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11. 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。

12. 发明授权

US4882338A Substituted isoquinoline derivatives and anti-ulcer agents 失效
标题翻译：取代的异喹啉衍生物和抗溃疡剂
公开(公告)号：US4882338A
公开(公告)日：1989-11-21
申请号：US68934
申请日：1987-07-01
申请人： Kentaro Hirai , Yukio Mizushima
发明人： Kentaro Hirai , Yukio Mizushima
IPC分类号： C07D217/16 , A61K31/47 , A61K31/472 , A61P1/04 , C07D217/26 , C07D401/12 , C07D405/14 , C07D491/04 , C07D491/056
CPC分类号： C07D401/12 , C07D405/14 , C07D491/04
摘要： A compound of the formula: ##STR1## (wherein R is hydrogen, hydroxy, methoxy, acetoxy, acetoxymethyl or trifluoromethyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each is hydrogen, hydroxy, optionally substituted C.sub.1 -C.sub.5 alkoxy, acetoxy, propynyloxy, allyloxy or benzyloxy; or R.sup.2 and R.sup.3 taken together form methylenedioxy;R.sup.5 is hydrogen, hydroxymethyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.5 acyloxymethyl or phthalidyl; and n is 0 or 1 except for the case in which R is methoxy and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each is hydrogen) or its pharmaceutically acceptable acid addition salt, being useful as anti-ulcer agents is provided through several routes.

13. 发明授权

US4341704A 4,1-Benzoxazepines and thia analogs thereof 失效
标题翻译： 4,1-苯并氧氮杂及其类似物
公开(公告)号：US4341704A
公开(公告)日：1982-07-27
申请号：US276632
申请日：1981-06-23
申请人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
发明人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
IPC分类号： A61K31/395 , A61K31/4196 , A61K31/55 , A61K31/553 , A61K31/554 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/22 , C07D249/08 , C07D249/10 , C07D267/14 , C07D273/00 , C07D281/10 , C07D285/36 , C07D498/04 , C07D513/04 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D267/14 , C07D273/00 , C07D285/36 , C07D513/04
摘要： 4,1-Benzoxazepines and thia analogs thereof of the formula: ##STR1## (wherein --A--B-- is the following group: ##STR2## (wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.3 alkyl, or C.sub.7 to C.sub.9 aralkyl;R.sup.2 is C.sub.1 to C.sub.3 alkyl or C.sub.1 to C.sub.3 .alpha.-aminoalkyl;R.sup.3 is C.sub.2 to C.sub.6 dialkylamino;R.sup.4 is C.sub.2 to C.sub.6 dialkylamino or C.sub.5 to C.sub.7 alkylpiperazino;R.sup.5 is C.sub.1 to C.sub.3 alkyl; andQ is oxygen or sulfur);D is oxygen or sulfur;X is halogen or nitro;Y is hydrogen or halogen; andZ is hydrogen, C.sub.1 to C.sub.3 alkoxy, or C.sub.3 to C.sub.9 dialkylaminoalkoxy;with the proviso that when --A--B-- is ##STR3## Z is not hydrogen.) useful as novel central nervous system drugs are prepared by various synthetic routes.
摘要翻译：（其中-AB-是下列基团：其中R 1是氢，C 1至C 3烷基或C 7至C 9芳烷基） ; R2是C1-C3烷基或C1-C3α-氨基烷基; R3是C2-C6二烷基氨基; R4是C2-C6二烷基氨基或C5-C7烷基哌嗪基; R5是C1-C3烷基; Q是氧或硫）; D 是氧或硫; X是卤素或硝基; Y是氢或卤素; Z是氢，C 1至C 3烷氧基或C 3至C 9二烷基氨基烷氧基;条件是当-AB-不是氢时。）作为新型中枢神经系统药物通过各种合成途径制备。

