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    Condensed diazepinones, processes for preparing them and pharmaceutical compositions containing these compounds
    42.
    发明授权
    Condensed diazepinones, processes for preparing them and pharmaceutical compositions containing these compounds 失效
    浓缩二氮杂酮，其制备方法和含有这些化合物的药物组合物

    公开(公告)号：US4873236A

    公开(公告)日：1989-10-10

    申请号：US136212

    申请日：1987-12-18

    申请人： Wolfhard Engel ,  Wolfgang Eberlein ,  Gerhard Mihm ,  Gunter Trummlitz ,  Norbert Mayer ,  Adriaan De Jonge

    发明人： Wolfhard Engel ,  Wolfgang Eberlein ,  Gerhard Mihm ,  Gunter Trummlitz ,  Norbert Mayer ,  Adriaan De Jonge

    IPC分类号： C07D519/00 ,  A61K31/55 ,  A61P9/06 ,  A61P25/02 ,  C07D223/20 ,  C07D243/38 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04

    CPC分类号： C07D401/12 ,  C07D243/38 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

    摘要： There are described new condensed diazepinones of general formula ##STR1## wherein .circle.B represents one of the divalent groups ##STR2## and D represents the groups ##STR3## and X.sup.1, X.sup.2 represents a .dbd.CH-- group or, if .circle.B assumes the meaning of the divalent group S, U or W, they may also represent an N atom, A.sup.1 and A.sup.2 in general represent lower alkylene groups, Z represents a C--C bond or the groups, --O--, --S--, --CH.sub.2 --, or --(CH.sub.2).sub.2 --; R represents hydrogen or methyl, R.sup.1 and R.sup.2 generally represent alkyl groups which, together with the nitrogen atom between them, may also form a saturated monocylic, heterocyclic group, R.sub.3 represents alkyl, chlorine or hydrogen, R.sub.4 represents hydrogen or methyl, R.sup.5 and R.sup.6 represent hydrogen, halogen or alkyl, R.sub.7 represents hydrogen, chlorine or methyl, R.sup.8 represents hydrogen or lower alkyl, R.sup.9 represents hydrogen, halogen, lower alkyl and R.sup.10 represents hydrogen or methyl and R.sup.12 represents branched or unbranched alkyl. The compounds of general formula I and the acid addition salts thereof may be resolved into their isomers. The compounds of formula I and their salts may be used as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia.

    摘要翻译： 描述了通式为“IMAGE”（I）的新的缩合二氮杂酮，其中＆cir＆B表示二价基团之一 + TR ，D表示基团 + TR 和X1 ，X2表示a = CH-基团，或者如果＆Cir＆B表示二价基团S，U或W的含义，它们也可以表示N原子，A1和A2一般表示低级亚烷基，Z表示CC键或 基团，-O - ， - S - ， - CH 2 - 或 - （CH 2）2 - ; R表示氢或甲基，R 1和R 2通常表示烷基，它们与氮原子一起也可以形成饱和单环，杂环基，R 3表示烷基，氯或氢，R 4表示氢或甲基，R 5和R 6 代表氢，卤素或烷基，R7代表氢，氯或甲基，R8代表氢或低级烷基，R9代表氢，卤素，低级烷基，R10代表氢或甲基，R12代表支链或非支链烷基。 通式I的化合物及其酸加成盐可以分解成它们的异构体。 式I化合物及其盐可用作迷走神经起搏器用于治疗心动过缓和缓慢性心律失常。

    2-Phenyl-pyrimidones
    48.
    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。

    Pyridazinone-substituted benzimidazoles and salts
    49.
    发明授权
    Pyridazinone-substituted benzimidazoles and salts 失效
    哒嗪酮取代的苯并咪唑和盐

    公开(公告)号：US4361563A

    公开(公告)日：1982-11-30

    申请号：US259537

    申请日：1981-05-01

    申请人： Volkhard Austel ,  Joachim Heider ,  Wolfgang Eberlein ,  Willi Diederen ,  Walter Haarmann

    发明人： Volkhard Austel ,  Joachim Heider ,  Wolfgang Eberlein ,  Willi Diederen ,  Walter Haarmann

    IPC分类号： A61K31/50 ,  C07D235/18 ,  C07D237/04 ,  C07D403/04

    CPC分类号： C07D237/04 ,  A61K31/50 ,  C07D235/18 ,  Y10S514/822

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; trifluoromethyl; alkyl of 1 to 11 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; hydroxyl; alkoxy of 1 to 6 carbon atoms; mercapto; (alkyl of 1 to 6 carbon atoms)-mercapto; phenyl-(alkyl of 1 to 3 carbon atoms); phenyl; or mono-, di- or tri-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, alkyl of 1 to 4 carbon atoms, (alkyl of 1 to 6 carbon atoms)-sulfinyl, hydroxyl, alkoxy of 1 to 6 carbon atoms, mercapto or (alkyl of 1 to 6 carbon atoms)-mercapto;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or phenyl-(alkyl of 1 to 3 carbon atoms); andR.sub.3 is alkyl of 1 to 6 carbon atoms; optically active antipodes thereof; and non-toxic, pharmaceutically acceptable acid addition salts of said compounds or of said optically active antiposed. The compounds are useful as cardiotonics and antithrombotics.

