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    Antitumoral18a-homoestra-1,3,5(10)-trien-3yl 2-substituted sulfamates
    1.
    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

    申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Eberhard Unger ,  Ina Scherlitz-Hofmann ,  Wilko Regenhardt

    发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Eberhard Unger ,  Ina Scherlitz-Hofmann ,  Wilko Regenhardt

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： C07J41/00 ,  A61K31/565 ,  C07J31/00

    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。

    Antitumoral D-homoestra-1,3,5(10)-trien-3-yl 2-substituted sulfamates
    6.
    再颁专利
    Antitumoral D-homoestra-1,3,5(10)-trien-3-yl 2-substituted sulfamates 失效
    抗肿瘤D-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：USRE42132E1

    公开(公告)日：2011-02-08

    申请号：US12351271

    申请日：2004-02-19

    申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Eberhard Unger ,  Bernd Menzenbach

    发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Gerhard Siemeister ,  Eberhard Unger ,  Bernd Menzenbach

    IPC分类号： A61K31/565 ,  C07J31/00 ,  C07J41/00 ,  A61P35/00

    CPC分类号： C07J63/00

    摘要： This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homo-substitution. They have a special action with respect to tubulin polymerization inhibition and can be used, for example, for treating prostate cancer

    摘要翻译： 本发明涉及通式I（I）的2-取代的D-均 - 雌-1,3,5（10） - 三烯-3-基氨基磺酸酯，其中R 3表示C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基以及它们用于生产用于治疗肿瘤疾病的药剂的用途，其可通过抑制微管蛋白聚合而受到积极的影响。 根据本发明的化合物通过D-均取代来区分。 它们在微管蛋白聚合抑制方面具有特殊的作用，可用于例如治疗前列腺癌

    Antitumor-active 2-alkoxyestradiol sulfamates
    7.
    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。

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

    公开(公告)号：US20060009434A1

    公开(公告)日：2006-01-12

    申请号：US11154947

    申请日：2005-06-17

    申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller

    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.