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    • 5. 发明授权
    • Benzene derivatives and pharmaceutical composition
    • 苯衍生物和药物组成
    • US5696118A
    • 1997-12-09
    • US457147
    • 1995-06-01
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26A61K31/445A61K31/535
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26
    • 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.
    • 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
    • Benzene derivatives and pharmaceutical composition
    • 苯衍生物和药物组成
    • US5739131A
    • 1998-04-14
    • US841621
    • 1997-04-30
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26A61K31/535
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26
    • 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.
    • 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
    • Benzene derivatives and pharmaceutical composition
    • 苯衍生物和药物组成
    • US5731310A
    • 1998-03-24
    • US702116
    • 1996-08-23
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariToshikazu DewaToru YamazakiMichihito Ise
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26A61K31/44A61K31/535C07D211/90C07D413/06
    • C07D213/79C07D213/81C07D257/04C07D295/192C07D295/26
    • 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.
    • 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
    • Pyrimidine derivatives and pharmaceutical composition
    • 嘧啶衍生物和药物组合物
    • US5585381A
    • 1996-12-17
    • US454629
    • 1995-05-31
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariMichihito Ise
    • Mikiro YanakaFuyuhiko NishijimaHiroyuki EnariMichihito Ise
    • A61P13/12C07D239/48C07D239/50A61K31/505
    • C07D239/48C07D239/49C07D239/50
    • 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.
    • 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。