    摘要翻译： 其中R 1是氢的式IMAMA的化合物; 三氟甲基 1至11个碳原子的烷基; 3至7个碳原子的环烷基; 羟; 1至6个碳原子的烷氧基; 巯基 （1-6个碳原子的烷基） - 巯基; 苯基 - （1至3个碳原子的烷基）; 苯基; 或单取代，二取代或三取代的苯基，其中可以相同或不同的取代基各自为卤素，具有1至4个碳原子的烷基，（1至6个碳原子的烷基） - 亚磺酰基 ，羟基，1至6个碳原子的烷氧基，巯基或（1至6个碳原子的烷基） - 巯基; R2是氢，1至6个碳原子的烷基，3至6个碳原子的环烷基或苯基 - （1至3个碳原子的烷基）; 且R 3为1至6个碳原子的烷基; 光学活性对映体; 和所述化合物或所述光学活性药物的无毒的药学上可接受的酸加成盐。 这些化合物可用作强心剂和抗血栓药物。

    (Aminoalkoxy-aryl)-substituted isoquinolinones and naphthydrinones and salts thereof, and hypotensive compositions and methods employing them
    50.
    发明授权
    (Aminoalkoxy-aryl)-substituted isoquinolinones and naphthydrinones and salts thereof, and hypotensive compositions and methods employing them 失效
    （氨基烷氧基 - 芳基） - 取代的异喹啉酮和萘啶酮及其盐，以及使用它们的低血压组合物和方法

    公开(公告)号：US4154837A

    公开(公告)日：1979-05-15

    申请号：US867308

    申请日：1978-01-06

    申请人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

    发明人： Joachim Heider ,  Volkhard Austel ,  Wolfgang Eberlein ,  Rudolf Kadatz ,  Jurgen Dammgen ,  Walter Kobinger ,  Christian Lillie

    IPC分类号： A61K31/444 ,  A61K31/47 ,  A61K31/472 ,  A61P9/00 ,  A61P9/12 ,  C07D217/24 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D217/24

    摘要： Compounds of the formula ##STR1## wherein A is benzo, mono-, di- or tri-substituted benzo, the substituents being selected from the group consisting of lower alkoxy, amino and nitro, or pyrido;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl of 1 to 6 carbon atoms or --X--R.sub.6, where X is straight alkylene of 1 to 4 carbon atoms or hydroxy-substituted straight alkylene of 1 to 4 carbon atoms; andR.sub.6 is amino; carbalkoxy of 2 to 6 carbon atoms; phenyl; mono-, di- or tri-substituted phenyl, the substituents being selected from the group consisting of lower alkyl and lower alkoxy; phenoxy; or mono-, di- or tri-substituted phenoxy, the substituents being selected from the group consisting of lower alkyl and lower alkoxy;R.sub.3 is hydrogen or hydroxyl;R.sub.4 is hydrogen, lower alkyl or lower alkoxy;R.sub.5 is hydrogen or lower alkyl; andN is 0, 1 or 2;And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as antiarrhythmics, .beta.-adrenergic-receptor blockers and anti-anginous agents.

    摘要翻译： 其中A是苯并，一或二取代或三取代的苯并，其取代基选自低级烷氧基，氨基和硝基，或吡啶并。 R1是氢或低级烷基; R2是1至6个碳原子的烷基或-X-R6，其中X是1至4个碳原子的直链亚烷基或1至4个碳原子的羟基取代的直链亚烷基; R6为氨基; 2至6个碳原子的烷氧基; 苯基; 单取代，二取代或三取代的苯基，所述取代基选自低级烷基和低级烷氧基; 苯氧基 或单 - ，二 - 或三 - 取代的苯氧基，所述取代基选自低级烷基和低级烷氧基; R3是氢或羟基; R4是氢，低级烷基或低级烷氧基; R5是氢或低级烷基; 和N IS 0，1或2; 和非毒性，药理学上可接受的酸添加量。 化合物和盐可用作抗心律失常药，β-肾上腺素能受体阻断剂和抗麻痹剂。