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126 条记录 (耗时 0.028 秒)

    Pentacyclic compounds, their pharmaceutical compositions, and methods of use
    36.
    发明授权
    Pentacyclic compounds, their pharmaceutical compositions, and methods of use 失效
    五环化合物，其药物组合物和使用方法

    公开(公告)号：US4469697A

    公开(公告)日：1984-09-04

    申请号：US479016

    申请日：1983-03-25

    申请人： Derek V. Gardner ,  Trevor J. White

    发明人： Derek V. Gardner ,  Trevor J. White

    IPC分类号： C07D223/20 ,  C07D471/16 ,  C07D487/04 ,  C07D487/16 ,  C07D498/16 ,  C07D513/16 ,  A61K31/55 ,  C07D487/14

    CPC分类号： C07D487/04 ,  C07D223/20

    摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is CH.sub.2, O, S or NR.sub.4 wherein R.sub.4 is hydrogen or C.sub.1-4 alkyl;one of Y and Z is NR.sub.5 and the other is CR.sub.6 R.sub.7 wherein R.sub.5 is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 acyl and R.sub.6 and R.sub.7 are either both hydrogen or together form an oxo group;R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen atom or by phenyl C.sub.1-4 alkyl optionally substituted in the phenyl ring by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl; andR.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, hydroxy, C.sub.1-4 alkyl C.sub.1-4 alkoxy or trifluoromethyl having pharmacological activity, a process for their preparation and their pharmaceutical use.

    摘要翻译： （I）化合物及其药学上可接受的盐：其中：X为CH 2，O，S或NR 4，其中R 4为氢或C 1-4烷基; Y和Z中的一个是NR 5，另一个是CR 6 R 7，其中R 5是氢，C 1-4烷基或C 1-4酰基，并且R 6和R 7都是氢或一起形成氧代基; R 1是氢，C 1-6烷基，C 3-7环烷基，C 4-7环烯基或被C 2-7烯基取代的C 1-4烷基，C 2-7炔基，C 3-7环烷基，任选地被一个或两个C 1-4取代的氨基 烷基或任选地含有氧原子的C 4-6的聚亚甲基或被苯基环上被C 1-4烷基，C 1-4烷氧基，卤素或三氟甲基任意取代的苯基C 1-4烷基; R2和R3相同或不同，为氢，卤素，羟基，具有药理活性的C1-4烷基C1-4烷氧基或三氟甲基，其制备方法及其药物用途。

    Pentacyclic derivatives of piperazine
    37.
    发明授权
    Pentacyclic derivatives of piperazine 失效
    哌嗪的五环衍生物

    公开(公告)号：US4442098A

    公开(公告)日：1984-04-10

    申请号：US332347

    申请日：1981-12-18

    申请人： Derek V. Gardner ,  Laramie M. Gaster

    发明人： Derek V. Gardner ,  Laramie M. Gaster

    IPC分类号： A61K31/55 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D267/20 ,  C07D471/16 ,  C07D487/04 ,  C07D498/04 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D471/06 ,  A61K31/495 ,  C07D498/06 ,  C07D513/06

    CPC分类号： C07D487/04 ,  C07D223/20 ,  C07D267/20

    摘要： Compounds of formula (I): ##STR1## wherein: X is CH.sub.2, O, S or NR wherein R is hydrogen or C.sub.1-4 alkyl;Y and Z are independently selected from hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or CF.sub.3 ;R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or CF.sub.3 ;R.sub.2 is hydrogen, OH, C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkoxy, C.sub.1-7 acyloxy or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently selected from hydrogen or C.sub.1-6 alkyl; R.sub.4 is hydrogen and R.sub.5 is OH or C.sub.1-4 alkoxy; or R.sub.4 and R.sub.5 together form C.sub.3-6 polymethylene optionally interrupted by O or NR.sub.6 where R.sub.6 is hydrogen or C.sub.1-4 alkyl; or together with R.sub.1 forms an oxo group or .dbd.NOR.sub.7 wherein R.sub.7 is hydrogen or C.sub.1-6 alkyl; andR.sub.3 is hydrogen or C.sub.1-6 alkyl have useful pharmacological activity, processes for their preparation and their use.

    摘要翻译： 式（I）化合物：其中：X为CH 2，O，S或NR，其中R为氢或C 1-4烷基; Y和Z独立地选自氢，C 1-4烷基，C 1-4烷氧基，卤素或CF 3; R 1是氢，C 1-6烷基，苯基或苯基-C 1-4烷基，其中任一个苯基部分可以被一个或多个C 1-6烷基，C 1-6烷氧基，卤素或CF 3取代; R 2是氢，OH，C 1-6烷氧基，苯基-C 1-4烷氧基，C 1-7酰氧基或NR 4 R 5，其中R 4和R 5独立地选自氢或C 1-6烷基; R4是氢，R5是OH或C1-4烷氧基; 或R 4和R 5一起形成任选地被O或NR 6中断的C 3-6的多亚甲基，其中R 6是氢或C 1-4烷基; 或与R 1一起形成氧基或= NOR7，其中R 7为氢或C 1-6烷基; R3为氢或C1-6烷基具有有用的药理活性，其制备方法及其用途。

    Dihydro-dibenzoxepines-thiepines and -morphanthridones, compositions and use
    38.
    发明授权
    Dihydro-dibenzoxepines-thiepines and -morphanthridones, compositions and use 失效
    二氢 - 二苯并氧杂吖庚因 - 硫杂卟啉和 - 哒嗪酮，组合物和用途

    公开(公告)号：US4335122A

    公开(公告)日：1982-06-15

    申请号：US225122

    申请日：1981-03-18

    申请人： Arthur R. McFadden ,  Daniel E. Aultz

    发明人： Arthur R. McFadden ,  Daniel E. Aultz

    IPC分类号： C07D223/20 ,  C07D313/12 ,  C07D337/12 ,  A61K31/335 ,  A61K31/55

    CPC分类号： C07D337/12 ,  C07D223/20 ,  C07D313/12

    摘要： The invention relates to diuretic dihydro-dibenzoxepines-thiepines and -morphanthridones of the formula ##STR1## wherein R is ##STR2## where R.sup.4 is a hydrogen or an alkyl; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen, alkyl or R.sup.2 and R.sup.3 are fused to form a pyrrolidino, morpholino, piperidino or azepino ring substituent; Y is hydrogen, halogen and alkoxy, X is ##STR3## where R.sup.4 is as defined above; m is an integer of 0 or 1; and n is an integer of 2 or 3; and the pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 本发明涉及式Ia的利尿二氢 - 二苯并氧杂吖庚因和哒嗪酮，其中R是氢或烷基; R1是氢或烷基; R2和R3相同或不同，为氢，烷基或R2和R3稠合形成吡咯烷子基，吗啉代，哌啶子基或氮杂环取代基; Y是氢，卤素和烷氧基，X是＆lt; IMAGE＆gt;其中R4如上所定义; m为0或1的整数; n为2或3的整数; 及其药学上可接受的酸加成盐。