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    Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same
    7.
    发明授权
    Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same 失效
    用于治疗雌激素依赖性疾病的化合物及其制备和使用方法

    公开(公告)号：US06288107B1

    公开(公告)日：2001-09-11

    申请号：US09536331

    申请日：2000-03-24

    申请人： Pui-Kai Li ,  Kyle W. Selcer

    发明人： Pui-Kai Li ,  Kyle W. Selcer

    IPC分类号： A61K3138

    CPC分类号： C07C307/02

    摘要： Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

    摘要翻译： 公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂/雌激素受体阻断剂化合物。 化合物通常包含氨基磺酸酯部分和芳族的雌激素受体阻断剂部分。 还公开了合成这些化合物并将其用于治疗和/或预防性治疗雌激素依赖性疾病的方法。

    Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
    8.
    发明授权
    Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use 失效
    雌1,3,5（10）三烯-17-酮，3-氨基化合物的衍生物及其用途

    公开(公告)号：US5866603A

    公开(公告)日：1999-02-02

    申请号：US476360

    申请日：1995-06-07

    申请人： Pui-Kai Li ,  Kyle W. Selcer

    发明人： Pui-Kai Li ,  Kyle W. Selcer

    IPC分类号： C07J41/00

    CPC分类号： C07J41/0005

    摘要： This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

    摘要翻译： 本发明公开了可用作类固醇硫酸酯酶抑制剂的化合物。 化合物包括式（1）其中（a）R选自氢，低级烷基，烷氧基，卤素，NH 2，NO 2，C 3 N 3，N = C = S; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄甾酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 化合物还包括式（5）其中（a）R 1是氢，R 2选自SO 2 CF 3，SO 2 NH 2，SO 2（C 1 -C 6烷基），COCF 3，CONH 2，CO（ C 1 -C 6 - 烷基）; 环系ABCD是选自雌酮，脱氢表雄酮，雌二醇，雌二醇，孕烯醇酮，取代的雌酮，取代的脱氢表雄酮，取代的雌二醇，取代的雌二醇酯和取代的孕烯醇酮的类固醇核。 本发明还公开了用本发明化合物治疗和预防性治疗雌激素依赖性疾病的方法。