Inhibiting osteoclast-mediated bone resorption using aminoalkyl-substituted phenyl derivatives
    8.
    发明公开
    Inhibiting osteoclast-mediated bone resorption using aminoalkyl-substituted phenyl derivatives 失效
    Verhinderung der durch Osteoklasten verursachten Knochenresorption durch aminoalkylsubstituierte Phenylderivate。

    公开(公告)号:EP0528586A1

    公开(公告)日:1993-02-24

    申请号:EP92307156.7

    申请日:1992-08-05

    申请人: MERCK & CO. INC.

    IPC分类号: A61K31/325 A61K31/445

    摘要: Compounds of the general formula
    and the pharmaceutically acceptable salts thereof
    wherein
       n is an integer of from 0 to 6;
       Y is CH₂, O, SO₂, -CONH-, -NHCO-, or

       R¹ and R² are independently
          hydrogen,
          C₁₋₈ alkyl,
          heterocyclyl C₀₋₄ alkyl,
          aryl C₀₋₄ alkyl,
          amino C₁₋₄ alkyl,
          C₁₋₄ alkylamino C₁₋₄ alkyl, or
          C₃₋₈ cycloalkyl
       wherein R¹ and R² may be unsubstituted or substituted with one or more groups chosen from R³, where
       R³ is
          hydrogen,
          C₁₋₆ alkyl,
          hydroxy C₀₋₄ alkyl,
          carboxy C₀₋₄ alkyl,
          C₁₋₄ alkyloxy C₀₋₄ alkyl,
          heterocyclyl C₀₋₄ alkyl,
          aryl C₀₋₄ alkyl,
          halogen, or
          CF₃;
       R⁴ is
          C₁₋₆ alkyl,
          heterocyclyl C₀₋₄ alkyl, or
          aryl C₀₋₄ alkyl;
       R⁵ is
          hydrogen,
          C₁₋₆ alkyl,
          aryl C₀₋₃ alkyl, or
          C₁₋₆ alkylcarbonyloxyethyl
    are used for the manufacture of a medicament for treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.

    摘要翻译: 通式的化合物及其药学上可接受的盐,其中n为0-6的整数; Y是CH 2,O,SO 2,-CONH - , - NHCO-或 R 1和R 2独立地是氢,C 1-8烷基,杂环基C 0-4烷基,芳基C 0-4烷基, 氨基C 1-4烷基,C 1-4烷基氨基C 1-4烷基或C 3-8环烷基,其中R 1和R 2可以是未被取代的或被一个或多个选自R 3的基团取代, R 3是氢,C 1-6烷基,羟基C 0-4烷基,羧基C 0-4烷基,C 1-4烷氧基C 0-4烷基,杂环基C 0-4烷基,芳基C 0-4烷基,卤素或CF 3; R 4是C 1-6烷基,杂环基C 0-4烷基或芳基C 0-4烷基; R 5是氢,C 1-6烷基,芳基C 0-3烷基或C 1-6烷基羰基氧基乙基用于制备通过抑制破骨细胞的骨吸收活性来治疗骨质疏松症的药物。