Sulfonamido-benzoic acid derivatives
    3.
    发明授权
    Sulfonamido-benzoic acid derivatives 失效
    磺酰氨基 - 苯甲酸衍生物

    公开(公告)号:US4244871A

    公开(公告)日:1981-01-13

    申请号:US58363

    申请日:1979-07-12

    摘要: The invention relates to novel sulfonamidobenzoic acid derivatives having the general formula ##STR1## wherein R.sup.1 denotes a C.sub.1-4 alkoxy group or a hydrazino group or an NR.sup.4 R.sup.5 group, wherein R.sup.4 and R.sup.5 denote each a hydrogen atom or an identical or different C.sub.1-4 alkyl group; furthermore R.sup.4 may denote an aralkyl or substituted aralkyl group provided that R.sup.5 denotes a hydrogen atom; furthermore NR.sup.4 R.sup.5 may denote a morpholine or piperazine ring;R.sup.2 and R.sup.3 may denote each a hydrogen atom or an identical or different C.sub.1-4 aliphatic group; furthermore R.sup.2 may denote a cycloaliphatic, aralkyl, substituted aralkyl or amino group provided that R.sup.3 denotes a hydrogen atom; furthermore R.sup.2 and R.sup.3 may denote together with the adjacent nitrogen atom a morpholino ring, an unsubstituted piperazine ring or a substituted piperazine ring,and to their pharmaceutically acceptable acid addition salts. Furthermore, the invention relates to a process for preparing these compounds.The novel sulfonamidobenzoic acid derivatives having the general formula I possess significant tyrosine-paralyzing activity and thus they retard the biosynthesis of noradrenaline.

    摘要翻译: 本发明涉及具有通式的新型磺酰胺基苯甲酸衍生物,其中R 1表示C 1-4烷氧基或肼基或NR 4 R 5基,其中R 4和R 5各自表示氢原子或相同或不同的C 1-4 烷基; 此外,R 4可以表示芳烷基或取代的芳烷基,条件是R 5表示氢原子; 此外NR4R5可以表示吗啉或哌嗪环; R2和R3可以表示氢原子或相同或不同的C1-4脂族基团; 此外,R 2可以表示脂环族,芳烷基,取代的芳烷基或氨基,条件是R 3表示氢原子; 此外R2和R3可以与相邻的氮原子一起表示吗啉代环,未取代的哌嗪环或取代的哌嗪环,以及它们的药学上可接受的酸加成盐。 此外,本发明涉及一种制备这些化合物的方法。 具有通式I的新型磺酰胺基苯甲酸衍生物具有显着的酪氨酸 - 麻痹活性,因此它们延缓了去甲肾上腺素的生物合成。