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    Novel indole carboxamides
    8.
    发明授权
    Novel indole carboxamides 失效
    新型吲哚甲酰胺

    公开(公告)号：US4791109A

    公开(公告)日：1988-12-13

    申请号：US883915

    申请日：1986-07-10

    申请人： Francois Clemence ,  Jacques Guillaume ,  Gilles Hamon

    发明人： Francois Clemence ,  Jacques Guillaume ,  Gilles Hamon

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/445 ,  A61K31/495 ,  A61P9/06 ,  C07D209/08 ,  C07D209/34 ,  A61K31/535 ,  C07D413/12

    CPC分类号： C07D209/34 ,  C07D209/08

    摘要： Novel indole-carboxamides of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.2, acylamide of an aliphatic carboxylic acid of 2 to 5 carbon atoms and mono and dialkylamino with alkyl of 1 to 5 carbon atoms, a and b form .dbd.O and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, A is selected from the group consisting of --(CH.sub.2).sub.n --and ##STR3## n is an integer from 2 to 5, m is an integer from 1 to 3, B is ##STR4## R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-arrhythmic properties.

    摘要翻译： 式I的新型吲哚甲酰胺其中R和R 1分别选自氢，1至5个碳原子的烷基，3至7个碳原子的环烷基，4至7个碳原子的环烷基烷基和芳烷基 任选被1至3个由卤素，甲基，乙基，甲氧基，乙氧基，-CF 3，CH 3 S - ， - NH 2和-NO 2组成的组中取代的7至12个碳原子，或者R 1和R 3与氮原子一起形成 任选地含有-O - ， - S-和R'的成员的任选的不饱和杂环选自氢，1至5个碳原子的烷基，苯基，萘基，7位的芳烷基 至12个碳原子和取代的苯基，R 3选自氢，1至5个碳原子的烷基，1至3个碳原子的烷氧基，氯，溴，碘，-NO 2，-NH 2，脂族 2至5个碳原子的羧酸和一烷基和二烷基氨基 1至5个碳原子，a和b形式= O，c是氢或a和c形成碳 - 碳键，b是氢，A选自 - （CH 2）n - 和＆lt; IMAGE＆gt; n 是2至5的整数，m是1至3的整数，B是选自氢和1至5个碳原子的烷基及其无毒的药学上可接受的酸加成盐 具有显着的抗心律失常性质。

    Process for preparation of piperidyl-indoles
    9.
    发明授权
    Process for preparation of piperidyl-indoles 失效
    哌啶基 - 吲哚的制备方法

    公开(公告)号：US4232031A

    公开(公告)日：1980-11-04

    申请号：US100909

    申请日：1979-12-06

    申请人： Claude Dumont ,  Jacques Guillaume ,  Lucien Nedelec

    发明人： Claude Dumont ,  Jacques Guillaume ,  Lucien Nedelec

    IPC分类号： C07D401/04 ,  A61K20060101 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/475 ,  A61P1/08 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  B01J23/04 ,  C07D20060101 ,  C07D209/04 ,  C07D211/68 ,  C07D211/70 ,  C07D401/02

    CPC分类号： C07D401/04

    摘要： A novel process for the preparation of piperidylindoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms and X is selected from the group consisting of hydrogen, nitro, fluorine, bromine, chlorine and alkoxy of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts thereof by reacting an indole of the formula ##STR2## with 4-piperidone hydrochloride in an alkaline medium to obtain the compound of formula I which is optionally salified and the novel product, 5-nitro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole and its non-toxic, pharmaceutically acceptable acid addition salts.

    摘要翻译： 一种制备式Ia的哌啶子基吲哚的新方法，其中R选自氢和1至3个碳原子的烷基，X选自氢，硝基，氟，溴， 氯和具有1至3个碳原子的烷氧基以及它们的无毒的药学上可接受的酸加成盐，其通过使式II的吲哚与4-哌啶酮盐酸盐在碱性介质中反应，得到式I化合物，其为 任选地盐化，并且新产物5-硝基-3-（1,2,3,6-四氢吡啶-4-基）-1H-吲哚及其无毒的药学上可接受的酸加成盐。