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。

    Compositions with potentiated hypotensive effects
    5.
    发明授权
    Compositions with potentiated hypotensive effects 失效
    具有强化降压作用的组合物

    公开(公告)号:US4287194A

    公开(公告)日:1981-09-01

    申请号:US55263

    申请日:1979-07-06

    CPC分类号: A61K31/50 A61K31/40

    摘要: A pharmaceutical compositions with hypotensive effects which comprise a compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof, ##STR1## wherein R.sup.1 is formula (II) ##STR2## wherein R.sup.4 and R.sup.5 each represent hydrogen, hydroxy, nitro at the same timeR.sup.2 and R.sup.3 are hydrogen, orR.sup.1 are 3-chloro-6-pyridazinylamino, 3-methyl-6-pyridazinylamino or 3-carbamoyl-6-pyridazinylamino, and at the same timeR.sup.2 and R.sup.3 form together formula (III), ##STR3## wherein R.sup.6 is C.sub.1-4 alkyl group,R.sup.7 is hydrogen or a C.sub.1-4 alkyl group, andn is an integer of 1 to 3, orR.sup.2 and R.sup.3 form together a group of the general formula (IV),=Q-R.sup.8 (IV)whereinQ is C.sub.5-7 cycloaliphatic, andR.sup.8 is hydrogen, a C.sub.1-4 alkoxycarbonyl or a C.sub.2-4 alkyl,and a compound of formula (V) or a pharmaceutically acceptable acid addition salt thereof, ##STR4## wherein R.sup.9 is naphthyl, 4-indolyl or 4-morpholino-1,2,5-thiadiazol-3-yl group or ##STR5## .

    摘要翻译: 具有降血压作用的药物组合物,其包含式(I)化合物或其药学上可接受的酸加成盐,其中R 1为式(II)其中R 4和R 5各自表示氢 ,羟基,硝基,同时R2和R3是氢,或R1是3-氯-6-哒嗪基氨基,3-甲基-6-哒嗪基氨基或3-氨基甲酰基-6-哒嗪基氨基,同时R2和R3形成 (III),其中R6为C1-4烷基,R7为氢或C1-4烷基,n为1〜3的整数,或R2和R3一起形成基团 通式(IV)的化合物= Q-R8(Ⅳ)其中Q为C5-7环脂族基,R8为氢,C1-4烷氧基羰基或C2-4烷基,式(Ⅴ)化合物或式 (V)其中R 9为萘基,4-吲哚基或4-吗啉代-1,2,5-噻二唑-3-基或Ⅵ(VI)。