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    Condensed benzazepine derivative and pharmaceutical composition thereof
    1.
    发明授权
    Condensed benzazepine derivative and pharmaceutical composition thereof 失效
    浓缩的苯并氮杂衍生物及其药物组合物

    公开(公告)号：US5723606A

    公开(公告)日：1998-03-03

    申请号：US586686

    申请日：1996-01-19

    申请人： Akihiro Tanaka ,  Hiroyuki Koshio ,  Nobuaki Taniguchi ,  Akira Matsuhisa ,  Ken-ichiro Sakamoto ,  Atsuki Yamazaki ,  Takeyuki Yatsu

    发明人： Akihiro Tanaka ,  Hiroyuki Koshio ,  Nobuaki Taniguchi ,  Akira Matsuhisa ,  Ken-ichiro Sakamoto ,  Atsuki Yamazaki ,  Takeyuki Yatsu

    IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/55 ,  A61P1/16 ,  A61P3/10 ,  A61P7/02 ,  A61P9/08 ,  C07C233/64 ,  C07D209/48 ,  C07D223/16 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D223/20

    CPC分类号： C07D209/48 ,  C07D223/16 ,  C07D487/04 ,  C07D513/04

    摘要： This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group, A: a single bond; a group represented by the formula --NHCO--(CR.sup.3 R.sup.4).sub.n --, n: 0 or an integer of from 1 to 3, R.sup.3 and R.sup.4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R.sup.3 and R.sup.4 may together form a lower alkylene group having 2 to 7 carbon atoms), and ring C: a benzene ring which may optionally have substituent(s)) and salts thereof; to pharmaceutical compositions which contain these compounds as an active ingredient and to intermediates which are useful in synthesizing these compounds. The compounds of this invention are useful as arginine vasopressin antagonists.

    摘要翻译： PCT No.PCT / JP94 / 01183 Sec。 371日期1996年1月19日 102（e）1996年1月19日PCT PCT 1994年7月19日PCT公布。 出版物WO95 / 03305 日本特开1995年2月2日本发明涉及以下通式（I）表示的含氮芳香族五元环稠合苯并氮杂衍生物： 环B：具有至少1个氮原子和任选的一个氧或硫原子的含氮芳族五元环，其可任选具有取代基，R 1和R 2：它们可以彼此相同或不同， 各自表示氢原子，卤素原子，低级烷基，可以被低级烷基取代的氨基或低级烷氧基，A：单键; 由式NHCO-（CR 3 R 4）n - ，n：0或1〜3的整数表示的基团，R 3和R 4可以相同或不同，表示氢原子，低级 烷基（条件是R3和R4可以一起形成具有2至7个碳原子的低级亚烷基）和环C：可任选具有取代基的苯环）及其盐; 涉及含有这些化合物作为活性成分的药物组合物和可用于合成这些化合物的中间体。 本发明的化合物可用作精氨酸加压素拮抗剂。

    Condensed benzazepine derivative and pharmaceutical composition thereof
    2.
    发明授权
    Condensed benzazepine derivative and pharmaceutical composition thereof 失效
    浓缩的苯并氮杂衍生物及其药物组合物

    公开(公告)号：US5856564A

    公开(公告)日：1999-01-05

    申请号：US972271

    申请日：1997-11-18

    申请人： Akihiro Tanaka ,  Hiroyuki Koshio ,  Nobuaki Taniguchi ,  Akira Matsuhisa ,  Ken-ichiro Sakamoto ,  Atsuki Yamazaki ,  Takeyuki Yatsu

    发明人： Akihiro Tanaka ,  Hiroyuki Koshio ,  Nobuaki Taniguchi ,  Akira Matsuhisa ,  Ken-ichiro Sakamoto ,  Atsuki Yamazaki ,  Takeyuki Yatsu

    IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/55 ,  A61P1/16 ,  A61P3/10 ,  A61P7/02 ,  A61P9/08 ,  C07C233/64 ,  C07D209/48 ,  C07D223/16 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07C229/00

    CPC分类号： C07D209/48 ,  C07D223/16 ,  C07D487/04 ,  C07D513/04

    摘要： This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group,A: a single bond; a group represented by the formula --NHCO--(CR.sup.3 R.sup.4).sub.n --,n: 0 or an integer of from 1 to 3,R.sup.3 and R.sup.4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R.sup.3 and R.sup.4 may together form a lower alkylene group having 2 to 7 carbon atoms), andring C: a benzene ring which may optionally have substituent(s)) and salts thereof; to pharmaceutical compositions which contain these compounds as an active ingredient and to intermediates which are useful in synthesizing these compounds. The compounds of this invention are useful as arginine vasopressin antagonists.

