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Method for Preparation of compounds having a Ring structure and a steroidal sulfamate Group useful for inhibiting the activity of steroid sulfatase.

机译:具有可抑制甾族硫酸酯酶活性的具有环结构和甾族氨基磺酸酯基团的化合物的制备方法。

摘要

Compound comprising a ring sulphamate system and a group of the formula where each of the R1 and R2 is selected regardless of alquenil h, alkyl, aryl, and cicloalquil,Or alquileno together represent optionally containing one or more heteroatoms or groups in the Chain alquilena; and where the compound is an inhibitor of an enzyme's activitySteroid sulfatase (e.c.3.1.6.2); and where the Group sulphamate Compound on the outside to be replaced with a sulfate Group to form a compound and incubated with a sulfated steroid sulfatase Enzyme(e.c.3.1.6.2) at a pH of 744 and 37 degrees C. it could have a value of km of less than 50 um. Pharmaceutical Composition and its use to inhibit steroid sulfatase activity in a subject.
机译:包含环氨基磺酸盐系统和下式的基团的化合物,其中R 1和R 2均被选择,而与亚烷基h,烷基,芳基和环氯喹啉基或alquileno一起任选地在链alquilena中含有一个或多个杂原子或基团;并且该化合物是酶活性的抑制剂类固醇硫酸酯酶(e.c.3.1.6.2);并且在外面用硫酸盐基团代替氨基磺酸盐化合物以形成化合物并与硫酸化的甾族硫酸酯酶(ec3.1.6.2)一起在744和37℃的pH下孵育的情况下,其值为小于50 um的km。药物组合物及其在受试者中抑制类固醇硫酸酯酶活性的用途。

著录项

  • 公开/公告号CL2000000642A1

    专利类型

  • 公开/公告日2001-02-05

    原文格式PDF

  • 申请/专利权人 STERIX LIMITED;

    申请/专利号CL2000000642

  • 申请日2000-03-17

  • 分类号A61K31/566;A61P35/00;C07J41/00;

  • 国家 CL

  • 入库时间 2022-08-22 01:25:51

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