Antitumoral18a-homoestra-1,3,5(10)-trien-3yl 2-substituted sulfamates
    5.
    发明申请
    Antitumoral18a-homoestra-1,3,5(10)-trien-3yl 2-substituted sulfamates 审中-公开
    抗肿瘤剂18a-高丝氨酸-1,3,5(10) - 三烯-3-基2-取代的氨基磺酸盐

    公开(公告)号:US20060211670A1

    公开(公告)日:2006-09-21

    申请号:US10546025

    申请日:2004-02-19

    IPC分类号: A61K31/56 C07J1/00

    摘要: The invention relates to the use of compounds of a general formula (I), wherein R2, R14 to R17 and X groups have the following significance: R2 is C1-C5-Alkyl, C1-C5-Alkoxy or a —O—C N FmHo rest, wherein n=1,2,3,4,5 or 6, m>1 and m+o=2n+1, R14 and R15 separately designate hydrogen or together a methyl group or a supplementary liaison, R16 is hydrogen; R17 is hydrogen, hydroxy, C1-C5-Alkyl, C1-C5-Alkoxy or SO3NHX; X is hydrogen, C1-C5-alkyl or C1-C5 acyl. In the cycle B and D of a steroid skeleton, stippled lines can additionally represent up to two double bonds. The salts of said compounds which are pharmaceutically acceptable for preparing a drug are also disclosed.

    摘要翻译: 本发明涉及通式(I)的化合物的用途,其中R 2,R 14与R 17和X基团具有 具有以下含义:R 2为C 1 -C 5 - 烷基,C 1 -C 5 - 烷氧基或-OC 1 H 3 - n = 1,2,3,4,5或6,m> 1和m + o = 2n + 1,R14和R15分别表示氢或一起形成甲基或辅助连接,R 16是氢; R 17是氢,羟基,C 1 -C 5 - 烷基,C 1 -C 5 - 烷氧基或SO 3 NHX; X是氢,C 1 -C 5 - 烷基或C 1 -C 5酰基。 在类固醇骨架的循环B和D中,点划线可以另外代表多达两个双键。 还公开了用于制备药物药学上可接受的所述化合物的盐。

    New 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1

    公开(公告)号:US20060009434A1

    公开(公告)日:2006-01-12

    申请号:US11154947

    申请日:2005-06-17

    IPC分类号: A61K31/57 C07J1/00

    CPC分类号: C07J1/00

    摘要: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of general formula I in which R2 means a saturated or unsaturated C1-C8-alkyl group, a C1-C5-alkyloxy group, an aralkyl radical or alkylaryl radical, a radical —O—CnFmHo, whereby n=1, 2, 3, 4, 5 or 6, m≧1 and m+o=2n+1, or a group CH2XY, in which X stands for an oxygen atom and Y stands for an alkyl radical with 1 to 4 carbon atoms, as well as a halogen atom or a nitrile group, R13 means a hydrogen atom or a methyl group, R16 means a hydrogen atom or a fluorine atom, Z means an oxygen atom or a sulfur atom, R3 and R5, in each case independently of one another, mean an α- or β-position hydrogen atom, R4 and R6, in each case independently of one another, mean an α- or β-position hydrogen atom, a C1-C5-alkyl group, a C1-C5-alkyloxy group, a C1-C5-acyl group or a hydroxy group or an aralkyl radical or alkylaryl radical, R3 and R4 together mean an oxygen atom, R5 and R6 together mean an oxygen atom, R7 and R8 in each case mean a hydrogen atom or together a CH2 group, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.