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11. 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.

12. 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。

13. 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。

14. 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.

15. 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。

16. 发明申请

US20120022255A1 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：US20120022255A1
公开(公告)日：2012-01-26
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： C07D413/10 , C07D409/06 , C07D417/06 , C07D401/06 , C07D409/10 , C07D405/10 , C07D401/10 , C07D401/04 , C07D213/89 , C07D413/06 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D409/12 , C07D401/14 , C07D213/79
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。

17. 发明授权

US07662826B2 Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same 失效
标题翻译：吡唑并[1,5-a]嘧啶衍生物和含有它们的nad（p）h氧化酶抑制剂
公开(公告)号：US07662826B2
公开(公告)日：2010-02-16
申请号：US10511840
申请日：2003-04-18
申请人： Kaoru Seno , Koichi Nishi , Yoshiyuki Matsuo , Toshio Fujishita
发明人： Kaoru Seno , Koichi Nishi , Yoshiyuki Matsuo , Toshio Fujishita
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P27/02 , A61P29/00 , A61P43/00
CPC分类号： C07D519/00 , A61K31/519 , A61K31/5377 , C07D487/04
摘要： A compound represented by the formula (Ia) (wherein R1a, R2a, and R3 to R5 are the same as defined in the description), a prodrug thereof, a pharmaceutically acceptable salt thereof, or solvate thereof. The compounds are useful in the prevention of or treatment for diseases relating to NAD(P)H.
摘要翻译：由式（Ia）表示的化合物（其中R1a，R2a和R3至R5与说明书中定义相同），其前药，其药学上可接受的盐或其溶剂化物。该化合物可用于预防或治疗与NAD（P）H有关的疾病。

18. 发明申请

US20060089362A1 Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same 失效
标题翻译：吡唑并[1,5-a]嘧啶衍生物和含有它们的nad（p）h氧化酶抑制剂
公开(公告)号：US20060089362A1
公开(公告)日：2006-04-27
申请号：US10511840
申请日：2003-04-18
申请人： Kaoru Seno , Koichi Nishi , Yoshiyuki Matsuo , Toshio Fujishita
发明人： Kaoru Seno , Koichi Nishi , Yoshiyuki Matsuo , Toshio Fujishita
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D519/00 , A61K31/519 , A61K31/5377 , C07D487/04
摘要： A compound represented by the formula (Ia) (wherein R1a, R2a, and R3 to R5 are the same as defined in the description), a prodrug thereof, a pharmaceutically acceptable salt thereof, or solvate thereof. The compounds are useful in the prevention of or treatment for diseases relating to NAD(P)H.
摘要翻译：由式（Ia）表示的化合物（其中R1a，R2a和R3至R5与说明书中定义相同），其前药，其药学上可接受的盐或其溶剂化物。该化合物可用于预防或治疗与NAD（P）H相关的疾病。

19. 发明授权

US06620841B1 Aromatic heterocycle compounds having HIV integrase inhibiting activities 失效
标题翻译：具有HIV整合酶抑制活性的芳族杂环化合物
公开(公告)号：US06620841B1
公开(公告)日：2003-09-16
申请号：US09857632
申请日：2001-06-07
申请人： Toshio Fujishita , Tomokazu Yoshinaga , Akihiko Sato
发明人： Toshio Fujishita , Tomokazu Yoshinaga , Akihiko Sato
IPC分类号： A61K3134
CPC分类号： C07D403/06 , C07D333/24 , C07D333/34
摘要： A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.
摘要翻译：式（I）的化合物：其中X是羟基，保护的羟基或任选取代的氨基; Y是-COORA，其中RA是氢或酯残基，-CONRBRC，其中RB和RC各自独立地是氢或酰胺残基，任选取代的芳基或任选取代的杂芳基; 并且A 1是任选取代的杂芳基; 不包括其中Y和/或A 1为任选取代的吲哚-3-基的化合物，其互变异构体，前药，药学上可接受的盐或其水合物对整合酶具有抑制活性。

20. 发明授权

US4753951A Condensed imidazopyridine derivatives useful as psychotropic agents 失效
标题翻译：用作精神药物的缩合咪唑并吡啶衍生物
公开(公告)号：US4753951A
公开(公告)日：1988-06-28
申请号：US920162
申请日：1986-10-17
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： C07D471/04 , C07D495/14 , A61K31/47 , C07D471/14
CPC分类号： C07D471/04 , C07D495/14
摘要： A compound of the formula: ##STR1## (wherein R is phenyl optionally substituted by one or two members selected from the group consisting of trifluoromethyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, nitro, amino C.sub.1 -C.sub.5 alkanoylamino and C.sub.1 -C.sub.5 alkoxycarbonyl or 5- or 6-membered heterocyclic group optionally substituted by one or two members selected from the group consisting of halogen, C.sub.1 -C.sub.5 alkyl and C.sub.1 -C.sub.5 alkoxy,Q is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.10 acyl, C.sub.1 -C.sub.5 alkylsulfonyl or C.sub.6 -C.sub.10 arylsulfonyl, ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen, halogen C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.5 haloalkyl,Q is present on the nitrogen atom of the 1,3 or 5-position, and the dotted line indicates the presence of three double bonds at the position of 2, 3; 3a, 3b; 4, 5 / 1, 3b; 2, 3; 3a, 4 / or 1, 2; 3a, 3b; 4, 5)or its salt, being useful as psychostimulants or anxiolytics, is provided.
摘要翻译：下式的化合物：其中R是任选被一个或两个选自三氟甲基，C 1 -C 5烷基，C 1 -C 5烷氧基，C 1 -C 5烷硫基，硝基，氨基，任选被一个或两个选自卤素，C 1 -C 5烷基和C 1 -C 5烷氧基的成员取代的C 1 -C 5烷酰基氨基和C 1 -C 5烷氧基羰基或5或6元杂环基，Q是氢，C 1 -C 5 烷基，C 1 -C 10酰基，C 1 -C 5烷基磺酰基或C 6 -C 10芳基磺酰基，R 1，R 2，R 3和R 4各自为氢，卤素C 1 -C 5烷基，C 1 -C 5烷氧基或C 1 -C 5烷氧基， C5卤代烷基，Q存在于1,3或5位的氮原子上，虚线表示在2,3,3a，3b; 4,5 / 1,3b的位置存在三个双键 ; 2,3,3a，4 /或1,2; 3a，3b; 4,5）或其盐，可用作精神兴奋剂或抗焦虑剂。

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