4H-1-benzopyran-4-one compounds which have anti-inflamatory or
immunodulating action
    10.
    发明授权
    4H-1-benzopyran-4-one compounds which have anti-inflamatory or immunodulating action 失效
    具有抗炎或免疫调节作用的4H-1-苯并吡喃-4-酮化合物

    公开(公告)号:US4900727A

    公开(公告)日:1990-02-13

    申请号:US302084

    申请日:1989-01-26

    摘要: The present invention relates to novel 4H-1-benzopyran-4-one derivatives, to processes for the preparation thereof and to their use as anti-inflammatory, analgesic, immuno-suppressive and anti-allergic agents. In particular, the present invention relates to novel compounds of the formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl having 1 to 6 carbon atoms, arly-C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, aryl or carboxyl or an aldehyde or COO--C.sub.1 -C.sub.4 -alkyl group, R.sub.2 is hydrogen, alkyl having 1 to 6 carbon atoms, nitro, amino, di-C.sub.1 -C.sub.4 -alkylamino or a halogen, R.sub.3 is C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.4 -alkyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, aryl-C.sub.1 -C.sub.4 -alkyl, nitro, amino, a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group or halogen, R.sub.4 is hydrogen, hydroxyl, C.sub.1 -C.sub.4 -alkyoxy, C.sub.1 -C.sub.4 -alkyoxycarbonyl, aryloxy, amino or a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group, R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, aryl-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkanoyl or aroyl, the aryl group being phenyl which is unsubstituted, monosubstituted or polysubstituted, m is an integer between 0 and 3 and n is an integer between 0 and 2, and to pharmacologically acceptable acid addition salts thereof.

    摘要翻译: 本发明涉及新的4H-1-苯并吡喃-4-酮衍生物,其制备方法及其作为抗炎,镇痛,免疫抑制和抗过敏剂的用途。 特别地,本发明涉及式Ⅰ的新化合物,其中R 1是氢,具有1至6个碳原子的烷基,芳基-C 1 -C 4烷基,取代的C 1 -C 6烷基,C 3 -C 6 环烷基,C 3 -C 6 - 环烷基-C 1 -C 4烷基,C 2 -C 6 - 烯基,C 3 -C 6炔基,芳基或羧基或醛或COO-C 1 -C 4烷基,R 2是氢,具有1至 6个碳原子,硝基,氨基,二-C 1 -C 4烷基氨基或卤素,R 3是C 1 -C 4 - 烷基,取代的C 1 -C 4 - 烷基,羟基,C 1 -C 4 - 烷氧基,芳基-C 1 -C 4烷基, 硝基,氨基,C1-C4-烷基氨基或二C1-C4-烷基氨基或卤素,R4是氢,羟基,C1-C4-烷氧基,C1-C4-烷氧基羰基,芳氧基,氨基或C1-C4烷基氨基 或二-C 1 -C 4烷基氨基,R 5是氢,C 1 -C 6烷基,取代的C 1 -C 6烷基,芳基-C 1 -C 4 - 烷基,C 3 -C 6 - 环烷基,C 3 -C 6环烷基-C 1 -C 4 - 烷基,C 1 -C 4 - 烷酰基或芳酰基,所述芳基是未取代的,单取代或多取代的苯基,m是0和3之间的整数,n是整数 0和2之间,以及其药理学上可接受的酸加成盐。