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1. 发明授权

US06242445B1 Benzimidazole derivative 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US06242445B1
公开(公告)日：2001-06-05
申请号：US09622788
申请日：2000-08-23
申请人： Mikiro Yanaka , Shigeru Suzuki , Fuyuhiko Nishijima , Hiroshi Takahashi , Mikio Sugano , Hiroshi Maruoka , Toru Yamazaki , Toshikazu Dewa , Hiroyuki Enari , Michihito Ise
发明人： Mikiro Yanaka , Shigeru Suzuki , Fuyuhiko Nishijima , Hiroshi Takahashi , Mikio Sugano , Hiroshi Maruoka , Toru Yamazaki , Toshikazu Dewa , Hiroyuki Enari , Michihito Ise
IPC分类号： A61K315377
CPC分类号： C07D235/26 , C07D235/30
摘要： A novel benzimidazole derivative [specifically, for example, 2-ethoxy-1-[{4′-(2″-N,N-dimethylaminoethoxycarbonyl)phenyl}methyl]-1H-benzimidazole-6-carboxylic acid morpholide] represented by formula (I) and a salt thereof. The compound exhibits satisfactory curative effects for cardiac and nephric diseases, although having little action on blood-pressure.
摘要翻译：一种新的苯并咪唑衍生物[具体地，例如2-乙氧基-1 - [{4' - （2“ - N，N-二甲基氨基乙氧基羰基）苯基}甲基] -1H-苯并咪唑-6-羧酸吗啉代] （I）化合物及其盐。该化合物对心脏和肾脏疾病表现出令人满意的治疗效果，尽管对血压几乎没有作用。

2. 发明授权

US5863913A Aromatic compound and pharmaceutical composition 失效
标题翻译：芳香族化合物和药物组成
公开(公告)号：US5863913A
公开(公告)日：1999-01-26
申请号：US857206
申请日：1997-05-15
申请人： Mikiro Yanaka , Hiroyuki Enari , Toru Yamazaki , Hiroshi Maruoka , Toshikazu Dewa , Fuyuhiko Nishijima , Hiroshi Takahashi , Michihito Ise
发明人： Mikiro Yanaka , Hiroyuki Enari , Toru Yamazaki , Hiroshi Maruoka , Toshikazu Dewa , Fuyuhiko Nishijima , Hiroshi Takahashi , Michihito Ise
IPC分类号： C07D295/18 , A61K31/195 , A61K31/24 , A61K31/44 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07C229/38 , C07C233/54 , C07C237/42 , C07C243/22 , C07D213/72 , C07D213/89 , C07D295/192 , C07D411/06
CPC分类号： C07D295/192 , C07C237/42
摘要： An aromatic compound of the formula (I): ##STR1## specifically, for example, 3-��(4-carboxyphenyl)methyl!valeramido!-4-dimethylaminobenzoic acid 4'-methylpiperazide, or a salt thereof, and a pharmaceutical composition comprising said aromatic compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent which provides sufficiently effective alleviation of renal dysfunction without affecting blood pressure at a low blood concentration.
摘要翻译：式（I）的芳族化合物：其中特别是例如3 - [[（4-羧基苯基）甲基]戊酰氨基] -4-二甲基氨基苯甲酸4'-甲基哌嗪或其盐，和包含所述芳族化合物或其药学上可接受的盐的药物组合物，以及药学上可接受的载体或稀释剂，其提供足够有效的肾功能障碍减轻而不影响低血药浓度的血压。

3. 发明授权

US06211175B1 Cardiac diseases improving method 失效
标题翻译：心脏疾病改善方法
公开(公告)号：US06211175B1
公开(公告)日：2001-04-03
申请号：US09166759
申请日：1998-10-06
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Mikio Sugano , Hiroshi Takahashi , Shigeru Suzuki , Hiroyuki Enari , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Mikio Sugano , Hiroshi Takahashi , Shigeru Suzuki , Hiroyuki Enari , Michihito Ise
IPC分类号： A61K31495
CPC分类号： C07D213/79 , C07D207/16 , C07D257/04 , C07D295/192
摘要： This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly, this invention relates to cardiac diseases improving agents composed of effective ingredients of aromatic compounds or pharmacologically acceptable salts thereof shown by below mentioned general formula. Chemical formula 1 [General formula (I)] (wherein, substituents thereof typically include, R1, R4, R13 representing hydrogen atom, an alkyl group, a haloalkyl group and so forth, R8 representing —CO—, —SO2— or single bond, R2 representing a 3-7 membered aliphatic cyclic amino group having at least one nitrogen atom, R7 representing —CO—or —SO2—, and R12 representing N-substituted valeramido group.)
摘要翻译：本发明涉及对参与低血压作用的血管紧张素II的1型受体基本上没有拮抗作用的心脏病改善剂。特别地，本发明涉及由下述通式所示的芳族化合物或其药理学上可接受的盐的有效成分组成的心脏病改善剂。化学式1 [通式（I）]（其中，取代基通常包括R1，R4 R 13表示氢原子，烷基，卤代烷基等，R 8表示-CO - ， - SO 2 - 或单键，R 2表示具有至少一个氮原子的3-7元脂肪族环状氨基，R 7表示 -CO-或-SO 2 - ，R 12表示N-取代的戊酰氨基）

