Naphthopyran derivatives and use thereof
    15.
    发明公开
    Naphthopyran derivatives and use thereof 失效
    萘普生衍生物及其用途

    公开(公告)号:EP0337413A3

    公开(公告)日:1990-11-22

    申请号:EP89106450.3

    申请日:1989-04-12

    IPC分类号: C07D311/92 A61K31/35

    CPC分类号: C07D311/92

    摘要: The present invention relates to an aromatase inhibiting composition which contains a compound of the formula:
    wherein R is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl; R¹ is hydrogen or lower alkyl; and A is hydrogen, a group of the formula
    in which R² is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl and R³ is hydrogen or lower alkyl, or a group of the formula
    in which R⁴ and R⁵ are independently hydrogen or lower alkyl, or a salt thereof. The present composition is useful in the prevention and treatment of estrogen-dependent diseases, such as breast cancer.

    摘要翻译: 本发明涉及芳香酶抑制组合物,其含有下式化合物:其中R是羟基,可被低级烷基取代的低级烷氧基或氨基; R 1是氢或低级烷基; A为氢,式为CHEM的基团,其中R 2为羟基,可被低级烷基取代的低级烷氧基或氨基,R 3为氢或低级烷基,或式 其中R 4和R 5独立地为氢或低级烷基,或其盐。 本发明的组合物可用于预防和治疗雌激素依赖性疾病,例如乳腺癌。

    Physiologically active substance tan-931, its derivatives, their production and use
    16.
    发明公开
    Physiologically active substance tan-931, its derivatives, their production and use 失效
    Physiologisch aktive Substanz tan-931,ihre Derivate,ihre Herstellung und Verwendung。

    公开(公告)号:EP0342665A2

    公开(公告)日:1989-11-23

    申请号:EP89108926.0

    申请日:1989-05-18

    摘要: A novel compound of the formula (I):
    wherein R₁ is optionally esterified or amidated carboxyl; R₂, R₃ and R₄ are the same or different and are hydrogen or alkyl; A is fcrmyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R₁ is carboxyl, R₂, R₃ and R₄ are hydrogen and X is formyl are also disclosed.

    摘要翻译: 式(I)的新型化合物:其中R 1任选被酯化或酰胺化的羧基; R2,R3和R4相同或不同,为氢或烷基; A是fcrmyl,羟基亚氨基甲基或羧基; 并且X是氢或卤素或其盐,其可用作芳香酶抑制剂或其生产的中间体。 制备式(I)化合物的方法和含有作为活性成分的式(I)化合物的芳香酶抑制剂的方法,其中A是甲酰基,X是氢,或其盐,以及能产生青霉素的青霉菌(Penicillium funiculosum) 还公开了其中R 1是羧基,R 2,R 3和R 4是氢并且X是甲酰基的化合物(I)。