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    Novel aminoalkylthio derivatives of triazolopyridine or triazoloquinoline, the processes for their preparation, and drugs, useful especially as analgesics, in which they are present
    7.
    发明授权
    Novel aminoalkylthio derivatives of triazolopyridine or triazoloquinoline, the processes for their preparation, and drugs, useful especially as analgesics, in which they are present 失效
    三唑并吡啶或三唑并喹啉的新型氨基烷基硫代衍生物，其制备方法和药物，特别是其中存在的止痛剂

    公开(公告)号：US4886805A

    公开(公告)日：1989-12-12

    申请号：US72337

    申请日：1987-07-10

    申请人： Nicole Bru-Magniez ,  Jean-Marie Teulon ,  Michele Launay

    发明人： Nicole Bru-Magniez ,  Jean-Marie Teulon ,  Michele Launay

    IPC分类号： A61K31/435 ,  A61P25/04 ,  A61P25/20 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel compounds corresponding to the formula: ##STR1## in which: n represents an integer between 1 and 8 and optimally 2 or 3; (CH.sub.2).sub.n --N can also form a ring or a heterocycle, for example having 5 to 7 atoms and preferably 6 atoms;R.sub.1 and R.sub.2 can represent hydrogen or a lower alkyl having 1 to 5 carbon atoms or can form, together with the nitrogen, a ring such as pyrrolidine, piperidine, morpholine, thiomorpholine, phenyltetrahydropyridine, piperazine or piperazine N-substituted by an alkyl, a phenyl or a heterocycle; in the case of the phenyltetrahydropyridines and the phenylpiperazines or heteroarylpiperazines, the phenyl or the heterocycle may or may not be substituted by halogens or methoxy, thiomethyl, hydroxyl, nitro, amino, cyano, lower alkyl, trifluoromethyl or trichloromethyl groups; andR.sub.3, R.sub.4 and R.sub.5 can represent hydrogen, a lower alkyl, a hydroxyalkyl or hydroxybenzyl group, a halogen, a trifluoromethyl, a methoxy, a thiomethyl or a nitro or two of them can form a ring, in particular a phenyl in the case of the triazoloquinolines or the triazoloisoquinolines; and the non-toxic acid addition salts.These products are useful as drugs and possess analgesic properties, acting especially on the central nervous system as minor tranquilizers.

    摘要翻译： 本发明涉及对应于下式的新化合物：其中：n表示1至8之间的整数，最佳为2或3; （CH 2）n -N也可以形成环或杂环，例如具有5至7个原子，优选6个原子; R 1和R 2可以表示氢或具有1至5个碳原子的低级烷基，或者可以与氮一起形成诸如吡咯烷，哌啶，吗啉，硫代吗啉，苯基四氢吡啶，哌嗪或被烷基N-取代的哌嗪的环， 苯基或杂环; 在苯基四氢吡啶和苯基哌嗪或杂芳基哌嗪的情况下，苯基或杂环可以被卤素或甲氧基，硫代甲基，羟基，硝基，氨基，氰基，低级烷基，三氟甲基或三氯甲基取代; 并且R 3，R 4和R 5可以表示氢，低级烷基，羟基烷基或羟基苄基，卤素，三氟甲基，甲氧基，硫代甲基或硝基或它们中的两个可以形成环，特别是在这种情况下的苯基 的三唑并喹啉或三唑并异喹啉; 和无毒的酸加成盐。 这些产品作为药物是有用的，具有镇痛作用，特别是作为轻度镇定剂对中枢神经系统起作用。