4. 发明授权

US5932575A Cardiac diseases improving agents 失效
标题翻译：心脏疾病改善剂
公开(公告)号：US5932575A
公开(公告)日：1999-08-03
申请号：US991411
申请日：1997-12-16
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Mikio Sugano , Hiroshi Takahashi , Shigeru Suzuki , Hiroyuki Enari , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Mikio Sugano , Hiroshi Takahashi , Shigeru Suzuki , Hiroyuki Enari , Michihito Ise
IPC分类号： C07D295/18 , A61K31/40 , A61K31/44 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D207/16 , C07D207/24 , C07D213/79 , C07D257/04 , C07D295/192 , A61K31/445
CPC分类号： C07D213/79 , C07D207/16 , C07D257/04 , C07D295/192
摘要： This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly, this invention relates to cardiac diseases improving agents composed of effective ingredients of aromatic compounds or pharmacologically acceptable salts thereof shown by below mentioned general formula. ##STR1## (wherein, substituents thereof typically include, R.sup.1, R.sup.4, R.sup.13 representing hydrogen atom, an alkyl group, a haloalkyl group and so forth, R.sup.8 representing --CO--, --SO.sub.2 -- or single bond, R.sup.2 representing a 3-7 membered aliphatic cyclic amino group having at least one nitrogen atom, R.sup.7 representing --CO-- or --SO.sub.2 --, and R.sup.12 representing N-substituted valeramido group.)
摘要翻译：本发明涉及对参与低血压作用的血管紧张素II的1型受体基本上没有拮抗作用的心脏病改善剂。特别地，本发明涉及由下述通式所示的芳族化合物的有效成分或其药理学上可接受的盐组成的心脏病改善剂。（其中，取代基通常包括代表氢原子，烷基，卤代烷基等的R 1，R 4，R 13，R 8表示-CO - ， - SO 2 - 或单键，R 2表示3-7元脂肪族环状具有至少一个氮原子的氨基，R 7表示-CO-或-SO 2 - ，R 12表示N-取代的戊酰氨基。

5. 发明授权

US5696118A Benzene derivatives and pharmaceutical composition 失效
标题翻译：苯衍生物和药物组成
公开(公告)号：US5696118A
公开(公告)日：1997-12-09
申请号：US457147
申请日：1995-06-01
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
IPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26 , A61K31/445 , A61K31/535
CPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26
摘要： A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH; R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, or --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.
摘要翻译：式（I）的苯衍生物：其中R 1是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NH 2，-NHR 21; R2是羟基，-OR22，任选地被一个或多个氮，氧或硫原子间隔的三至七元饱和脂环族氨基，-NHR 23，-N（R 24）2，-NH 2; R 4是氢，C 1-6 - 烷基或-C（= O）R 25; R 7是-CO - ， - SO 2 - ; R8是-CO-，单键; R12为-R11-R5; R 11是-N（R 5） - ， - NH - ， - O - ， - N（R 26） - ， - N（C（= O）R 27） - ， - N（C（= O）NH 2）（C（= O）NHR 28） - ; R 13是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NHC（= O）（CH 2）m C 6 H 5，-NHC（= O）R 29，-NHC（= O）CH（C 6 H 5）2，-NH 2， -NHR 30， - （CH 2）n C 6 H 5; Z是C，CH，N; A是CH，N; R5是氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑，-CH2C6H4NHR34，-CH2C6H4C6H4R14; R14是唑，-COOH; R 21至R 34独立地为C 1-6 - 烷基或C 1-6 - 卤代烷基; m为0〜6; n为0〜6; t为0或1，条件是当Z为N时，R5为氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑或-CH2C6H4NHR34，或其盐，以及包含所述苯衍生物或其药学上可接受的盐和药学上可接受的载体的药物组合物。

