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    Process for producing triazolylbenzophenone derivatives
    1.
    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
    2.
    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
    4.
    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。

    Dipeptide derivatives and their production
    8.
    发明授权
    Dipeptide derivatives and their production 失效
    二肽衍生物及其生产

    公开(公告)号：US4076704A

    公开(公告)日：1978-02-28

    申请号：US716267

    申请日：1976-08-20

    申请人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/10 ,  C07C103/52

    CPC分类号： C07K5/1027 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55

    摘要： Dipeptide derivatives represented by the formula: ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.7 alkenyl group, C.sub.2 -C.sub.7 cyanoalkyl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.3 -C.sub.10 dialkylaminoalkyl group or cyclopropylmethyl group, R.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.7 -C.sub.14 hydroxyaralkyl group, C.sub.6 -C.sub.12 aryl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.2 -C.sub.7 carboxyalkyl group, C.sub.1 -C.sub.6 aminoalkyl group, C.sub.4 -C.sub.10 guanidylalkyl group, C.sub.1 -C.sub.6 mercaptoalkyl group, C.sub.2 -C.sub.7 alkylthioalkyl group, C.sub.9 -C.sub.15 indolylalkyl group or C.sub.4 -C.sub.9 imidazolylalkyl group, R.sup.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.6 -C.sub.12 aryl group, glycyl group or glycyl-glycyl group, R.sup.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl group or amino-protecting group, R.sup.1 and R.sup.2 optionally combine to from C.sub.2 -C.sub.4 alkylene group, group ##STR2## optionally represents phthalimido group, piperidino group, 4-hydroxy-4-(p-halogenophenyl)piperidino, morpholino, or piperazino group substituted by C.sub.1 -C.sub.6 alkyl group or phenyl group, A ring represents benzene ring or pyridine ring optionally substituted by halogen and B ring represents benzene ring or thiophene ring optionally substituted by halogen, trifluoromethyl group, methylsulfonyl group, nitro group or C.sub.1 -C.sub.6 alkyl group and their acid addition salts, being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, muscle relaxants, or their synthetic intermediates, are prepared.

    摘要翻译： 由下式表示的二肽衍生物：其中R表示氢，C1-C6烷基，C2-C7链烯基，C2-C7氰基烷基，C2-C7氨基甲酰基烷基，C3-C10二烷基氨基烷基或环丙基甲基，R1表示氢，C1-C6烷基 基团，C 7 -C 14芳烷基，C 7 -C 14羟基烷基，C 6 -C 12芳基，C 2 -C 7氨基甲酰基烷基，C 2 -C 7羧基烷基，C 1 -C 6氨基烷基，C 4 -C 10冠酰基烷基，C 1 -C 6巯基烷基，C 2 -C 7烷硫基烷基，C 9 -C 15吲哚基 基团或C 4 -C 9咪唑基烷基，R 2表示氢，C 1 -C 6烷基，C 7 -C 14芳烷基，C 6 -C 12芳基，甘氨酰基或甘氨酰 - 甘氨酰基，R 3表示氢，C 1 -C 6烷基或氨基保护基，R 1和 R2任选地与C 2 -C 4亚烷基相结合，基团“任选地表示被C 1 -C 6烷基或苯基取代的邻苯二甲酰亚氨基，哌啶子基，4-羟基-4-（对卤代苯基）哌啶子基，吗啉代或哌嗪基， 一个rin g表示任选被卤素取代的苯环或吡啶环，B环表示任选被卤素，三氟甲基，甲基磺酰基，硝基或C 1 -C 6烷基取代的苯环或噻吩环及其酸加成盐，可用作抗焦虑剂，镇静剂 ，抗惊厥药，催眠药，肌肉松弛剂或其合成中间体。

    Dipeptide derivatives and their production
    9.
    发明授权
    Dipeptide derivatives and their production 失效
    二肽衍生物及其生产

    公开(公告)号：US4076703A

    公开(公告)日：1978-02-28

    申请号：US716266

    申请日：1976-08-20

    申请人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/10 ,  C07C103/52

    CPC分类号： C07K5/1027 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55

    摘要： Dipeptide derivatives represented by the formula: ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.7 alkenyl group, C.sub.2 -C.sub.7 cyanoalkyl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.3 -C.sub.10 dialkylaminoalkyl group or cyclopropylmethyl group, R.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.7 -C.sub.14 hydroxyaralkyl group, C.sub.6 -C.sub.12 aryl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.2 -C.sub.7 carboxyalkyl group, C.sub.1 -C.sub.6 aminoalkyl group, C.sub.4 -C.sub.10 guanidylalkyl group, C.sub.1 -C.sub.6 mercaptoalkyl group, C.sub.2 -C.sub.7 alkylthioalkyl group, C.sub.9 -C.sub.15 indolylalkyl group or C.sub.4 -C.sub.9 imidazolylalkyl group, R.sup.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.6 -C.sub.12 aryl group, glycyl group or glycyl-glycyl group, R.sup.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl group or amino-protecting group, R.sup.1 and R.sup.2 optionally combine to from C.sub.2 -C.sub.4 alkylene group, ##STR2## optionally represents phthalimido group, piperidino group, 4-hydroxy-4-(p-halogenophenyl)piperidino, morpholino, or piperazino group substituted by C.sub.1 -C.sub.6 alkyl group or phenyl group, A ring represents benzene ring or pyridine ring optionally substituted by halogen and B ring represents benzene ring or thiophene ring optionally substituted by halogen, trifluoromethyl group, methylsulfonyl group, nitro group or C.sub.1 -C.sub.6 alkyl group and their acid addition salts, being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, muscle relaxants, or their synthetic intermediates, are prepared.

