Compounds that inhibit oestrone sulphatase; compositions thereof; and methods employing the same
    42.
    发明授权
    Compounds that inhibit oestrone sulphatase; compositions thereof; and methods employing the same 失效
    抑制雌二醇硫酸酯酶的化合物; 组合物; 和采用该方法的方法

    公开(公告)号:US06642220B1

    公开(公告)日:2003-11-04

    申请号:US09319213

    申请日:1999-11-23

    IPC分类号: A61K3156

    CPC分类号: C07J41/0072

    摘要: Disclosed and claimed are compounds suitable for use as an inhibitor of oestrone sulphatase in a subject in need thereof, as well as compositions containing such compounds and methods for using such compounds. Such compounds can be a sulphamate compound that has the Formula (X) and wherein X is a sulphamate group, and Y is CH2 and optionally any other H attached directly to the ring system is substituted by another group

    摘要翻译: 公开并要求保护的是适合用作有需要的受试者中的奥斯丁硫酸酯酶抑制剂的化合物,以及含有这些化合物的组合物和使用这些化合物的方法。 这样的化合物可以是具有式(X)的氨基磺酸盐化合物,其中X是氨基磺酸盐基团,Y是CH 2,并且任选地直接与环系统连接的任何其它H被另一个基团取代

    Compound
    44.
    发明授权
    Compound 失效
    复合

    公开(公告)号:US07846965B2

    公开(公告)日:2010-12-07

    申请号:US11710846

    申请日:2007-02-26

    IPC分类号: A61K31/352 C07D311/78

    摘要: A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.

    摘要翻译: 描述化合物。 特别地,描述了非甾体氨基磺酸盐化合物。 该化合物适合用作奥斯汀硫酸酯酶的抑制剂。 该化合物为通式(A),其中R 1 -R 6独立地选自H,卤素,羟基,氨基磺酸酯,烷基和取代的变体或其盐; 但其中R 1 -R 6中的至少一个为氨基磺酸酯基; 并且其中X是S,NH,取代的N,CH 2或取代的C中的任何一个。

    Compound
    46.
    发明授权
    Compound 失效

    公开(公告)号:US07129269B2

    公开(公告)日:2006-10-31

    申请号:US10327500

    申请日:2002-12-20

    IPC分类号: A61K31/352 C07D311/74

    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 bound thereto a sulphamate group.

    Methods for treating or preventing cancer by preventing, inhibiting or arresting cell cycling
    47.
    发明授权
    Methods for treating or preventing cancer by preventing, inhibiting or arresting cell cycling 失效
    通过预防,抑制或阻止细胞循环来治疗或预防癌症的方法

    公开(公告)号:US07078395B1

    公开(公告)日:2006-07-18

    申请号:US09561453

    申请日:2000-04-28

    IPC分类号: A61K31/56

    CPC分类号: A61K31/56

    摘要: There is provided use of a cyclic compound or a pharmaceutically active salt thereof in the manufacture of a medicament to prevent and/or inhibit and/or arrest cell cycling, wherein the cyclic compound comprises at least one ring, wherein Group I and Group II, independently of each other, are attached to a ring of the cyclic compound; wherein Group I is a hydrocarbyl or an oxyhydrocarbyl group; and wherein Group II is a group of the formula X is P or S; when X is P, Y is ═O or S, Z is —OH and R is hydrocarbyl or H; when X is S, Y is ═O, Z is ═O, and R is hydrocarbyl or N(R1)(R2), wherein each of R1 and R2 is independently selected from H or a hydrocarbyl group.

    摘要翻译: 提供环状化合物或其药物活性盐在制备用于预防和/或抑制和/或阻止细胞循环的药物中的用途,其中所述环状化合物包含至少一个环,其中第I组和第II组, 彼此独立地连接到环状化合物的环上; 其中组I是烃基或氧代烃基; 并且其中II族是式X的基团是P或S; 当X为P时,Y为-O或S,Z为-OH,R为烃基或H; 当X为S时,Y为-O,Z为-O,R为烃基或N(R 1 H 2)(R 2),其中R > 1 和R 2 <2个独立地选自H或烃基。

    Steroid sulphatase inhibitors
    50.
    发明授权

    公开(公告)号:US6011024A

    公开(公告)日:2000-01-04

    申请号:US111927

    申请日:1998-07-08

    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 a sulphamate group of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 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.degree. C. it would provide a K.sub.m value of less than 50 .mu.M.