    摘要翻译： 本发明涉及由通式（I）表示的含氮芳族五元环稠合苯并氮杂衍生物（I）（式中符号具有以下含义;环B：含氮芳族5- 具有至少1个氮原子和任选的一个氧或硫原子的多元环，其可以任选具有取代基，R 1和R 2：它们可以相同或不同，并且各自表示氢原子，卤素原子， 低级烷基，可以被低级烷基或低级烷氧基取代的氨基，A：单键;由式-NHCO-（CR 3 R 4）n表示的基团，n： 0或1〜3的整数，R3和R4：它们可以相同或不同，各自表示氢原子，低级烷基（条件是R3和R4可以一起形成具有2个的低级亚烷基 至7个碳原子）和环C：可以任选具有取代基的苯环 （s））及其盐; 涉及含有这些化合物作为活性成分的药物组合物和可用于合成这些化合物的中间体。 本发明的化合物可用作精氨酸加压素拮抗剂。

    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them
    4.
    发明授权
    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them 失效
    取代的四氢异喹啉化合物及其制备方法和含有它们的组合物

    公开(公告)号：US4966904A

    公开(公告)日：1990-10-30

    申请号：US320975

    申请日：1989-03-09

    申请人： Akihiro Tanaka ,  Takashi Fujikura ,  Ryuji Tsuzuki ,  Masaki Yokota ,  Takeyuki Yatsu

    发明人： Akihiro Tanaka ,  Takashi Fujikura ,  Ryuji Tsuzuki ,  Masaki Yokota ,  Takeyuki Yatsu

    IPC分类号： C07D217/16 ,  C07D277/44 ,  C07D495/04 ,  C07D513/04

    CPC分类号： C07D495/04 ,  C07D217/16 ,  C07D513/04

    摘要： A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt therof.

    摘要翻译： 式（I）化合物或其盐及其制备方法; 该化合物具有扩张新生血管束的作用; （I）其中代表式（IMAGE）（其中R4是氢原子或低级烷基磺酰基）; R1是氢，低级烷基，羟基，卤素，氨基或低级酰基氨基; R2是氢，低级烷基，羟基，氨基或低级烷基磺酰基氨基; R3是氢，低级烷基或羟基; R是氢或卤素; 条件是当R 1是羟基时，不存在所有的R 2，R 3和R都是氢的情况，并且进一步条件是当R是氢时，A不包括囟素或盐。

    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them
    6.
    发明授权
    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them 失效
    取代的四氢异喹啉化合物及其制备方法和含有它们的组合物

    公开(公告)号：US5623074A

    公开(公告)日：1997-04-22

    申请号：US269733

    申请日：1994-06-30

    申请人： Akihiro Tanaka ,  Takashi Fujikura ,  Ryuji Tsuzuki ,  Masaki Yokota ,  Takeyuki Yatsu

    发明人： Akihiro Tanaka ,  Takashi Fujikura ,  Ryuji Tsuzuki ,  Masaki Yokota ,  Takeyuki Yatsu

    IPC分类号： C07D217/16 ,  C07D495/04 ,  C07D513/04

    CPC分类号： C07D495/04 ,  C07D217/16 ,  C07D513/04

    摘要： A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt thereof.

    摘要翻译： 式（I）化合物或其盐及其制备方法; 该化合物具有扩张新生血管束的作用; 式（IMA）（其中R4是氢原子或低级烷基磺酰基）; R1是氢，低级烷基，羟基，卤素，氨基或低级酰基氨基; R2是氢，低级烷基，羟基，氨基或低级烷基磺酰基氨基; R3是氢，低级烷基或羟基; R是氢或卤素; 条件是当R 1是羟基时，不存在所有的R 2，R 3和R都是氢的情况，并且进一步条件是当R是氢时，A不包括它们或其盐。