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1. 发明授权

US08835461B2 Substituted 3-hydroxy-4-pyridone derivative 有权
标题翻译：取代的3-羟基-4-吡啶酮衍生物
公开(公告)号：US08835461B2
公开(公告)日：2014-09-16
申请号：US13259956
申请日：2010-03-23
申请人： Toshio Fujishita , Minako Mikamiyama , Makoto Kawai , Toshiyuki Akiyama
发明人： Toshio Fujishita , Minako Mikamiyama , Makoto Kawai , Toshiyuki Akiyama
IPC分类号： A61K31/497 , A61K31/44 , A61K31/445 , C07D413/02 , C07D401/02 , C07D239/02 , C07D403/02 , C07D471/02 , C07D417/02 , C07D413/00 , C07D215/00 , C07D409/12
CPC分类号： C07D413/06 , A61K9/0019 , A61K9/1652 , A61K9/2054 , C07D213/80 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/08 , C07D405/10 , C07D409/06 , C07D409/08 , C07D409/10 , C07D409/14 , C07D413/08 , C07D413/14 , C07D417/06 , C07D417/08 , C07D417/14 , C07D471/04
摘要： This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
摘要翻译：本发明提供具有抗病毒活性的化合物，特别是抑制流感病毒的活性，更优选提供具有cap依赖性内切核酸酶抑制活性的取代的3-羟基-4-吡啶酮衍生物。

2. 发明授权

US4940714A 2-substituted carbonylimidazo[4,5-c]quinolines 失效
标题翻译： 2-取代的羰基咪唑并[4,5-c]喹啉
公开(公告)号：US4940714A
公开(公告)日：1990-07-10
申请号：US309868
申请日：1989-02-14
申请人： Susumu Takada , Toshio Fujishita , Takashi Sasatani , Akira Matsushita , Masami Eigyo
发明人： Susumu Takada , Toshio Fujishita , Takashi Sasatani , Akira Matsushita , Masami Eigyo
IPC分类号： A61K31/435 , A61K31/44 , A61P25/00 , A61P25/20 , A61P25/26 , C07D471/04
CPC分类号： C07D471/04
摘要： 2-Substituted carbonylimidazo[4,5-c]quinolines of formula: ##STR1## having a high affinity for benzodiazepin receptor and showing an excellent psychostimulating action orally at a dose of 0.1-500 mg are provided through several routes.
摘要翻译：通过几条途径提供2-取代的对苯并二氮杂受体具有高亲和力的式（I）的羰基咪唑并[4,5-c]喹啉，并以0.1-500mg的剂量口服显示极好的精神刺激作用。

3. 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.

4. 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。

5. 发明授权

US06809101B2 Compounds having anti-hepatitis C virus effect 失效
标题翻译：具有抗丙型肝炎病毒作用的化合物
公开(公告)号：US06809101B2
公开(公告)日：2004-10-26
申请号：US10362368
申请日：2003-02-27
申请人： Toshio Fujishita , Kenji Abe
发明人： Toshio Fujishita , Kenji Abe
IPC分类号： C07D27734
CPC分类号： A61K31/381 , A61K31/365 , A61K31/4162 , A61K31/421 , A61K31/426 , C07D277/34
摘要： It is found out that compounds represented by the formula (I): wherein R1 is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; and R2 and R3 taken together with the adjacent carbon atom form an optionally substituted heterocyclic group having one or more of oxo and/or thioxo; have an HCV RNA-dependent RNA synthase inhibitory effect.

6. 发明授权

US06716605B2 Indole derivatives having an antiviral activity 失效
标题翻译：具有抗病毒活性的吲哚衍生物
公开(公告)号：US06716605B2
公开(公告)日：2004-04-06
申请号：US10259903
申请日：2002-09-30
申请人： Toshio Fujishita , Tomokazu Yoshinaga
发明人： Toshio Fujishita , Tomokazu Yoshinaga
IPC分类号： C12N1509
CPC分类号： C07D403/06 , C07D209/12 , C07D209/18 , C07D209/20 , C07D209/22
摘要： A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralkyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR (R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.
摘要翻译：下式的化合物：其中R 1是氢，低级烷基或任选取代的芳基磺酰基等，R 2是氢，低级烷基或任选取代的芳烷基等，R 3，R R 5，R 5和R 6各自独立地为氢，卤素，三卤代低级烷基等，X为羟基或任选取代的氨基，Y为COOR（R为氢或酯残基）任选取代的芳基或任选取代的杂芳基具有整合酶抑制活性，并且可用作抗HIV药物。

7. 发明授权

US06506787B2 Indole derivatives having an antiviral activity 失效
标题翻译：具有抗病毒活性的吲哚衍生物
公开(公告)号：US06506787B2
公开(公告)日：2003-01-14
申请号：US09929486
申请日：2001-08-15
申请人： Toshio Fujishita , Tomokazu Yoshinaga
发明人： Toshio Fujishita , Tomokazu Yoshinaga
IPC分类号： A61K3132
CPC分类号： C07D403/06 , C07D209/12 , C07D209/18 , C07D209/20 , C07D209/22
摘要： A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralkyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR (R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.
摘要翻译：下式化合物：其中R 1是氢，低级烷基或任选取代的芳基磺酰基等，R 2是氢，低级烷基或任选取代的芳烷基等，R 3，R 4，R 5和R 6各自独立地是氢，卤素，三卤代低级烷基等，X是羟基或任选取代的氨基，Y是COOR（R是氢或酯残基），任选取代的芳基或任选取代的杂芳基，具有整合酶抑制活性，并且可用作一种抗艾滋病药物。

8. 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.

9. 发明授权

US4141901A Process for producing triazolylbenzophenone derivatives 失效
标题翻译：制备三唑基二苯甲酮衍生物的方法
公开(公告)号：US4141901A
公开(公告)日：1979-02-27
申请号：US861010
申请日：1977-12-15
申请人： Kentato Hirai , Toshio Fujishita , Teruyuki Ishiba , Hiroshiko Sugimoto
发明人： Kentato Hirai , Toshio Fujishita , Teruyuki Ishiba , Hiroshiko 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-C6 叠氮基 - 烷基，C 6 -C 10芳基，C 2 -C 8酰基或基团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，C 1 -C 6烷基，C 7 -C 10芳烷基或C 2 -C 11α-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 cid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。

10. 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。

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