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    • 1. 发明授权
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4076703A
    • 1978-02-28
    • US716266
    • 1976-08-20
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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.
    • 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。
    • 3. 发明授权
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4076704A
    • 1978-02-28
    • US716267
    • 1976-08-20
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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.
    • 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。
    • 5. 发明授权
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4076705A
    • 1978-02-28
    • US716268
    • 1976-08-20
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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.
    • 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。
    • 6. 发明授权
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4240957A
    • 1980-12-23
    • US775646
    • 1977-03-07
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07D233/90C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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.
    • 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。
    • 7. 发明授权
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4154727A
    • 1979-05-15
    • US867605
    • 1978-01-06
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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 form 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 each 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.
    • 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,R1和R2任选地结合形成C 2 -C 4亚烷基,基团可以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,吗啉代或哌嗪基,各自被 C1-C6烷基或苯基 A环表示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 抗焦虑药,镇静剂,抗惊厥药,催眠药,肌肉松弛剂或其合成中间体。
    • 8. 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
    • Dipeptide derivatives and their production
    • 二肽衍生物及其生产
    • US4076702A
    • 1978-02-28
    • US716265
    • 1976-08-20
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • Kentaro HiraiTeruyuki IshibaKazuyuki SasakuraHirohiko Sugimoto
    • A61K38/00C07K5/06C07K5/065C07K5/10C07C103/52
    • C07K5/1027C07K5/06026C07K5/06078C07K5/06191A61K38/00Y02P20/55
    • 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 R.sup.2 --N--R.sup.3 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.
    • 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,基团R 2 -N-R 3任选表示苯二酰亚胺基,哌啶子基,4-羟基-4-(对卤代苯基)哌啶子基,吗啉代或被C1取代的哌嗪基 -C 1-6烷基或苯基, 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, 制备镇静剂,抗惊厥药,催眠药,肌肉松弛剂或其合成中间体。