Flavone derivative and medicine comprising the same
    1.
    发明公开
    Flavone derivative and medicine comprising the same 失效
    Flavon Derivative und deren enthaltende Arzneimittel

    公开(公告)号:EP0834510A2

    公开(公告)日:1998-04-08

    申请号:EP97117158.2

    申请日:1997-10-02

    申请人: KOWA CO. LTD.

    摘要: This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same.
    wherein A represents H, halogen, phenyl, naphthyl, a group of the formula (2) in which X is H or halogen, B is -CH=CH-, -CH=N-, -N(R 7 )- (R 7 : lower alkyl or alkoxyalkyl), -O- or -S-; W represents a single bond, -CH 2 O- or -CH=CH-; at least one of R 1 to R 4 represents -COOH, -CN, alkyloxycarbonyl, tetrazolyl or -CONHR 8 (R 8 : H, lower alkyl or phenylsulfonyl), the remainder thereof individually represent H, halogen, -OH, lower alkyl or lower alkoxyl; R 5 represents H, -OH, lower alkoxyl, -O(CH 2 ) m NR 9 R 10 (R 9 ,R 10 : H or lower alkyl, or coupled together with the adjacent N to form a phthalimido group; m: 1-5), or a group of the formula (3) (n: 1-5, ℓ: 2-3; and R 6 represents H, halogen, lower alkyl or lower alkoxyl. A situation where A is H or halogen, W is a single bond and R 5 is H is excluded. The compound (1) has excellent cys-LT 1 receptor antagonism.

    摘要翻译: 本发明涉及由式(1)表示的黄酮衍生物或其盐,以及含有该衍生物的药物。 其中A表示H,卤素,苯基,萘基,其中X是H或卤素的式(2)的基团,B是-CH = CH-,-CH = N-,-N(R 7) ) - (R 7:低级烷基或烷氧基烷基),-O-或-S-; W表示单键,-CH 2 O-或-CH = CH-; R 1至R 4中的至少一个表示-COOH,-CN,烷氧基羰基,四唑基或-CONHR 8(R 8:H,低级烷基或苯基磺酰基),其余部分分别表示H, 卤素,-OH,低级烷基或低级烷氧基; R 5表示H,-OH,低级烷氧基,-O(CH 2)m NR 9 R 10(R 9,R 10):H或低级烷基,或与相邻的N至 形成苯二甲酰亚氨基; m:1-5)或式(3)的基团(n:1-5,1:2-3; R 6表示H,卤素,低级烷基或低级烷氧基。 A为H或卤素,W为单键,R 5为H的情况除外。化合物(1)具有优异的cys-LT1受体拮抗作用。

    Flavone derivative and medicine comprising the same
    2.
    发明公开
    Flavone derivative and medicine comprising the same 失效
    黄酮衍生物和包含它的药物

    公开(公告)号:EP0834510A3

    公开(公告)日:1998-04-29

    申请号:EP97117158.2

    申请日:1997-10-02

    申请人: KOWA CO. LTD.

    摘要: This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same.
    wherein A represents H, halogen, phenyl, naphthyl, a group of the formula (2) in which X is H or halogen, B is -CH=CH-, -CH=N-, -N(R 7 )- (R 7 : lower alkyl or alkoxyalkyl), -O- or -S-; W represents a single bond, -CH 2 O- or -CH=CH-; at least one of R 1 to R 4 represents -COOH, -CN, alkyloxycarbonyl, tetrazolyl or -CONHR 8 (R 8 : H, lower alkyl or phenylsulfonyl), the remainder thereof individually represent H, halogen, -OH, lower alkyl or lower alkoxyl; R 5 represents H, -OH, lower alkoxyl, -O(CH 2 ) m NR 9 R 10 (R 9 ,R 10 : H or lower alkyl, or coupled together with the adjacent N to form a phthalimido group; m: 1-5), or a group of the formula (3) (n: 1-5, ℓ: 2-3; and R 6 represents H, halogen, lower alkyl or lower alkoxyl. A situation where A is H or halogen, W is a single bond and R 5 is H is excluded. The compound (1) has excellent cys-LT 1 receptor antagonism.

    摘要翻译: 本发明涉及由式(1)表示的黄酮衍生物或其盐,还涉及含有其的药物。 其中A代表H,卤素,苯基,萘基,其中X是H或卤素,B是-CH = CH-,-CH = N-,-N(R7) - (R7: 低级烷基或烷氧基烷基), - O-或-S-; W表示单键,-CH 2 O-或-CH = CH-; R 1至R 4中至少一个表示-COOH,-CN,烷氧基羰基,四唑基或-CONHR 8(R 8:H,低级烷基或苯基磺酰基),其余的各自表示H,卤素,-OH,低级烷基或低级烷氧基; R5代表H,-OH,低级烷氧基,-O(CH2)mNR9R10(R9,R10:H或低级烷基,或与相邻的N偶联形成邻苯二甲酰亚氨基; m:1-5),或 (3)(n:1-5,1:2-3; R6代表H,卤素,低级烷基或低级烷氧基,A是H或卤素,W是单键,R5是H的情况是 化合物(1)具有优异的cys-LT1受体拮抗作用。