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    Substituted dibenzodiazepinones
    42.
    发明授权
    Substituted dibenzodiazepinones 失效
    取代的二苯并二氮杂酮

    公开(公告)号：US4447434A

    公开(公告)日：1984-05-08

    申请号：US462149

    申请日：1983-01-31

    申请人： Gunter Trummlitz ,  Wolfhard Engel ,  Wolfgang Eberlein ,  Gunther Schmidt ,  Rudolf Hammer ,  Piero del Soldato

    发明人： Gunter Trummlitz ,  Wolfhard Engel ,  Wolfgang Eberlein ,  Gunther Schmidt ,  Rudolf Hammer ,  Piero del Soldato

    IPC分类号： C07D243/26 ,  A61K31/00 ,  A61K31/55 ,  A61K31/5513 ,  A61P1/04 ,  C07D243/38 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D451/02 ,  C07F9/645

    CPC分类号： C07D451/02 ,  C07D243/38 ,  C07D401/06 ,  C07F9/645

    摘要： The specification describes new substituted dibenzodiazepinones of formula ##STR1## wherein R.sub.1 is hydrogen or chlorine atom and R is (1-methyl-4-piperidinyl)methyl, (1-methyl-1,2,5,6-tetrahydro-4-pyridinyl)methyl,1-methyl-1,2,5,6-tetrahydro-4-pyridinyl, (1-methyl-4-piperidinylidene)methyl,(2,3-dehydro-8-methyl-8-aza-bicyclo[3,2,1]oct-3-yl)-methyl, (8-methyl-8-aza-bicyclo[3,2,1]oct-3-ylidene)-methyl or an endo-or exo-(8-methyl-8-azabicyclo[3,2,1]oct-3-yl)methyl each being optionally substituted by one or two methyls on the heterocyclic ring, and the nontoxic, pharmaceutically acceptable acid addition salts thereof, processes for preparing them and pharmaceutical compositions containing these compounds.The compounds of formula I have an antiulcerative effect and an inhibitory effect on the secretion of gastric substances having anticholinergic activity, such as dryness of the mouth and mydriasis.

    摘要翻译： 该说明书描述了式（Ⅰ）的新的取代二苯并二氮杂酮，其中R 1是氢或氯原子，R是（1-甲基-4-哌啶基）甲基，（1-甲基-1,2,5,6-四氢 - 4-吡啶基）甲基，1-甲基-1,2,5,6-四氢-4-吡啶基，（1-甲基-4-亚哌啶基）甲基，（2,3-脱氢-8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基） - 甲基，（8-甲基-8-氮杂 - 双环[3,2,1]辛-3-基） - 甲基或内 - 或外 - - （8-甲基-8-氮杂双环[3,2,1]辛-3-基）甲基，其各自任选被杂环上的一个或两个甲基取代，及其无毒的药学上可接受的酸加成盐，用于 制备它们和含有这些化合物的药物组合物。 式I化合物具有抗溃疡作用和对具有抗胆碱能活性的胃物质分泌的抑制作用，例如口干和散瞳。

    2-Phenyl-pyrimidones
    50.
    发明授权
    2-Phenyl-pyrimidones 失效
    2-苯基 - 嘧啶酮

    公开(公告)号：US4379788A

    公开(公告)日：1983-04-12

    申请号：US327348

    申请日：1981-12-04

    申请人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Christian Lillie

    发明人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Christian Lillie

    IPC分类号： C07D239/88 ,  A61K31/513 ,  A61P9/00 ,  C07D213/82 ,  C07D239/91 ,  C07D265/22 ,  C07D471/04 ,  C07D498/04 ,  A61K31/505

    CPC分类号： C07D213/82 ,  C07D239/91 ,  C07D265/22 ,  C07D471/04

    摘要： Compounds of the formula ##STR1## wherein A and B, together with each other and the respective carbon atoms to which they are attached, form a phenyl or pyridine ring;R.sub.1 is hydrogen, halogen, amino, nitro, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;R.sub.2 is hydrogen or alkoxy of 1 to 3 carbon atoms;D is alkylene of 3 to 4 carbon atoms or hydroxy(alkylene of 3 to 4 carbon atoms);R.sub.3 and R.sub.5, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen or alkoxy of 1 to 3 carbon atoms; andR.sub.6 is straight or branched alkyl of 1 to 6 carbon atoms or --E--R.sub.7 ;where E is straight alkylene of 2 to 4 carbon atoms or hydroxy-substituted straight alkylene of 2 to 4 carbon atoms, andR.sub.7 is ##STR2## where R.sub.8 and R.sub.9 are each hydrogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof formed with inorganic or organic acids; the compounds as well as their salts are useful as hypotensives, antiarrhythmics and .beta.-receptor-blockers.

    摘要翻译： 其中A和B与它们相连的相互连接的碳原子一起形成苯基或吡啶环; R 1是氢，卤素，氨基，硝基，1至3个碳原子的烷基或1至3个碳原子的烷氧基; R2是氢或1〜3个碳原子的烷氧基; D是3至4个碳原子的亚烷基或羟基（3至4个碳原子的亚烷基）; R 3和R 5可以相同或不同，分别为氢或1-3个碳原子的烷基; R4是氢或1〜3个碳原子的烷氧基; R6是1-6个碳原子的直链或支链烷基或-E-R7; 其中E是2至4个碳原子的直链亚烷基或2至4个碳原子的羟基取代的直链亚烷基，并且R 7是R 8和R 9各自为氢，1至3个碳原子的烷基或1至 3个碳原子; 和与无机或有机酸形成的无毒的，药学上可接受的酸加成盐; 化合物及其盐可用作低血糖，抗心律失常药和β-受体阻滞剂。