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    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS
    6.
    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。

    Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system
    8.
    发明授权
    Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system 失效
    用于治疗中枢神经系统雌激素缺乏症的药物制剂

    公开(公告)号：US06245756B1

    公开(公告)日：2001-06-12

    申请号：US09252726

    申请日：1999-02-19

    申请人： Vladimir Patchev ,  Michael Oettel ,  Sigfrid Schwarz ,  Ina Thieme ,  Wolfgang Roemer

    发明人： Vladimir Patchev ,  Michael Oettel ,  Sigfrid Schwarz ,  Ina Thieme ,  Wolfgang Roemer

    IPC分类号： A61K31566

    CPC分类号： A61K31/567 ,  A61K31/565

    摘要： Pharmaceutical preparations containing selected steroid compounds and methods of treating estrogen deficiency in the central nervous system (CNS) without influencing other organs or systems are described. These steroids have selective neurotropic estrogen-like transcription action in contrast to the systemically acting natural and synthetic estrogen compounds, such as 17&agr;-estradiol. The selected steroids surprisingly have a selective influence on the transcription estrogen-dependent gene in the CNS and cause changes of physiological parameters as well as CNS-specific transcription effects in the dosages used with no biological effects in reproductive system tissues. They have CNS specific transcription effects at those dosages at which neither 17 &bgr;-estradiol nor 17&agr;-estradiol had any action and the transcription estrogen-dependent gene in the CNS is not influenced by secondarily formed 17&bgr;-estradiol.

    摘要翻译： 描述了含有选择的类固醇化合物的药物制剂和治疗中枢神经系统（CNS）中雌激素缺乏症的方法，而不影响其他器官或系统。 与系统作用的天然和合成雌激素化合物（如17α-雌二醇）相比，这些类固醇具有选择性神经营养因子雌激素样转录作用。 所选择的类固醇令人惊奇地对CNS中的转录雌激素依赖性基因具有选择性影响，并且在生殖系统组织中没有生物效应的剂量中引起生理参数的变化以及CNS特异性转录效应。 它们在17β-雌二醇和17α-雌二醇都不具有任何作用的那些剂量下具有CNS特异性转录效应，并且CNS中的转录雌激素依赖性基因不受二次形成的17β-雌二醇的影响。

    Antitumor-active 2-alkoxyestradiol sulfamates
    9.
    发明授权
    Antitumor-active 2-alkoxyestradiol sulfamates 失效
    抗肿瘤活性2-烷氧基雌二醇亚磺酸盐

    公开(公告)号：US08026229B2

    公开(公告)日：2011-09-27

    申请号：US10217165

    申请日：2002-08-13

    申请人： Ina Scherlitz-Hofmann ,  Jens Hoffmann ,  Alexander Hillisch ,  Eberhard Unger ,  Tobias Neumann ,  Sigfrid Schwarz ,  Olaf Peters ,  Thomas Michel

    发明人： Ina Scherlitz-Hofmann ,  Jens Hoffmann ,  Alexander Hillisch ,  Eberhard Unger ,  Tobias Neumann ,  Sigfrid Schwarz ,  Olaf Peters ,  Thomas Michel

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： A61K31/565 ,  A61K31/56

    摘要： The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.

    摘要翻译： 本发明涉及通式Ⅰ的2-烷氧基雌激素亚磺酸盐的用途，其中R 1和R 2独立地表示H，甲基，C 1 -C 4酰基，苯甲酰基，R 3表示C 1 -C 4烷基或式C n F m H 0基团，其中n = 2，3，4，5或6，m≥1，m + o = 2n + 1，R4和R5各自表示H或一起为亚甲基或另外的双键，R6表示H，R7表示 OH，OC1-C4-烷基，OC1-C11-酰基或OSO2NR1R2，类固醇骨架的B和C环中的虚线另外代表多达两个双键，用于生产用于治疗肿瘤疾病的药物 这可以通过抑制微管蛋白聚合而受到积极的影响。 本发明化合物通过2-烷氧基取代与17-羟基取代相结合来区分。 它们在抑制微管蛋白聚合方面具有特殊的效果，并且可以用于例如前列腺癌的治疗。

    Compounds with sulphonamide group and pharmaceutical compositions containing these compounds
    10.
    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。