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    Process for producing triazolylbenzophenone derivatives
    1.
    发明授权
    Process for producing triazolylbenzophenone derivatives 失效
    制备三唑基二苯甲酮衍生物的方法

    公开(公告)号：US4141901A

    公开(公告)日：1979-02-27

    申请号：US861010

    申请日：1977-12-15

    申请人： Kentato Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hiroshiko Sugimoto

    发明人： Kentato Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hiroshiko Sugimoto

    IPC分类号： A61K38/00 ,  C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07D249/14

    CPC分类号： C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00 ,  Y10S514/906

    摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n -X-R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.

    摘要翻译： 下式的三唑基二苯甲酮衍生物：其中R表示氢，C1-C6烷基，C1-C6卤代烷基，基团 - （CH2）nX-R5或基团R5表示氢，C1-C6 烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 6 -C 10芳基或C 2 -C 8酰基; X表示硫或氧; n表示0,1,2或3; R 6和R 7各自表示氢或C 1 -C 6烷基 或者“IMAGE”代表吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基; R1代表氢或卤素; R2代表卤素硝基或三氟甲基; R3代表C1-C6烷基，C1-C6卤代烷基，C1-C6 叠氮基 - 烷基，C 6 -C 10芳基，C 2 -C 8酰基或基团R 4和R 8各自表示氢，C 1 -C 6烷基或C 7 -C 10芳烷基; R 9表示氢或C 1 -C 6烷基; R 10表示氢 ，C 1 -C 6烷基，C 7 -C 10芳烷基或C 2 -C 11α-氨基酰基;或者“IMAGE”代表苯二甲酰亚氨基，吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基）及其药学上可接受的 cid加成盐，可用作抗焦虑剂，镇静剂，催眠药，抗惊厥药，肌肉松弛剂，抗抑郁药，其合成中间体及其制备。

    Process for producing triazolylbenzophenone derivatives
    3.
    发明授权
    Process for producing triazolylbenzophenone derivatives 失效
    生产三唑并苯酮衍生物的方法

    公开(公告)号：US4143048A

    公开(公告)日：1979-03-06

    申请号：US861009

    申请日：1977-12-15

    申请人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07D249/14

    CPC分类号： C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00 ,  Y10S514/906

    摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n --X--R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen, nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.

    Triazolylbenzophenone derivatives and production thereof
    6.
    发明授权
    Triazolylbenzophenone derivatives and production thereof 失效
    三唑基二苯甲酮衍生物及其制备

    公开(公告)号：US4147700A

    公开(公告)日：1979-04-03

    申请号：US861011

    申请日：1977-12-15

    申请人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07D249/14

    CPC分类号： C07D239/86 ,  C07D239/92 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06078 ,  A61K38/00 ,  Y10S514/906

    摘要： Triazolylbenzophenone derivatives of the formula: ##STR1## (wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, the group --(CH.sub.2).sub.n --X--R.sup.5, or the group ##STR2## R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.6 -C.sub.10 aryl, or C.sub.2 -C.sub.8 acyl; X represents sulfur or oxygen; n represents 0, 1, 2, or 3; R.sup.6 and R.sup.7 each represents hydrogen or C.sub.1 -C.sub.6 alkyl; or the group ##STR3## represents pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino; R.sup.1 represents hydrogen or halogen; R.sup.2 represents halogen, nitro, or trifluoromethyl; R.sup.3 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halo-alkyl, C.sub.1 -C.sub.6 azido-alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.8 acyl, or the group ##STR4## R.sup.4 and R.sup.8 each represents hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.7 -C.sub.10 aralkyl; R.sup.9 represents hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.10 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkyl, or C.sub.2 -C.sub.11 .alpha.-amino-acyl; or the group ##STR5## represents phthalimido, pyrrolidino, piperidino, morpholino, or .gamma.-methylpiperazino) and their pharmaceutically acceptable acid addition salts, useful as anxiolytics, sedatives, hypnotics, anticonvulsants, muscle relaxants, antidepressants, their synthetic intermediates, and their preparation.

    摘要翻译： 下式的三唑基二苯甲酮衍生物：其中R表示氢，C1-C6烷基，C1-C6卤代烷基，基团 - （CH2）nX-R5或基团R5表示氢，C1-C6 烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 6 -C 10芳基或C 2 -C 8酰基; X表示硫或氧; n表示0,1,2或3; R 6和R 7各自表示氢或C 1 -C 6 烷基;或者“IMAGE”代表吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基; R1代表氢或卤素; R2代表卤素，硝基或三氟甲基; R3代表C1-C6烷基，C1-C6卤代烷基，C1 -C 6叠氮基 - 烷基，C 6 -C 10芳基，C 2 -C 8酰基或者R 4和R 8各自表示氢，C 1 -C 6烷基或C 7 -C 10芳烷基; R 9表示氢或C 1 -C 6烷基; R 10 表示氢，C1-C6烷基，C7-C10芳烷基或C2-C11α-氨基酰基;或者“IMAGE”代表苯二甲酰亚氨基，吡咯烷子基，哌啶子基，吗啉代或γ-甲基哌嗪基）及其药学上可接受的 酸加成盐，可用作抗焦虑剂，镇静剂，催眠药，抗惊厥药，肌肉松弛剂，抗抑郁药，其合成中间体及其制备。

    1-Substituted thiomethyltriazolobenzodiazepines
    8.
    发明授权
    1-Substituted thiomethyltriazolobenzodiazepines 失效
    1-取代的硫代甲基三唑并苯并二氮杂卓

    公开(公告)号：US4231930A

    公开(公告)日：1980-11-04

    申请号：US16615

    申请日：1979-03-01

    申请人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba

    发明人： Kentaro Hirai ,  Toshio Fujishita ,  Teruyuki Ishiba

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D249/08 ,  C07D487/04 ,  C07D519/00

    CPC分类号： C07D249/08 ,  C07D487/04 ,  Y02P20/55

    摘要： A compound of the formula: ##STR1## wherein R is hydrogen, 2-5C alkoxycarbonyl, 1-7C acyl, 1-4C alkylthio, 7-10C phenylalkylthio, phenylthio, halo-phenylthio, disubstituted aminothio, ##STR2## R.sup.1 is hydrogen or halogen; R.sup.2 is halogen or nitro;and its pharmaceutically acceptable acid addition salts. The compounds and salts thereof are useful as psychotropic agents and as anxiolytics, anticonvulsants and hypnotics.

    摘要翻译： 下式的化合物：其中R是氢，2-5C烷氧基羰基，1-7C酰基，1-4C烷硫基，7-10C苯基烷硫基，苯硫基，卤代苯硫基，二取代氨基硫代，＆lt; IMAGE＆gt; + TR＆lt; IMAGE > R1是氢或卤素; R2是卤素或硝基; 及其药学上可接受的酸加成盐。 其化合物和盐可用作精神药物和抗焦虑剂，抗惊厥药和催眠药。