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    • 9. 发明授权
    • Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
    • 金属蛋白酶抑制剂 - 其组合物,用途,制备及其中间体
    • US06500948B1
    • 2002-12-31
    • US09675555
    • 2000-09-29
    • Scott E. ZookRaymond Dagnino, Jr.Michael E. DeasonSteven L. BenderMichael J. Melnick
    • Scott E. ZookRaymond Dagnino, Jr.Michael E. DeasonSteven L. BenderMichael J. Melnick
    • C07D41700
    • C07D401/12C07D239/04C07D241/04C07D279/12C07D417/12
    • The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
    • 本发明涉及式1化合物:其中:Z为O或S; V是与C *和N一起形成具有六个环原子的环的二价基团,其中除C *和N之外的所述环原子各自独立地是未取代的或被合适的取代基取代,并且所述另一个环中的至少一个 原子是选自O,N和S的杂原子,其余为碳原子; Ar为芳基或杂芳基; 其药学上可接受的前药,其盐和溶剂化物。本发明还涉及这些化合物的药学上可接受的前药,盐和溶剂化物。 本发明还涉及通过给予式I化合物或其前药,其溶剂合物的盐来抑制金属蛋白酶的活性的方法。 本发明还涉及包含有效量的这些化合物,前药,盐和溶剂合物的药物组合物。 本发明还涉及可用于制备这些化合物,前药,盐和溶剂合物的方法和中间体。