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    • 7. 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。