6. 发明授权

US5739131A Benzene derivatives and pharmaceutical composition 失效
标题翻译：苯衍生物和药物组成
公开(公告)号：US5739131A
公开(公告)日：1998-04-14
申请号：US841621
申请日：1997-04-30
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
IPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26 , A61K31/535
CPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26
摘要： A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH; R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, or --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.
摘要翻译：式（I）的苯衍生物：其中R 1是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NH 2，-NHR 21; R2是羟基，-OR22，任选地被一个或多个氮，氧或硫原子间隔的三至七元饱和脂环族氨基，-NHR 23，-N（R 24）2，-NH 2; R 4是氢，C 1-6 - 烷基或-C（= O）R 25; R 7是-CO - ， - SO 2 - ; R8是-CO-，单键; R12为-R11-R5; R 11是-N（R 5） - ， - NH - ， - O - ， - N（R 26） - ， - N（C（= O）R 27） - ， - N（C（= O）NH 2）（C（= O）NHR 28） - ; R 13是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NHC（= O）（CH 2）m C 6 H 5，-NHC（= O）R 29，-NHC（= O）CH（C 6 H 5） -NHR 30， - （CH 2）n C 6 H 5; Z是C，CH，N; A是CH，N; R5是氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑，-CH2C6H4NHR34，-CH2C6H4C6H4R14; R14是唑，-COOH; R 21至R 34独立地为C 1-6 - 烷基或C 1-6 - 卤代烷基; m为0〜6; n为0〜6; t为0或1，条件是当Z为N时，R5为氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑或-CH2C6H4NHR34，或其盐，以及包含所述苯衍生物或其药学上可接受的盐和药学上可接受的载体的药物组合物。

7. 发明授权

US5731310A Benzene derivatives and pharmaceutical composition 失效
标题翻译：苯衍生物和药物组成
公开(公告)号：US5731310A
公开(公告)日：1998-03-24
申请号：US702116
申请日：1996-08-23
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Toshikazu Dewa , Toru Yamazaki , Michihito Ise
IPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26 , A61K31/44 , A61K31/535 , C07D211/90 , C07D413/06
CPC分类号： C07D213/79 , C07D213/81 , C07D257/04 , C07D295/192 , C07D295/26
摘要： A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O) (CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O) R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, --CH.sub.2 C.sub.6 H.sub.4 C.sub.6 H.sub.4 R.sup.14 ; R.sup.14 is azole, --COOH; R.sup.21 to R.sup.34 are independently C.sub.1-6 -alkyl or C.sub.1-6 -haloalkyl; m is 0 to 6; n is 0 to 6; t is 0 or 1, with the proviso that when Z is N, R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.sub.2 C.sub.6 H.sub.4 OH, --CH.sub.2 C.sub.6 H.sub.4 OR.sup.32, --CH.sub.2 C.sub.6 H.sub.4 NH.sub.2, --CH.sub.2 C.sub.6 H.sub.4 N(R.sup.33).sub.2, --CH.sub.2 C.sub.6 H.sub.4 -azole, or --CH.sub.2 C.sub.6 H.sub.4 NHR.sup.34, or a salt thereof, and a pharmaceutical composition comprising said benzene derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.
摘要翻译：式（I）的苯衍生物：其中R 1是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NH 2，-NHR 21; R2是羟基，-OR22，任选地被一个或多个氮，氧或硫原子间隔的三至七元饱和脂环族氨基，-NHR 23，-N（R 24）2，-NH 2; R 4是氢，C 1-6 - 烷基或-C（= O）R 25; R 7是-CO - ， - SO 2 - ; R8是-CO-，单键; R12为-R11-R5; R 11是-N（R 5） - ， - NH - ， - O - ， - N（R 26） - ， - N（C（= O）R 27） - ， - N（C（= O）NH 2）（C（= O）NHR 28） - ; R 13是氢，C 1-6 - 烷基，C 1-6 - 卤代烷基，-NHC（= O）（CH 2）m C 6 H 5，-NHC（= O）R 29，-NHC（= O）CH（C 6 H 5）2，-NH 2， -NHR 30， - （CH 2）n C 6 H 5; Z是C，CH，N; A是CH，N; R5是氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑，-CH2C6H4NHR34，-CH2C6H4C6H4R14; R14是唑，-COOH; R 21至R 34独立地为C 1-6 - 烷基或C 1-6 - 卤代烷基; m为0〜6; n为0〜6; t为0或1，条件是当Z为N时，R5为氢，-CH2C6H4COOH，-CH2C6H4COOR31，-CH2C6H4OH，-CH2C6H4OR32，-CH2C6H4NH2，-CH2C6H4N（R33）2，-CH2C6H4-唑或-CH2C6H4NHR34，或其盐，以及包含所述苯衍生物或其药学上可接受的盐和药学上可接受的载体的药物组合物。

