Tetracyclic compounds for enhancing biosynthesis of erythropoietin,
compositions containing same, and methods of use thereof
    3.
    发明授权
    Tetracyclic compounds for enhancing biosynthesis of erythropoietin, compositions containing same, and methods of use thereof 失效
    用于增强促红细胞生成素生物合成的四环化合物,含有它们的组合物及其使用方法

    公开(公告)号:US5985913A

    公开(公告)日:1999-11-16

    申请号:US69693

    申请日:1998-04-29

    CPC分类号: C07D311/94 A61K31/352

    摘要: The present invention provides a compound in substantially pure form having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 may independently be hydrogen, halogen, nitro, CF.sub.3, hydroxy, C.sub.1-5 alkyl, aryl or OR.sub.9, wherein R.sub.9 is C.sub.1-5 alkyl, wherein R.sub.10 is COC.sub.1-5 alkyl; or wherein any two consecutive R groups may be members of a C.sub.5 -C.sub.6 membered ring, and wherein the intracyclic-dashed line represents a covalent bond which may be present or absent, with the proviso that when R.sub.10 is present, the exocyclic-covalent bond is absent, and when R.sub.10 is absent, the exocyclic-covalent bond is present, and with the proviso that when R.sub.10 is absent, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen and when R.sub.10 is absent, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 cannot all be hydrogen when either R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is hydroxy, or R2 is carboethoxy. The present invention further provides a composition comprising the compound described above in an amount effective to modulate cellular expression of a mammalian gene encoding erythropoietin and a carrier.

    摘要翻译: 本发明提供具有以下结构的基本上纯的形式的化合物:其中R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8各自独立地为氢,卤素,硝基,CF 3,羟基,C 1-5烷基 ,芳基或OR9,其中R9为C1-5烷基,其中R10为COC1-5烷基; 或其中任何两个连续的R基团可以是C 5 -C 6的环的成员,并且其中所述环内虚线表示可以存在或不存在的共价键,条件是当R 10存在时,所述环外共价键为 当不存在R 10时,存在环外共价键,条件是当R 10不存在时,R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8不能全部为氢,当R 10为 当R 1,R 2,R 3或R 4为羟基或R 2为乙氧基乙氧基时,R 5,R 6,R 7和R 8不能全部为氢。 本发明还提供一种包含上述化合物的组合物,其量可有效调节编码促红细胞生成素和载体的哺乳动物基因的细胞表达。