18-Methyl-19-norandrost-4-ene 17, 17-spiro ether (18-methyl-19-nor-20-spirox-4-en-3-one), and pharmaceutical products comprising the same
    3.
    发明申请
    18-Methyl-19-norandrost-4-ene 17, 17-spiro ether (18-methyl-19-nor-20-spirox-4-en-3-one), and pharmaceutical products comprising the same 有权
    18-甲基-19-去雄甾-4-烯17,17-螺醚(18-甲基-19-去甲-20-螺-4-烯-3-酮)和包含它们的药物

    公开(公告)号:US20080153787A1

    公开(公告)日:2008-06-26

    申请号:US11769952

    申请日:2007-06-28

    IPC分类号: A61K31/58 C07J71/00

    CPC分类号: C07J53/008

    摘要: The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ═NOR or ═NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have a or a configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.

    摘要翻译: 本发明描述了通式I的新颖的18-甲基-19-壬二酸-4-烯17,17-螺醚,其中Z是氧原子,两个氢原子,-NOR或-NNHSO - 2 R,其中R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 原子或三氟甲基,R 6和/或R 7可以具有或其结构,并且R 6和R 6可以是 7个彼此独立地为氢原子或具有1至4或3至4个碳原子的直链或支链烷基或具有2至4或3至4个碳原子的直链或支链烯基 4个碳原子或3〜5个碳原子的饱和环烷基或一起是亚甲基或双键。 新化合物具有促孕和抗皮质激素活性。

    17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE
    8.
    发明申请
    17Beta-CYANO-19-NOR-ANDROST-4-ENE DERIVATIVE, ITS USE AND MEDICAMENTS COMPRISING THE DERIVATIVE 失效
    17Beta-CYANO-19-NOR-ANDROST-4-ENE衍生物,其使用和药物包含衍生物

    公开(公告)号:US20090048217A1

    公开(公告)日:2009-02-19

    申请号:US12137111

    申请日:2008-06-11

    IPC分类号: A61K31/567 C07J3/00 A61P5/24

    摘要: The 17β-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7, R9, R10 are hydrogen or are omitted with formation of a double bond between C9 and C10, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, where at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 is unequal to hydrogen or R6b and R7 are omitted with formation of a double bond between C6 and C7, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts.

    摘要翻译: 本发明的17β-氰基-19-去甲 - 雄甾-4-烯衍生物具有孕激活作用。 它们具有一般化学式1,其中Z选自O,两个氢原子,NOR和NNHSO 2 R,其中R是氢或C 1 -C 4 - 烷基,R 4是氢或卤素,此外:R 6a, R6b一起形成亚甲基或1,2-乙二基或R6a为氢,R6b选自氢,甲基和羟基亚甲基,R7选自氢,C1-C4-烷基,C2-C3-烯基和 环丙基,或者:R6a是氢,R6b和R7一起形成亚甲基,或者在C6和C7之间形成双键被省略,R9,R10是氢或在C9与C10之间形成R15,R16 是氢或一起形成亚甲基,R 17选自氢,C 1 -C 4 - 烷基和烯丙基,其中至少一个取代基R4,R6a,R6b,R7,R15,R16和R17不等于氢或R6b 并且在C6和C7之间形成双键而省略R7,此外, 上升它们的溶剂合物,水合物,立体异构体,非对映异构体,对映体和盐。

    18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter
    9.
    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

    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。