Benzene derivatives and pharmaceutical composition
    3.
    发明授权
    Benzene derivatives and pharmaceutical composition 失效
    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

    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。

    Benzene derivatives and pharmaceutical composition
    4.
    发明授权
    Benzene derivatives and pharmaceutical composition 失效
    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

    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。

    Benzene derivatives and pharmaceutical composition
    5.
    发明授权
    Benzene derivatives and pharmaceutical composition 失效
    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

    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。

    Cardiac diseases improving method
    6.
    发明授权
    Cardiac diseases improving method 失效
    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

    IPC分类号: A61K31495

    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)

    Pyrimidine derivatives and pharmaceutical composition
    8.
    发明授权
    Pyrimidine derivatives and pharmaceutical composition 失效
    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

    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。

    Method for the treatment of hemorrhoidal diseases
    9.
    发明授权
    Method for the treatment of hemorrhoidal diseases 失效
    治疗痔疮疾病的方法

    公开(公告)号:US5562901A

    公开(公告)日:1996-10-08

    申请号:US450465

    申请日:1995-05-25

    IPC分类号: A61K33/40 A61K33/44

    CPC分类号: A61K33/40

    摘要: The disclosure describes a method of treating a patient suffering from hemorrhoidal diseases, comprising orally administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a spherical activated carbon having a particle size of 0.05 to 2 mm.

    摘要翻译: 本公开内容描述了治疗患有痔疮疾病的患者的方法,其包括向所述患者口服施用有效量的药物组合物,其剂量单位形式包含粒径为0.05至2mm的球形活性炭。

    Enhancer for the antianemia effect of erythropoietin and method of
augmenting the antianemia effect of erythropoietin
    10.
    发明授权
    Enhancer for the antianemia effect of erythropoietin and method of augmenting the antianemia effect of erythropoietin 失效
    促红细胞生成素抗血症作用的增强剂及促红细胞生成素抗血栓作用的方法

    公开(公告)号:US5399551A

    公开(公告)日:1995-03-21

    申请号:US137789

    申请日:1993-10-19

    摘要: There is disclosed an enhancer for the antianemia effect of erythropoietin using a spherical carbon as an active ingredient in an amount effective for treating anemia in combination with erythropoietin. The enhancer is orally administered. The antianemia effect of erythropoietin can be remarkably enhanced, the dosage of erythropoietin can be remarkably decreased, and side effects from erythropoietin can be remarkably reduced. There is further disclosed a method of augmenting the antianemia effect of erythropoietin by administering to a patient an effective amount of a spherical carbon in combination with a portion of an effective amount of erythropoietin for treating anemia.

    摘要翻译: 公开了使用球形碳作为活性成分的促红细胞生成素的抗血症效果的增强剂,其用量与红细胞生成素联合治疗贫血有效。 口服施用增强剂。 红细胞生成素的抗血症作用显着增强,促红细胞生成素的用量显着降低,促红细胞生成素的副作用明显降低。 还公开了通过与有效量的促红细胞生成素的一部分组合施用有效量的球形碳用于治疗贫血的方法来增加促红细胞生成素的抗血症效果的方法。