    摘要翻译： 由下式表示的二肽衍生物：其中R表示氢，C1-C6烷基，C2-C7链烯基，C2-C7氰基烷基，C2-C7氨基甲酰基烷基，C3-C10二烷基氨基烷基或环丙基甲基，R1表示氢，C1-C6烷基 基团，C 7 -C 14芳烷基，C 7 -C 14羟基烷基，C 6 -C 12芳基，C 2 -C 7氨基甲酰基烷基，C 2 -C 7羧基烷基，C 1 -C 6氨基烷基，C 4 -C 10冠酰基烷基，C 1 -C 6巯基烷基，C 2 -C 7烷硫基烷基，C 9 -C 15吲哚基 基团或C 4 -C 9咪唑基烷基，R 2表示氢，C 1 -C 6烷基，C 7 -C 14芳烷基，C 6 -C 12芳基，甘氨酰基或甘氨酰 - 甘氨酰基，R 3表示氢，C 1 -C 6烷基或氨基保护基，R 1和 R2任选地与C 2 -C 4亚烷基结合，可任选地表示被C 1 -C 6烷基或苯基取代的邻苯二甲酰亚氨基，哌啶子基，4-羟基-4-（对卤代苯基）哌啶子基，吗啉代或哌嗪基， 戒指代表 苯环或任选被卤素取代的吡啶环，B环表示任选被卤素，三氟甲基，甲基磺酰基，硝基或C 1 -C 6烷基取代的苯环或噻吩环及其酸加成盐，可用作抗焦虑剂，镇静剂， 抗惊厥药，催眠药，肌肉松弛剂或其合成中间体。

    Dipeptide derivatives and their production
    10.
    发明授权
    Dipeptide derivatives and their production 失效
    二肽衍生物及其生产

    公开(公告)号：US4076705A

    公开(公告)日：1978-02-28

    申请号：US716268

    申请日：1976-08-20

    申请人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    发明人： Kentaro Hirai ,  Teruyuki Ishiba ,  Kazuyuki Sasakura ,  Hirohiko Sugimoto

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/10 ,  C07C103/52

    CPC分类号： C07K5/1027 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55

    摘要： Dipeptide derivatives represented by the formula: ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.7 alkenyl group, C.sub.2 -C.sub.7 cyanoalkyl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.3 -C.sub.10 dialkylaminoalkyl group or cyclopropylmethyl group, R.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.7 -C.sub.14 hydroxyaralkyl group, C.sub.6 -C.sub.12 aryl group, C.sub.2 -C.sub.7 carbamoylalkyl group, C.sub.2 -C.sub.7 carboxyalkyl group, C.sub.1 -C.sub.6 aminoalkyl group, C.sub.4 -C.sub.10 guanidylalkyl group, C.sub.1 -C.sub.6 mercaptoalkyl group, C.sub.2 -C.sub.7 alkylthioalkyl group, C.sub.9 -C.sub.15 indolylalkyl group or C.sub.4 -C.sub.9 imidazolylalkyl group, R.sup.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl group, C.sub.7 -C.sub.14 aralkyl group, C.sub.6 -C.sub.12 aryl group, glycyl group or glycyl-glycyl group, R.sup.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl group or amino-protecting group, R.sup.1 and R.sup.2 optionally combine to from C.sub.2 -C.sub.4 alkylene group, ##STR2## optionally represents phthalimido group, piperidino group, 4-hydroxy-4-(p-halogenophenyl)piperidino, morpholino, or piperazino group substituted by C.sub.1 -C.sub.6 alkyl group or phenyl group, A ring represents benzene ring or pyridine ring optionally substituted by halogen and B ring represents benzene ring or thiophene ring optionally substituted by halogen, trifluoromethyl group, methylsulfonyl group, nitro group or C.sub.1 -C.sub.6 alkyl group and their acid addition salts, being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, muscle relaxants, or their synthetic intermediates, are prepared.

    摘要翻译： 由下式表示的二肽衍生物：其中R表示氢，C1-C6烷基，C2-C7链烯基，C2-C7氰基烷基，C2-C7氨基甲酰基烷基，C3-C10二烷基氨基烷基或环丙基甲基，R1表示氢，C1- C 6烷基，C 7 -C 14芳烷基，C 7 -C 14羟基烷基，C 6 -C 12芳基，C 2 -C 7氨基甲酰基烷基，C 2 -C 7羧基烷基，C 1 -C 6氨基烷基，C 4 -C 10冠酰基烷基，C 1 -C 6巯基烷基，C 2 -C 7烷硫基烷基， C 9 -C 15吲哚基烷基或C 4 -C 9咪唑基烷基，R 2表示氢，C 1 -C 6烷基，C 7 -C 14芳烷基，C 6 -C 12芳基，甘氨酰基或甘氨酰 - 甘氨酰基，R 3表示氢，C 1 -C 6烷基或氨基保护 基团，R 1和R 2任选地与C 2 -C 4亚烷基相结合，可任选地代表邻苯二甲酰亚氨基，哌啶子基，4-羟基-4-（对卤代苯基）哌啶子基，吗啉代或被C 1 -C 6烷基取代的哌嗪基 或苯基，A环 表示任选被卤素取代的苯环或吡啶环，B环表示任选被卤素，三氟甲基，甲基磺酰基，硝基或C 1 -C 6烷基取代的苯环或噻吩环及其酸加成盐，可用作抗焦虑剂，镇静剂， 抗惊厥药，催眠药，肌肉松弛剂或其合成中间体。