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    • 8. 发明授权
    • Aminobenzoic acid derivatives
    • 氨基苯甲酸衍生物
    • US4294851A
    • 1981-10-13
    • US919747
    • 1978-06-27
    • Gunter MetzManfred Specker
    • Gunter MetzManfred Specker
    • C07D207/09C07D213/40C07D213/80C07D239/90C07D295/13C07D295/192A61K31/17A61K31/165C07C101/00C07C103/78
    • C07D213/40C07D207/09C07D213/80C07D239/90C07D295/13C07D295/192Y10S514/821
    • The object of the present invention are novel aminobenzoic acid derivatives having the general formula: ##STR1## wherein R.sub.1 is hydrogen, chlorine, hydroxy, acetoxy or C.sub.1 -C.sub.3 -alkoxy;R.sub.2 is hydrogen, chlorine or sulfamoyl;R.sub.5 is hydrogen or combined with R.sub.6 a C.sub.2 -C.sub.3 -alkylene;Y is the group ##STR2## or in ortho-position together with the hydrogen atom on the nitrogen and with R.sub.5 the group ##STR3## wherein R.sub.3 is hydrogen or methyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.3 -alkyl, or with Z substituted phenoxy; andZ is hydrogen, halogen or trifluoromethyl;X is C.sub.1 -C.sub.3 -alkylene forming, if necessary, under substitution with R.sub.6 a 5- or 6-link aliphatic or aromatic ring system;R.sub.6 is C.sub.1 -C.sub.4 -alkyl or in combination with X a C.sub.3 -C.sub.4 -cycloalkylene or cycloarylene;R.sub.7 is hydrogen, C.sub.1 -C.sub.3 -alkyl, formyl, the group Y, or together with R.sub.6 a C.sub.4 -C.sub.5 -cycloalkylene, or together with X and R.sub.6 pyridylmethyl;R.sub.8 is hydrogen or, if necessary, halogen- or phenyl-substituted C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkenyl; andn has the value 0 or 1,and if n=1, their salts with pharmaceutically compatible acid radicals.Said compounds show antilipemic activity.The present invention relates furthermore to the preparation of said compounds and of drugs containing such compounds.
    • 本发明的目的是具有以下通式的新的氨基苯甲酸衍生物:其中R 1是氢,氯,羟基,乙酰氧基或C 1 -C 3 - 烷氧基; R2是氢,氯或氨磺酰; R5是氢或R6与C2-C3-亚烷基结合; Y是基团或与氮原子上的氢原子一起在邻位置,R5是基团,其中R3是氢或甲基; R4是氢,C1-C3-烷基或与Z取代的苯氧基; Z是氢,卤素或三氟甲基; 如果需要,X是C 1 -C 3 - 亚烷基,用R 6取代为5-或6-连接的脂族或芳族环系; R6是C1-C4-烷基或与X一个C3-C4-亚环烷基或环亚芳基组合; R 7为氢,C 1 -C 3 - 烷基,甲酰基,Y基团,或与R6一起为C4-C5-亚环烷基,或与X和R6吡啶基甲基一起; R8是氢或必要时卤素或苯基取代的C 1 -C 4 - 烷基或C 1 -C 4 - 烯基; 并且n具有0或1的值,并且如果n = 1,则其与药学上相容的酸基的盐。 所述化合物显示抗血脂活性。 本发明还涉及所述化合物和含有这些化合物的药物的制备。