14. 发明授权

US4318858A Thioethylamide derivatives 失效
标题翻译：硫代乙酰胺衍生物
公开(公告)号：US4318858A
公开(公告)日：1982-03-09
申请号：US212222
申请日：1980-12-02
申请人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino , Masami Doteuchi , Koichi Otani
发明人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino , Masami Doteuchi , Koichi Otani
IPC分类号： C07D333/16 , A61K31/34 , A61K31/341 , A61P43/00 , C07D307/52 , C07D307/68 , C07D333/20 , C07D333/38 , C07D405/12 , C07D409/12 , C07D207/04 , C07D333/18
CPC分类号： C07D307/68 , C07D307/52 , C07D333/20 , C07D333/38 , Y10S514/927
摘要： A compound of the formula: ##STR1## [wherein R is dimethylamino or 1-pyrrolidinyl;R.sup.1 and R.sup.2 each is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl (optionally substituted by one member selected from the group consisting of cyano, C.sub.1 -C.sub.3 alkoxy, phenyl, and 5- or 6-membered heterocyclic group), C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.5 alkenyl (optionally substituted by one member selected from the group consisting of C.sub.1 -C.sub.3 alkoxy, phenyl, and phenoxy), C.sub.6 -C.sub.10 aryl (optionally substituted by one or two members selected from the group consisting of hydroxy, halogen, nitro, sulfamoyl, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkanoyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.3 alkanesulfonyl), or 5- or 6-membered heterocyclic group (optionally substituted by one member selected from the group consisting of oxo, halogen, C.sub.1 -C.sub.3 alkyl, and C.sub.1 -C.sub.3 alkoxy);and X is oxygen or sulfur]and its pharmaceutically acceptable acid addition salts is useful as histamine H.sub.2 blockers.
摘要翻译：下式的化合物：其中R是二甲基氨基或1-吡咯烷基; R1和R2各自为氢或C1-C3烷基; R 3是氢，C 1 -C 3烷基（任选地被选自氰基，C 1 -C 3烷氧基，苯基和5-或6-元杂环基中的一个取代），C 3 -C 6环烷基，C 2 -C 5烯基（任选地被选自C 1 -C 3烷氧基，苯基和苯氧基的一个取代基取代），C 6 -C 10芳基（任选被一个或两个选自羟基，卤素，硝基，氨磺酰基，C1- C 3烷基，C 1 -C 3烷氧基，C 1 -C 3烷酰基，C 2 -C 4烷氧基羰基，C 2 -C 4二烷基氨基和C 1 -C 3烷磺酰基）或5或6元杂环基（任选被一个选自的氧代，卤素，C 1 -C 3烷基和C 1 -C 3烷氧基）; 并且X是氧或硫]，其药学上可接受的酸加成盐可用作组胺H2阻断剂。

15. 发明授权

US4309433A Pyridinecarbonamido-oxy or thio loweralkyl-1-(diloweralkylaminoloweralkyl)benzene and derivatives thereof, compositions containing same and method of using same 失效
标题翻译：吡啶羰基酰氧基或硫代低级烷基-1-（二低烷基氨基低级烷基）苯及其衍生物，含有它们的组合物及其使用方法
公开(公告)号：US4309433A
公开(公告)日：1982-01-05
申请号：US164016
申请日：1980-06-30
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 , C07D213/56 , C07D401/10
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, cycloalkyl, 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.
摘要翻译：下式的氨基烷基苯衍生物：其中A是氧或硫; Y是氧代，硫代或氰基亚氨基; a为1〜3的整数， b为0〜3的整数; c为1〜4的整数， R1是烷基; R2是氢或烷基; 或者R 1和R 2一起代表吡咯烷基; R是氢，环烷基，三卤代烷基，烷氧基，二烷基氨基，芳基，芳酰基，杂环基或下式基团：其中R 3是氢，卤素，氨基，烷基，烷基氨基，二烷基氨基，烷硫基或芳氧基; R4是氢，烷基，烯基，芳基或杂环基;或R3和R4一起代表亚烷基或亚烷叉基;条件是上述芳基，芳酰基和杂环基可以被1至3个取代基取代] 作为组胺H2阻断剂，特别是消化性溃疡治疗剂可用的可接受的酸加成盐通过几种途径提供。

16. 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.

