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    Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments
    4.
    发明授权
    Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments 失效
    取代的三环噻吩化合物，它们的合成，其用途，组合物和药物

    公开(公告)号：US4381301A

    公开(公告)日：1983-04-26

    申请号：US175244

    申请日：1980-08-04

    申请人： Georg Rainer

    发明人： Georg Rainer

    IPC分类号： C07D495/04 ,  A61K31/495 ,  C07D521/00

    CPC分类号： C07D495/04

    摘要： Substituted thienobenzodiazepinones of the general formula I ##STR1## [wherein R.sup.1 denotes a hydrogen atom (--H) or an alkyl radical with 1 to 4 carbon atoms; R.sup.2 represents a halogen atom (halo) or has one of the meanings of R.sup.1 ; R.sup.3 denotes a halogen atom (halo) or the group --N(R.sup.4)R.sup.5 ; R.sup.4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R.sup.5 has one of the meanings of R.sup.4 or represents the group --(CH.sub.2).sub.m --N(R.sup.6)R.sup.7 ; or R.sup.4 and R.sup.5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R.sup.6 denotes an alkyl group with 1 to 4 carbon atoms; R.sup.7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.

    摘要翻译： （I）[其中R1表示氢原子（-H）或具有1至4个碳原子的烷基）的取代的噻吩并二氮杂酮; R 2表示卤原子（卤素）或具有R 1的含义之一; R3表示卤素原子（卤素）或基团-N（R4）R5; R4表示具有1至4个碳原子的烷基或具有3至5个碳原子的烯基; R5具有R4的含义之一或表示基团 - （CH 2）m -N（R 6）R 7; 或R 4和R 5与两个键合的氮原子一起表示吗啉代基，吡咯烷子基，哌啶子基，六氢吖庚因-1-基，哌嗪-1-基（其任选被取代在 4-甲基，乙基或苄基的4-位），2,4-二甲基哌嗪-1-基或六氢-1H-1,4-二氮杂-1-基（其在4- 甲基或乙基的位置）; R6表示具有1至4个碳原子的烷基; R 7表示碳原子数1〜4的烷基。 A表示具有1至5个碳原子的直链或支链亚烷基; m表示2或3]，它们的酸加成盐是新化合物。 它们对胃和肠具有保护作用，并且适用于基于胃或肠的疾病治疗疾病，或者它们是用于制备具有保护作用的产品的中间体。 提出了制备新的药理活性化合物和中间产物的方法。