DIARYLBENZOPYRAN DERIVATIVES AS CYCLOOXYGENASE-2 INHIBITORS
    1.
    发明公开
    DIARYLBENZOPYRAN DERIVATIVES AS CYCLOOXYGENASE-2 INHIBITORS 有权
    DIARYLBENZOPYRANDERIVATE如环氧合酶-2抑制剂

    公开(公告)号:EP1105384A1

    公开(公告)日:2001-06-13

    申请号:EP99938646.9

    申请日:1999-08-20

    摘要: The diarylbenzopyran derivatives represented by general formula (I): wherein Y is an oxygen atom or a sulfur atom; R?1 and R2¿, identical to or different from each other, are independently a hydrogen atom, a halogen atom, a C¿1?-C6 lower alkyl group, a trifluromethyl group, an alkoxy group, a hydroxy group, a nitro group, a nitrile group, or a carboxyl group; R?3¿ is a group of a formula: S(O)nR5 wherein n is an integer of 0∩2, R5 is a hydrogen atom, a C¿1?-C6 lower alkyl group, or a group of a formula: NR?6R7¿ wherein R?6 and R7¿, identical to or different from each other, are independently a hydrogen atom, or a C¿1?-C6 lower alkyl group; R?4¿ is oxazolyl, benzo[b]thienyl, furanyl, thienyl, naphthyl, thiazolyl, indolyl, pyrolyl, benzofuranyl, benzodioxoyl, or a substituted group presented by structures (a), (b), (c) or (d) wherein R8 through R12 identical to or different from one another, are independently a hydrogen atom, a halogen atom, a C¿1?-C6 lower alkyl group, a trifluromethyl group, an alkoxy group, a hydroxy group, a hydroxyalkyl group, a nitro group, a group of a formula: S(O)nR?5¿, a group of a formula NR6R7, a trifluromethoxy group, a nitrile group, a carboxyl group, an acetyl group, or a formyl group wherein n, R?5, R6 and R7¿ have the same meaning as defined X and R3 above; and R13 is a hydrogen atom, a halogen atom, a C¿1?-C6 lower alkyl group, a trifluromethyl group, an alkoxy group, a hydroxy group, a trifluromethoxy group, a carboxyl group, or an acetyl group; or their pharmaceutically acceptable salts are disclosed. And also cyclooxygenase-2 inhibitor composition, which consists of an effective amount of a diarylbenzopyran derivative and pharmaceutically acceptable salts of diarylbenzopyran derivative and shows an excellent selective inhibition, is disclosed.