8. 发明授权

US5585381A Pyrimidine derivatives and pharmaceutical composition 失效
标题翻译：嘧啶衍生物和药物组合物
公开(公告)号：US5585381A
公开(公告)日：1996-12-17
申请号：US454629
申请日：1995-05-31
申请人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Michihito Ise
发明人： Mikiro Yanaka , Fuyuhiko Nishijima , Hiroyuki Enari , Michihito Ise
IPC分类号： A61P13/12 , C07D239/48 , C07D239/50 , A61K31/505
CPC分类号： C07D239/48 , C07D239/49 , C07D239/50
摘要： A pyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or --NHR.sup.11 group; R.sup.2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, --(CH.sub.2).sub.m C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.12, --NH(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH(CH.sub.2).sub.p C.sub.6 H.sub.4 --OR.sup.13, --N(R.sup.14)(CH.sub.2).sub.q C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.15, --NHC(.dbd.O)(CH.sub.2).sub.r C.sub.6 H.sub.5, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --OR.sup.16, or --O(CH.sub.2).sub.s C.sub.6 H.sub.5 group; R.sup.3 is --COOH, --COOR.sup.17, hydroxyl, --OR.sup.18, --NH.sub.2, --N(R.sup.19).sub.2, --NHR.sup.20, azole, or sulfonic acid group; R.sup.11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, and R.sup.20 are independently alkyl of 1 to 6 carbon atoms; m is 0 or an integer of 1 to 6; n is 0 or an integer of 1 to 6; p is 0 or an integer of 1 to 6; q is 0 or an integer of 1 to 6; r is 0 or an integer of 1 to 6; and s is 0 or an integer of 1 to 6, or a salt thereof, and a pharmaceutical composition comprising said pyrimidine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed.
摘要翻译：式（I）的嘧啶衍生物：其中R 1为氢原子，1至6个碳原子的烷基，1至6个碳原子的卤代烷基或-NHR 11基团; R2是氢或卤素原子，1-6个碳原子的烷基，1-6个碳原子的卤代烷基， - （CH2）mC6H5，-NH2，-NHR12，-NH（CH2）nC6H5，-NH（CH2）pC6H4- OR 13，-N（R 14）（CH 2）q C 6 H 5，-NHC（= O）R 15，-NHC（= O）（CH 2）rC 6 H 5，-NHC（= O）CH（C 6 H 5）2，-OR 16或-O CH2）sC6H5组; R3是-COOH，-COOR17，羟基，-OR18，-NH2，-N（R19）2，-NHR20，唑或磺酸基团; R11为1〜6个碳原子的烷基或1〜6个碳原子的卤代烷基; R 12，R 13，R 14，R 15，R 16，R 17，R 18，R 19和R 20独立地为1至6个碳原子的烷基; m为0或1〜6的整数; n为0或1〜6的整数， p为0或1〜6的整数; q为0或1〜6的整数; r为0或1〜6的整数，和s为0或1〜6的整数，或其盐，以及包含所述嘧啶衍生物或其药学上可接受的盐和药学上可接受的载体的药物组合物。

9. 发明申请

US20090181095A1 Oxidative stress inhibitor 审中-公开
标题翻译：氧化应激抑制剂
公开(公告)号：US20090181095A1
公开(公告)日：2009-07-16
申请号：US11920534
申请日：2006-05-15
申请人： Sumie Goto , Mikio Sugano , Kenji Bannai , Fuyuhiko Nishijima
发明人： Sumie Goto , Mikio Sugano , Kenji Bannai , Fuyuhiko Nishijima
IPC分类号： A61K9/14 , A61K33/44 , A61P9/00 , A61P13/12 , A61P35/00 , A61P3/10 , A61P9/10
CPC分类号： A61K33/44
摘要： An oxidative stress inhibitor comprising a spherical activated carbon as an effective component is disclosed. The present invention is effective in the prevention or the treatment of a disease caused by oxidative stress, such as a kidney disease, a circulatory disease (for example, cardiovascular disease), a cancer, a diabetes, a cerebral stroke, or an arterial sclerosis.
摘要翻译：公开了包含球形活性炭作为有效成分的氧化应激抑制剂。本发明有效地预防或治疗由氧化应激引起的疾病，例如肾脏疾病，循环系统疾病（例如心血管疾病），癌症，糖尿病，脑卒中或动脉硬化。

10. 发明申请

US20070264347A1 Agent for Treating or Preventing Diabetic Neuropathy 审中-公开
标题翻译：治疗或预防糖尿病性神经病的药物
公开(公告)号：US20070264347A1
公开(公告)日：2007-11-15
申请号：US11662746
申请日：2005-09-21
申请人： Yuusuke Higuchi , Kazumi Obara , Fuyuhiko Nishijima
发明人： Yuusuke Higuchi , Kazumi Obara , Fuyuhiko Nishijima
IPC分类号： A61K33/44 , A61P25/00 , A61P3/10
CPC分类号： A61K33/44
摘要： An agent effective for treating or preventing a diabetic neuropathy, which is a diabetic complication, is provided. The agent comprises a spherical activated carbon as an effective ingredient.
摘要翻译：提供了有效治疗或预防糖尿病并发症的糖尿病性神经病变的药剂。该试剂包含球形活性炭作为有效成分。

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