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    Use of biogenic estrogen sulfamates for hormone replacement therapy
    5.
    发明授权
    Use of biogenic estrogen sulfamates for hormone replacement therapy 有权
    使用生物源性雌激素氨基磺酸盐治疗激素替代疗法

    公开(公告)号：US07053077B1

    公开(公告)日：2006-05-30

    申请号：US09744574

    申请日：1999-05-13

    申请人： Walter Elger ,  Pekka Lähteenmäki ,  Matti Lehtinen ,  Gudrun Reddersen ,  Holger Zimmermann ,  Michael Oettel ,  Sigfrid Schwarz

    发明人： Walter Elger ,  Pekka Lähteenmäki ,  Matti Lehtinen ,  Gudrun Reddersen ,  Holger Zimmermann ,  Michael Oettel ,  Sigfrid Schwarz

    IPC分类号： A61K31/56

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/57 ,  Y10S514/874 ,  A61K2300/00

    摘要： The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.

    摘要翻译： 本发明涉及用于激素替代治疗（HRT）的口服不连续应用的生物源性雌激素氨基磺酸盐的用途。 不连续给药时间间隔为2至40天。 本发明还提供了孕妇的额外应用，优选连续地以植入物的形式或以子宫内释放系统（IUD）的形式。 氨基磺酸氨基磺酸酯，氨基磺酸雌二醇酯或酰基链中具有至多7个C原子的雌酮，雌二醇或雌三醇的N-酰基氨基磺酸酯或由两种或更多种所述活性成分组成的组合物用作生物来源的雌激素亚磺酸盐。

    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS
    8.
    发明申请
    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
    具有磺酰胺基团的化合物和含有这些化合物的药物组合物

    公开(公告)号：US20090023896A1

    公开(公告)日：2009-01-22

    申请号：US12142332

    申请日：2008-06-19

    申请人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    发明人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    IPC分类号： C07K7/06 ,  C07J1/00

    CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

    摘要： This invention relates to compounds that as prodrugs and/or vehicles make it possible for an active ingredient to be taken up into erythrocytes and/or an active ingredient to bind to erythrocytes, whereby the uptake of the compounds into erythrocytes and/or the binding of the compounds to erythrocytes is made possible by a group —SO2NR1R2, whereby R1 and R2, independently of one another, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. By the prodrugs according to the invention, active ingredients, such as endogenous substances, natural substances and synthetic substances with therapeutically valuable properties with a high “first pass” effect are made available orally to a reasonable extent or are decisively improved relative to oral activity.

    摘要翻译： 本发明涉及作为前药和/或载体的化合物，使活性成分能够摄入红细胞和/或活性成分以结合红细胞，由此将化合物摄入红细胞和/或结合 对于红细胞的化合物可以通过基团-SO 2 NR 1 R 2来实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基，环烷基，芳基，氰基或羟基 组。 通过根据本发明的前药，可以以合理的方式口服提供活性成分，例如内源物质，天然物质和具有高“第一道”效果的治疗有价值的性质的合成物质，或者相对于口服活性而言是有显着改善的。

    Compounds with sulphonamide group and pharmaceutical compositions containing these compounds
    9.
    发明授权
    Compounds with sulphonamide group and pharmaceutical compositions containing these compounds 失效
    具有磺酰胺基团的化合物和含有这些化合物的药物组合物

    公开(公告)号：US07507725B2

    公开(公告)日：2009-03-24

    申请号：US10296973

    申请日：2001-05-08

    申请人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    发明人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    IPC分类号： A61K31/56

    CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

    摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.

    摘要翻译： 本发明涉及作为前药和/或支持物的化合物，使活性剂能够被红细胞和/或活性剂吸收以结合红细胞。 这些化合物通过和/或其与红细胞的结合的吸收通过式-SO 2 NR 1 R 2的基团可以实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基， 环烷基，芳基，氰基或羟基。 本发明的前药使得具有高“第一途径”效果的具有治疗有用性质的内源性物质，天然物质和合成物质等活性剂能够有效口服或显着改善其口服活性。