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1. 发明授权

US4076703A Dipeptide derivatives and their production 失效
标题翻译：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。

2. 发明授权

US4076704A Dipeptide derivatives and their production 失效
标题翻译：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。

3. 发明授权

US4076705A Dipeptide derivatives and their production 失效
标题翻译：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。

4. 发明授权

US4240957A Dipeptide derivatives and their production 失效
标题翻译：二肽衍生物及其生产
公开(公告)号：US4240957A
公开(公告)日：1980-12-23
申请号：US775646
申请日：1977-03-07
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 , C07D233/90 , 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。

5. 发明授权

US4154727A Dipeptide derivatives and their production 失效
标题翻译：二肽衍生物及其生产
公开(公告)号：US4154727A
公开(公告)日：1979-05-15
申请号：US867605
申请日：1978-01-06
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 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.
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，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。

6. 发明授权

US4076702A Dipeptide derivatives and their production 失效
标题翻译：二肽衍生物及其生产
公开(公告)号：US4076702A
公开(公告)日：1978-02-28
申请号：US716265
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 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.
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，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。

7. 发明授权

US4143048A Process for producing triazolylbenzophenone derivatives 失效
标题翻译：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.

8. 发明授权

US4147700A Triazolylbenzophenone derivatives and production thereof 失效
标题翻译：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。

9. 再颁专利

USRE37314E1 Pyrimidine derivatives 有权
标题翻译：嘧啶衍生物
公开(公告)号：USRE37314E1
公开(公告)日：2001-08-07
申请号：US09141731
申请日：1998-08-27
申请人： Kentaro Hirai , Teruyuki Ishiba , Haruo Koike , Masamichi Watanabe
发明人： Kentaro Hirai , Teruyuki Ishiba , Haruo Koike , Masamichi Watanabe
IPC分类号： A61K31505
CPC分类号： C07D239/42 , C07D239/34 , C07D239/38
摘要： The compounds of the present invention inhibit the HMG-CoA reductase, and subsequently suppress the biosynthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.
摘要翻译：本发明的化合物抑制HMG-CoA还原酶，并且随后抑制胆固醇的生物合成。它们可用于治疗高胆固醇血症，高脂蛋白血症和动脉粥样硬化。

10. 发明授权

US4564623A Aminoalkylbenzene derivatives 失效
标题翻译：氨基烷基苯衍生物
公开(公告)号：US4564623A
公开(公告)日：1986-01-14
申请号：US573685
申请日：1984-01-25
申请人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
发明人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doteuchi , Koichi Otani
IPC分类号： C07D295/18 , A61K31/16 , A61K31/165 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/4245 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/455 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07C67/00 , C07C231/00 , C07C233/18 , C07C233/20 , C07C233/22 , C07C233/60 , C07C233/69 , C07C235/20 , C07C235/48 , C07C235/72 , C07C237/08 , C07C237/32 , C07C237/42 , C07C239/00 , C07C261/04 , C07C301/00 , C07C311/18 , C07C313/00 , C07C323/29 , C07C323/39 , C07C323/41 , C07C325/00 , C07C327/40 , C07C327/46 , C07C327/48 , C07C327/50 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D249/10 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/08 , C07D295/096 , C07D295/14 , C07D295/15 , C07D307/68 , C07D333/38 , C07D335/06 , C07D498/04 , C07D207/04
CPC分类号： C07D213/81 , C07C323/29 , C07D207/16 , C07D207/28 , C07D213/82 , C07D257/04 , C07D261/18 , C07D271/06 , C07D295/096 , C07D295/15 , C07D333/38 , C07D335/06 , Y10S514/927
摘要： An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;Y is oxo, thioxo, or cyanoimino;a is an integer of 1 to 3;b is an integer of 0 to 3;c is an integer of 1 to 4;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl; orR.sup.1 and R.sup.2 taken together represent pyrrolidinyl;R is hydrogen, cycloaklkyl, trihaloalkyl, alkoxy, dialkylamino, aryl, aroyl, heterocyclic group, or a group of the formula: ##STR2## (wherein R.sup.3 is hydrogen, halogen, amino, alkyl, alkylamino, dialkylamino, alkylthio, or aryloxy;R.sup.4 is hydrogen, alkyl, alkenyl, aryl, or heterocyclic group; orR.sup.3 and R.sup.4 taken together represent alkylidene or aralkylidene);with the proviso that the above aryl, aroyl, and heterocyclic group can be substituted by 1 to 3 substituents] and its pharmaceutically acceptable acid addition salts being useful as histamine H.sub.2 blockers, especially peptic ulcer remedies, are provided via several routes.

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