PREPARATION OF 6-OXA-8ALPHA-STEROID ESTROGEN ANALOGUES - A NEW GROUP OF UNNATURAL ESTROGENS AND THEIR USE IN MEDICINE
    2.
    发明申请
    PREPARATION OF 6-OXA-8ALPHA-STEROID ESTROGEN ANALOGUES - A NEW GROUP OF UNNATURAL ESTROGENS AND THEIR USE IN MEDICINE 审中-公开
    6-OXA-8ALPHA-STEROID雌激素类似物的制备 - 一组新的独特的雌激素及其在医学中的应用

    公开(公告)号:WO2009059806A3

    公开(公告)日:2009-10-29

    申请号:PCT/EP2008009619

    申请日:2008-11-10

    CPC classification number: C07J73/003

    Abstract: The invention is related to the area of new 6-Oxa-8a-steroid estrogen analogues and the synthesis of these new biological active steroid estrogen analogues, namely, to the preparation of 6-oxa-8a-steroid estrogens and their use as estrogen receptor modulators. These new estrogen analogues are ligands for estrogen receptors and as such may be useful for the treatment and prevention of a variety of conditions related to estrogen functioning. These conditions include bone and cartilage disorders, increased levels of LDL cholesterol, cardiovascular diseases, impairment of cognitive function, cerebral degeneration disorders, endometriosis and other types of inflammation, the metabolic syndrome, and cancer, in particular of the breast, uterus and prostate.

    Abstract translation: 本发明涉及新的6-Oxa-8a-类固醇雌激素类似物的面积和这些新的生物活性类固醇雌激素类似物的合成,即6-氧杂-8a类固醇雌激素的制备及其作为雌激素受体的用途 调制器。 这些新的雌激素类似物是雌激素受体的配体,因此可用于治疗和预防与雌激素功能相关的各种病症。 这些病症包括骨和软骨障碍,LDL胆固醇水平升高,心血管疾病,认知功能障碍,脑变性障碍,子宫内膜异位症和其他类型的炎症,代谢综合征和癌症,特别是乳腺,子宫和前列腺。

    PROCESS FOR THE PRODUCTION OF OXANDROLONE
    5.
    发明申请
    PROCESS FOR THE PRODUCTION OF OXANDROLONE 审中-公开
    生产氧杂丙酮的方法

    公开(公告)号:WO2004064722A3

    公开(公告)日:2004-11-18

    申请号:PCT/US0239673

    申请日:2002-12-11

    CPC classification number: C07D311/94 C07D311/78 C07J1/0037 C07J73/003

    Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17beta -hydroxy-17alpha -methyl-5 -androst-1-en-3-one; (b) hydroxylating the 17beta - hydroxy-17alpha -methyl-5alpha -androst-1-en-3-one to form 1alpha , 2alpha , 17beta -trihydroxy-17alpha - methylandrostan-3-one; (c) cleaving the 1alpha , 2alpha , 17beta -trihydroxy-17alpha -methylandrostan-3- one to form 17beta -hydroxy-17alpha -methyl-1-oxo-1,2,-seco-A-nor-5 -androstan-2-oic acid; and (d) reducing the 17beta -hydroxy-17 -methyl-1-oxo-1,2,-seco-A-nor-5alpha -androstan-2-oic acid to form oxandrolone.

    Abstract translation: 本发明涉及从mestanolone合成氧杂雄酮的方法。 该方法包括以下步骤:(a)氧化mestanolone以形成17β-羟基-17α-甲基-5-雄甾-1-烯-3-酮; (b)使17β-羟基-17α-甲基-5α-雄甾-1-烯-3-酮羟基化形成1α,2α,17β-三羟基-17α-甲基雄甾-3-酮; (c)切割1α,2α,17β-三羟基-17α-甲基雄甾烷-3-酮以形成17β-羟基-17α-甲基-1-氧代-1,2'-环十一碳-5-雄甾烷-2 - 酸; 和(d)还原17β-羟基-17-甲基-1-氧代-1,2, - 异-α-降-5α-雄烷-2-烯酸以形成氧雄龙。

    PROCESS FOR THE PRODUCTION OF 2-OXA-3-ONE ANDROSTANE DERIVATIVES
    6.
    发明申请
    PROCESS FOR THE PRODUCTION OF 2-OXA-3-ONE ANDROSTANE DERIVATIVES 审中-公开
    2-OXA-3-ONE安非他酮衍生物的生产方法

    公开(公告)号:WO2004074305A2

    公开(公告)日:2004-09-02

    申请号:PCT/US2004004548

    申请日:2004-02-13

    Inventor: PONDER GARRATT W

    CPC classification number: C07J73/003

    Abstract: The present invention relates to processes for the production of 2-oxa-3-one androstane derivatives. The processes comprise reacting a 3-one androstane derivative with ozone to form a 2-oxa-3-one androstane derivative.

    Abstract translation: 本发明涉及2-氧杂-3-酮雄甾烷衍生物的制备方法。 该方法包括使3-酮雄甾烷衍生物与臭氧反应以形成2-氧杂-3-酮的雄甾烷衍生物。

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