发明授权
US5866603A 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
- 专利标题: Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
- 专利标题(中): 雌1,3,5(10)三烯-17-酮,3-氨基化合物的衍生物及其用途
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申请号: US476360申请日: 1995-06-07
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公开(公告)号: US5866603A公开(公告)日: 1999-02-02
- 发明人: Pui-Kai Li , Kyle W. Selcer
- 申请人: Pui-Kai Li , Kyle W. Selcer
- 申请人地址: PA Pittsburgh
- 专利权人: Duquesne University of the Holy Ghost
- 当前专利权人: Duquesne University of the Holy Ghost
- 当前专利权人地址: PA Pittsburgh
- 主分类号: C07J41/00
- IPC分类号: C07J41/00
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.
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