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。

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。

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。

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。

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。

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。

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.

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。

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。

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.