17. 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。

18. 发明授权

US4492794A 2-Guanidino-4-hydroxymethylthiazole and derivatives thereof 失效
标题翻译： 2-胍基-4-羟甲基噻唑及其衍生物
公开(公告)号：US4492794A
公开(公告)日：1985-01-08
申请号：US488821
申请日：1983-04-26
申请人： Kentaro Hirai
发明人： Kentaro Hirai
IPC分类号： C07D277/20 , C07D277/48 , C07D277/38
CPC分类号： C07D277/48
摘要： A compound of the formula: ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.5 alkanoyl or substituted sulfonyl, which is useful as a synthetic intermediate to 2-guanidino-4-[2-(formamido)ethylthiomethyl]thiazole, histamine H.sub.2 receptor antagonist.
摘要翻译：下式的化合物：其中R是氢，C 1 -C 5烷酰基或取代的磺酰基，其可用作2-胍基-4- [2-（甲酰氨基）乙硫基甲基]噻唑的合成中间体，组胺H 2受体拮抗剂。

19. 发明授权

US4476133A Triazolo-4,1-benzoxazepines having CNS activity 失效
标题翻译：具有中枢神经系统活性的三氮唑-4,1-苯并氧氮杂
公开(公告)号：US4476133A
公开(公告)日：1984-10-09
申请号：US397855
申请日：1982-07-13
申请人： Kentaro Hirai , Shigeru Matsutani , Itsuo Makino , Teruyuki Ishiba
发明人： Kentaro Hirai , Shigeru Matsutani , Itsuo Makino , Teruyuki Ishiba
IPC分类号： C07D267/14 , C07D498/04 , A61K31/55
CPC分类号： C07D267/14
摘要： 4,1-Benzoxazepines of the following formula are novel central nervous system: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl;X is hydrogen, halogen, or nitro;Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle;R.sup.2 is C.sub.1 to C.sub.5 alkyl;and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl;with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl)
摘要翻译：下式的4,1-苯并氧氮杂是新的中枢神经系统：其中R是氢或C1至C5烷基; X是氢，卤素或硝基; Y是苯基，2-卤代苯基，4-卤代苯基，2-三氟甲基苯基或吡啶基; 并且是下列基团：其中Q是氧，硫或亚肼基，条件是当Y是苯基或2-卤代苯基且R是氢时，Q是氧还不硫; R1是氢，卤素，C1至C5烷基，C1至C5烷硫基，5-或6-元杂环或被选自卤素，羟基，巯基，C1的取代基取代的C1至C5烷基 C 1-5烷酰氧基，C 1至C 5烷硫基，C 7至C 9芳烷基二硫代，C 2至C 10二烷基氨基，C 3至C 15二烷基氨基烷氧基，C 3至C 15二烷基氨基烷硫基以及5-或6-元杂环; R 2为C 1至C 5烷基; 且R 3为C 1至C 5烷基或C 3至C 10二烷基氨基烷基;条件是当R 1为C 1至C 5烷基且R为氢时，Y

20. 发明授权

US4264499A 1-Substituted thiomethyltriazolobenzodiazepines and production thereof 失效
标题翻译： 1-取代的硫代甲基三唑并二氮杂及其制备
公开(公告)号：US4264499A
公开(公告)日：1981-04-28
申请号：US110842
申请日：1980-01-10
申请人： Kentaro Hirai , Toshio Fujishita , Teruyuki Ishiba
发明人： Kentaro Hirai , Toshio Fujishita , Teruyuki Ishiba
IPC分类号： A61K31/55 , A61P21/02 , A61P25/08 , A61P25/20 , C07D249/08 , C07D487/04 , C07D519/00
CPC分类号： C07D249/08 , C07D487/04 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein R is hydrogen, 2-5C alkoxycarbonyl, 1-7C acyl, 1-4C alkylthio, 7-10C phenylalkylthio, phenylthio, halo-phenylthio, disubstituted aminothio, ##STR2## R.sup.1 is hydrogen or halogen; R.sup.2 is halogen or nitro;and its pharmaceutically acceptable acid addition salts.The compounds and salts thereof are useful as psychotropic agents and as anxiolytics, anticonvulsants and hypnotics.

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