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    • 61. 发明授权
    • Steroid sulphatase inhibitors
    • 类固醇硫酸酶抑制剂
    • US06642397B1
    • 2003-11-04
    • US09579163
    • 2000-05-25
    • Michael John ReedBarry Victor Lloyd Potter
    • Michael John ReedBarry Victor Lloyd Potter
    • C07J100
    • A61K31/37C07D311/16C07D311/30C07D311/32C07D311/36C07J41/0072
    • A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 &mgr;M.
    • 描述了在需要相同的受试者中抑制类固醇硫酸酯酶活性的方法。 所述方法包括向所述受试者施用抑制甾族硫酸酯酶的量的环系化合物; 所述环系化合物包含连接在其上的环,其中R 1和R 2各自独立地选自H,烷基,烯基,环烷基和芳基,或一起表示任选地含有一个或多个杂原子或基团的亚烷基 亚烷基链; 并且其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂(E.C.3.1.6.2); 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物,并在pH 7.4和37℃下与类固醇硫酸酶(EC3.1.6.2)一起温育,则其将提供小于 50亩。
    • 65. 发明授权
    • Steroid sulphatase inhibitors
    • 类固醇硫酸酶抑制剂
    • US06187766B1
    • 2001-02-13
    • US09238345
    • 1999-01-27
    • Michael John ReedBarry Victor Potter
    • Michael John ReedBarry Victor Potter
    • A61K31165
    • A61K31/37C07D311/16C07D311/30C07D311/32C07D311/36C07J41/0072
    • A method of inhibiting steroid sulphatase activity in a subject in need of same as described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 &mgr;M.
    • 一种抑制需要与上述相同的对象的类固醇硫酸酯酶活性的方法。该方法包括向所述受试者施用抑制甾类硫酸酯酶的量的环系化合物; 所述环系化合物包含与R 1和R 2各自独立地选自H,烷基,烯基,环烷基和芳基的或者一起表示任选含有一个或多个杂原子或基团的亚烷基 亚烷基链; 并且其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂(E.C.3.1.6.2); 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物,并在pH 7.4和37℃下与类固醇硫酸酶(EC3.1.6.2)一起温育,则其将提供小于 50亩。