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    • 4. 发明授权
    • Triazolylbenzophenone derivatives and production thereof
    • 三唑基二苯甲酮衍生物及其制备
    • US4147700A
    • 1979-04-03
    • US861011
    • 1977-12-15
    • Kentaro HiraiToshio FujishitaTeruyuki IshibaHirohiko Sugimoto
    • Kentaro HiraiToshio FujishitaTeruyuki IshibaHirohiko Sugimoto
    • A61K38/00C07D239/86C07D239/92C07D249/08C07K5/06C07K5/065C07D249/14
    • C07D239/86C07D239/92C07D249/08C07K5/06026C07K5/06078A61K38/00Y10S514/906
    • 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.
    • 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。
    • 9. 发明授权
    • Process for producing triazolylbenzophenone derivatives
    • 制备三唑基二苯甲酮衍生物的方法
    • US4141901A
    • 1979-02-27
    • US861010
    • 1977-12-15
    • Kentato HiraiToshio FujishitaTeruyuki IshibaHiroshiko Sugimoto
    • Kentato HiraiToshio FujishitaTeruyuki IshibaHiroshiko Sugimoto
    • A61K38/00C07D239/86C07D239/92C07D249/08C07K5/06C07K5/065C07D249/14
    • C07D239/86C07D239/92C07D249/08C07K5/06026C07K5/06078A61K38/00Y10S514/906
    • 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.
    • 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。