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    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter
    2.
    发明申请
    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter 失效
    18-甲基-19-去甲-17-孕-4-烯-21,17-碳内酯，以及含有后者的药物制剂

    公开(公告)号：US20060252737A1

    公开(公告)日：2006-11-09

    申请号：US11321449

    申请日：2005-12-30

    申请人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    发明人： Rolf Bohlmann ,  Dieter Bittler ,  Hermann Kuenzer ,  Peter Esperling ,  Hans-Peter Muhn ,  Karl-Heinrich Fritzemeier ,  Ulrike Fuhrmann ,  Katja Prelle ,  Steffen Borden

    IPC分类号： A61K31/58 ,  C07J19/00

    CPC分类号： C07J19/00

    摘要： This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ═NOR or ═NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in α- or β-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an α- or β-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an α- or β-position methylene group or an additional bond. The new compounds have gestagenic and anti-mineralocorticoid action and are suitable for the production of pharmaceutical preparations, for example for oral contraception and the treatment of pre-, peri- and post-menopausal symptoms.

    摘要翻译： 本发明描述了通式I的新的18-甲基-19-去甲-17-孕甾-4-烯-21,17-碳内酯，其中Z表示氧原子，两个氢原子，-NOR或-NNHSO- R 2是氢原子或具有1至4或3至4个碳原子的直链或支链烷基，R 4是氢原子 ，卤素原子，甲基或三氟甲基，R 6和/或R 7可以是α-或β-位，并且独立地为一个 另一个是指具有1至4或3至4个碳原子的直链或支链烷基，或R 6表示氢原子，R 7表示 具有1至4或3至4个碳原子的α-或β-位的直链或支链烷基，或R 6和R 7各自表示 氢原子或R 6和R 7一起是指α-或β-位亚甲基或另外的键。 新化合物具有孕激素和抗盐皮质激素的作用，并且适用于制备药物制剂，例如用于口服避孕和治疗绝经前，绝经期和绝经后症状。

    Nonsteroidal progesterone receptor modulators
    4.
    发明授权
    Nonsteroidal progesterone receptor modulators 失效
    非甾体孕激素受体调节剂

    公开(公告)号：US07408060B2

    公开(公告)日：2008-08-05

    申请号：US11473336

    申请日：2006-06-23

    申请人： Norbert Schmees ,  Ulrich Bothe ,  Wolfgang Schwede ,  Carsten Moeller ,  Ulrike Fuhrmann ,  Anja Schmidt

    发明人： Norbert Schmees ,  Ulrich Bothe ,  Wolfgang Schwede ,  Carsten Moeller ,  Ulrike Fuhrmann ,  Anja Schmidt

    IPC分类号： C07D265/02 ,  C07D265/00 ,  C07D305/12

    CPC分类号： C07D307/88 ,  C07D307/94 ,  C07D407/12

    摘要： This invention relates to nonsteroidal progesterone receptor modulators of general formula I, a process for their production, the use of progesterone receptor modulators for the production of pharmaceutical agents as well as pharmaceutical compositions that contain these compounds. The compounds according to the invention are suitable for therapy and prophylaxis of gynecological diseases, such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhea, as well as for the therapy and prophylaxis of hormone-dependent tumors and for use for female birth control as well as for hormone replacement therapy.

    摘要翻译： 本发明涉及通式I的非甾体孕激素受体调节剂，其制备方法，使用孕酮受体调节剂制备药剂以及含有这些化合物的药物组合物。 根据本发明的化合物适用于治疗和预防妇科疾病，例如子宫内膜异位症，子宫平滑肌瘤，功能障碍性出血和痛经，以及用于治疗和预防激素依赖性肿瘤并用于女性避孕 以及激素替代疗法。

    Composition comprising progesterone-receptor antagonists and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases
    5.
    发明申请
    Composition comprising progesterone-receptor antagonists and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases 审中-公开
    包含孕酮受体拮抗剂和用于预防和治疗激素依赖性疾病的纯抗雌激素的组合物

    公开(公告)号：US20050014736A1

    公开(公告)日：2005-01-20

    申请号：US10854761

    申请日：2004-05-27

    申请人： Ulrike Fuhrmann ,  Jens Hoffmann ,  Martin Schneider ,  Gerhard Siemeister

    发明人： Ulrike Fuhrmann ,  Jens Hoffmann ,  Martin Schneider ,  Gerhard Siemeister

    IPC分类号： A61K31/567 ,  A61K31/573 ,  A61K45/06 ,  A61P5/32 ,  A61P5/36 ,  A61K31/56

    CPC分类号： A61K31/567 ,  A61K31/573 ,  A61K45/06

    摘要： The present invention relates to methods and uses for preventing or treating hormone-dependent diseases, in particular breast cancer, in a mammal, by a combination of an progesterone-receptor antagonist, in particular the progesterone-receptor antagonist 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, and a pure antiestrogen, in particular a compound of general formula I as defined in the specification, for instance 11β-Fluoro-17α-methyl-7α-{5-[methyl(8,8,9,9,9-pentafluorononyl)amino]pentyl}-estra-1,3,5(10)-triene-3,17β-diol. The invention further relates to pharmaceutical compositions comprising said combination.

    摘要翻译： 本发明涉及用于预防或治疗哺乳动物中的激素依赖性疾病，特别是乳腺癌的方法和用途，其通过孕酮 - 受体拮抗剂，特别是孕酮 - 受体拮抗剂11beta-（4-乙酰基苯基） -17β-羟基-17α-（1,1,2,2,2-五氟乙基） - 雌-4,9-二烯-3-酮或其药学上可接受的衍生物或类似物，和纯抗雌激素，特别是化合物 如本说明书中定义的通式I，例如11b-氟-17α-甲基-7α-{5- [甲基（8,8,9,9,9-五氟壬基）氨基]戊基} - 雌-1,3 ，5（10） - 三烯-3,17β-二醇。 本发明还涉及包含所述组合的药物组合物。