专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4159374A Triazolylphenyl ketone derivatives and production thereof 失效
标题翻译：三唑基苯基酮衍生物及其制备
公开(公告)号：US4159374A
公开(公告)日：1979-06-26
申请号：US803303
申请日：1977-06-03
申请人： Kentaro Hirai , Hirohiko Sugimoto
发明人： Kentaro Hirai , Hirohiko Sugimoto
IPC分类号： A61K31/41 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , C07D249/08 , C07D249/10 , C07D249/14 , C07D401/06 , C07D403/06 , C07D403/12 , C07D413/06 , C07D401/10
CPC分类号： C07C251/72 , C07D249/10 , Y10S514/906
摘要： Triazolyl ketone derivatives of the formula: ##STR1## (wherein R represents lower alkoxy or the group ##STR2## R.sup.4 and R.sup.5 each represents hydrogen, lower alkyl, ##STR3## represents hetero ring selected from pyrrolidino, piperidino, and morpholino; R.sup.1 represents halogen or nitro; R.sup.2 represents hydrogen or lower alkyl; R.sup.3 represents lower alkyl, phenyl, or the group ##STR4## R.sup.6 represents hydrogen, lower alkyl, or benzyl; R.sup.7 and R.sup.8 each represents hydrogen, lower alkyl, or ##STR5## represents hetero ring selected from pyrrolidino, piperidino, and morpholino; and Ar represents phenyl, o-halogenophenyl, or 2-pyridyl) and their pharmaceutically acceptable acid addition salts, being useful as anxiolytics, hypnotics, anticonvulsants, muscle relaxants, or their synthetic intermediates, are prepared by several routes.
摘要翻译：下式的三唑基酮衍生物（其中R表示低级烷氧基或基团R 4和R 5各自表示氢，低级烷基，表示选自吡咯烷子基，哌啶子基和吗啉代的杂环; R 1表示卤素或硝基; R 2表示氢或低级烷基; R 3表示低级烷基，苯基或基团R 6表示氢，低级烷基或苄基; R 7和R 8各自表示氢，低级烷基或者表示杂环选自吡咯烷子基，哌啶子基和吗啉代; Ar表示苯基，邻 - 卤代苯基或2-吡啶基）及其药学上可接受的酸加成盐，可用作抗焦虑剂，催眠药，抗惊厥药，肌肉松弛剂或其合成中间体通过几条路线。

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

US5326780A Imidazole derivatives having anti-HIV activity 失效
标题翻译：具有抗HIV活性的咪唑衍生物
公开(公告)号：US5326780A
公开(公告)日：1994-07-05
申请号：US3126
申请日：1993-01-12
申请人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
发明人： Hirohiko Sugimoto , Masaru Ogata , Hiroshi Matsumoto , Ken-ichi Sugita , Akihiko Sato , Tamio Fujiwara
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61P31/12 , C07D233/54 , C07D233/60 , C07D233/64 , C07D233/70 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D233/66
CPC分类号： C07D233/56 , C07D233/64 , C07D233/80 , C07D233/84 , C07D233/86 , C07D233/90 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： A novel imidazole derivatives of formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, or optionally substituted aryl; R.sup.2 is alkyl, optionally substituted aryl optionally substituted aralkyl, or optionally substituted hetero ring group; R.sup.3 is hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted hydroxyalkyl; R.sup.4 is hydrogen, alkyl, halogen, acyl, optionally substituted hydroxyalkyl, optionally esterified or amidated carboxyl group, hydroxy group, aryl or arylthio; X is S, SO, SO.sub.2, CH.sub.2, or Se; n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, said derivative having anti-HIV activity and being useful for the treatment of HIV infections.
摘要翻译：式I的新型咪唑衍生物：其中R 1是氢，烷基，卤素或任选取代的芳基; R 2是烷基，任选取代的芳基任选取代的芳烷基或任选取代的杂环基团; R 3是氢，烷基，任选取代的芳基，任选取代的芳烷基或任选取代的羟烷基; R 4为氢，烷基，卤素，酰基，任选取代的羟基烷基，任选酯化或酰胺化的羧基，羟基，芳基或芳硫基; X是S，SO，SO 2，CH 2或Se; n为1〜3的整数，或其药学上可接受的盐，所述衍生物具有抗HIV活性，可用于治疗HIV感染。

4. 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.

5. 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。

6. 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。

7. 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。

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. 发明授权

US5910506A Imidazole derivatives as anti-HIV agents 失效
标题翻译：咪唑衍生物作为抗HIV剂
公开(公告)号：US5910506A
公开(公告)日：1999-06-08
申请号：US809624
申请日：1997-05-30
申请人： Hirohiko Sugimoto , Tamio Fujiwara
发明人： Hirohiko Sugimoto , Tamio Fujiwara
IPC分类号： A61K31/4164 , A61K31/4178 , A61P31/18 , C07D233/54 , C07D233/58 , C07D233/60 , C07D233/64 , C07D233/84 , C07D401/04 , C07D401/06 , C07D409/04 , A01N43/50 , C07D233/28 , C07D233/40
CPC分类号： C07D233/56 , C07D233/64 , C07D233/84 , C07D401/04 , C07D401/06 , C07D409/04
摘要： An imidazole derivative represented by general formula (I) or a salt thereof, having the effect of specifically inhibiting the growth of HIV as a pathogenic virus and being reduced in toxicity. In said formula R.sup.1 represents hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.7 alkenyl, C.sub.4 -C.sub.12 cycloalkylalkyl, etc.; R.sup.2 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 acyl, hydroxyiminomethyl, hydrazonomethyl or --(CH.sub.2)n--R.sup.4 (R.sup.4 being halogeno, alkoxy, hydroxy, etc.; and n being an integer of 1 to 3); R.sup.3 represents substituted or unsubstituted C.sub.1 -C.sub.6 alkyl; X and Y represent each independently hydrogen, C.sub.1 -C.sub.3 alkyl, halogeno, or nitro; and Z represents S, SO, SO.sub.2 or CH.sub.2. ##STR1##
摘要翻译： PCT No.PCT / JP95 / 01936 Sec。 371日期1997年5月30日 102（e）日期1997年5月30日PCT提交1995年9月25日PCT公布。 WO96 / 10019 PCT出版物日期：1996年5月4日由通式（I）表示的咪唑衍生物或其盐，具有特异性抑制作为致病病毒的HIV生长且毒性降低的作用。在所述式中，R 1表示氢，C 1 -C 20烷基，C 2 -C 7烯基，C 4 -C 12环烷基烷基等; R 2表示C 1 -C 6烷基，C 1 -C 6酰基，羟基亚氨基甲基，亚肼基甲基或 - （CH 2）n -R 4（R 4为卤代，烷氧基，羟基等; n为1至3的整数）。 R 3表示取代或未取代的C 1 -C 6烷基; X和Y各自独立地表示氢，C1-C3烷基，卤代或硝基; Z表示S，SO，SO 2或CH 2。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式