Steroid sulphatase inhibitors
    61.
    发明授权
    Steroid sulphatase inhibitors 失效
    类固醇硫酸酶抑制剂

    公开(公告)号:US06642397B1

    公开(公告)日:2003-11-04

    申请号:US09579163

    申请日:2000-05-25

    IPC分类号: C07J100

    摘要: 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.

    摘要翻译: 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。

    Compounds that inhibit oestrone sulphatase and/or aromatase and methods for making and using
    62.
    发明授权
    Compounds that inhibit oestrone sulphatase and/or aromatase and methods for making and using 失效
    抑制雌二醇硫酸酯酶和/或芳香酶的化合物及其制备和使用方法

    公开(公告)号:US06506792B1

    公开(公告)日:2003-01-14

    申请号:US09638315

    申请日:2000-08-14

    IPC分类号: A61K31352

    摘要: The instant invention relates to sulphamate compounds of formula I, wherein A represents a ring structure, B represents a ring structure, D a ring structure, C is a bond, E is a link joining ring structure B to the ring structure D, X represents a suitable first group, and Y represents a suitable second group; wherein one ring of the compound is a phenolic ring; and wherein any one of ring structures A, B and D has a bound thereto a sulphamate group.

    摘要翻译: 本发明涉及式I的氨基磺酸酯化合物,其中A表示环结构,B表示环结构,D表示环结构,C为键,E为环结构B与环结构D的连接,X表示 合适的第一组,Y表示合适的第二组; 其中所述化合物的一个环是酚醛环; 并且其中环结构A,B和D中的任何一个具有与其结合的氨基磺酸酯基团。

    Steroid sulphatase inhibitors
    65.
    发明授权
    Steroid sulphatase inhibitors 失效
    类固醇硫酸酶抑制剂

    公开(公告)号:US06187766B1

    公开(公告)日:2001-02-13

    申请号:US09238345

    申请日:1999-01-27

    IPC分类号: A61K31165

    摘要: 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.

    摘要翻译: 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。

    Use of interleukin-6 antagonists for the treatment of diseases characterized by high levels of aromatase
    66.
    发明授权
    Use of interleukin-6 antagonists for the treatment of diseases characterized by high levels of aromatase 失效
    使用白细胞介素-6拮抗剂治疗以高水平芳香酶为特征的疾病

    公开(公告)号:US07160860B2

    公开(公告)日:2007-01-09

    申请号:US10988628

    申请日:2004-11-16

    申请人: Michael John Reed

    发明人: Michael John Reed

    IPC分类号: A61K38/00

    CPC分类号: A61K38/204

    摘要: The invention described herein relates to the use of human interleukin-6 antagonists, totally incapable of binding to gp 130, as specific inhibitors of the enzyme aromatase, useful for the treatment of hormone-dependent tumours, and particularly tumours of the breast.

    摘要翻译: 本文描述的本发明涉及完全不能结合gp 130的人白细胞介素-6拮抗剂作为芳香族酶的特异性抑制剂的用途,其可用于治疗激素依赖性肿瘤,特别是乳腺肿瘤。

    Triterpenoid compound for the treatment of diabetes
    67.
    发明授权
    Triterpenoid compound for the treatment of diabetes 失效
    三萜类化合物治疗糖尿病

    公开(公告)号:US5691386A

    公开(公告)日:1997-11-25

    申请号:US633396

    申请日:1996-04-16

    摘要: A novel hypoglycemically active triterpenoid compound isolated in purified, preferably substantially purified, form from Salacia spp., processes for obtaining the novel triterpenoid compound, compositions comprising the triterpenoid compound and methods for use a hypoglycemic agent, for example, in the treatment of diabetes, are described. In a preferred embodiment, the triterpenoid compound is obtained from Salacia prinoides. As an agent for the treatment of diabetes, the novel triterpenoid is useful for treating insulin-dependent (type I) and/or non-insulin-dependent (type II) diabetes.

    摘要翻译: 从Salacia spp。纯化,优选基本上纯化的形式中分离的一种新型低血糖活性三萜化合物,获得新型三萜化合物的方法,包含三萜化合物的组合物和使用降血糖剂的方法,例如治疗糖尿病, 被描述。 在一个优选的实施方案中,三萜化合物是从Salacia prinoides获得的。 作为治疗糖尿病的药物,新型三萜类化合物可用于治疗胰岛素依赖型(I型)和/或非胰岛素依赖型(II型)糖尿病。