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1. 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.

2. 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。

3. 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。

4. 发明授权

US4482566A Substituted aminoalkylbenzene type lower acylamides 失效
标题翻译：取代氨基烷基苯型低级酰基酰胺
公开(公告)号：US4482566A
公开(公告)日：1984-11-13
申请号：US277161
申请日：1981-06-25
申请人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doeteuchi , Koichi Otani
发明人： Kentaro Hirai , Teruyuki Ishiba , Shigeru Matsutani , Itsuo Makino , Toshio Fujishita , Masami Doeteuchi , 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 , A61K31/135 , C07C103/34 , C07C103/37
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.

5. 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。

6. 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

7. 发明授权

US4374842A 4,1-Benzoxazepines and compositions 失效
标题翻译： 4,1-苯并氧氮杂和组合物
公开(公告)号：US4374842A
公开(公告)日：1983-02-22
申请号：US250299
申请日：1981-04-02
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 , C07D498/14
CPC分类号： C07D267/14
摘要： 4,1-Benzoxazepines of the following formula are central nervous system drugs: ##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-苯并氧氮杂是中枢神经系统药物：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; 并且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不为苯基或2-卤代苯基）。

8. 发明授权

US4297280A 4,1-Benzoxazepines 失效
标题翻译： 4,1-苯并氧氮杂
公开(公告)号：US4297280A
公开(公告)日：1981-10-27
申请号：US91814
申请日：1979-11-06
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。

9. 发明授权

US4231930A 1-Substituted thiomethyltriazolobenzodiazepines 失效
标题翻译： 1-取代的硫代甲基三唑并苯并二氮杂卓
公开(公告)号：US4231930A
公开(公告)日：1980-11-04
申请号：US16615
申请日：1979-03-01
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.
摘要翻译：下式的化合物：其中R是氢，2-5C烷氧基羰基，1-7C酰基，1-4C烷硫基，7-10C苯基烷硫基，苯硫基，卤代苯硫基，二取代氨基硫代，＆lt; IMAGE＆gt; + TR＆lt; IMAGE > R1是氢或卤素; R2是卤素或硝基; 及其药学上可接受的酸加成盐。其化合物和盐可用作精神药物和抗焦虑剂，抗惊厥药和催眠药。

10. 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.

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