10个碳原子,并且公开了它们的药学上可接受的盐。 这些化合物具有抗高血压活性。