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    17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase inhibitors
    5.
    发明授权
    17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase inhibitors 失效
    17-烷基-7-取代-4-氮杂类固醇衍生物作为5-α-还原酶抑制剂

    公开(公告)号：US5763361A

    公开(公告)日：1998-06-09

    申请号：US734705

    申请日：1996-10-21

    申请人： Georgianna Harris ,  Richard L. Tolman ,  Soumya P. Sahoo

    发明人： Georgianna Harris ,  Richard L. Tolman ,  Soumya P. Sahoo

    IPC分类号： C07J73/00 ,  A61K31/58

    CPC分类号： C07J73/005

    摘要： The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula I are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostafic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I. The use of compounds of formula I in combination with other, active agents, for example with a 5.alpha.-reductase type 2 inhibitor such as finasteride or epristeride, or a potassium channel opener, such as minoxidil, or a retinoic acid or a derivative thereof is also taught, wherein such combinations would be useful in one or more of the above-mentioned methods of treatment or pharmaceutical compositions.

    摘要翻译： 本发明的新化合物是结构式I的化合物：其中（I）化合物或其药学上可接受的盐或立体异构体，其为5α-还原酶，特别是5型α-还原酶1型的抑制剂。 式I可用于全身，包括口服或肠胃外或局部治疗高雄性性疾病，如寻常痤疮，皮脂溢，雄激素性脱发，包括女性和男性型秃发，女性多毛症，良性前列腺增生，以及预防和治疗前列腺 癌，以及前列腺炎的治疗。 使用式I化合物治疗高雄激素病症如寻常痤疮，皮脂溢，雄激素性脱发，男性型秃发，女性多毛症，良性前列腺增生以及预防和治疗前列腺癌的方法，以及治疗 提供前列腺炎，以及用于式I化合物的药物组合物。式I化合物与其它活性剂，例如5α-还原酶2抑制剂如非那雄胺或艾美他啶的组合或 钾通道开放剂如米诺地尔或视黄酸或其衍生物也被教导，其中这些组合可用于一种或多种上述治疗方法或药物组合物。

    Treatment of hyperandrogenic conditions
    8.
    发明授权
    Treatment of hyperandrogenic conditions 失效
    治疗雄激素过多症状

    公开(公告)号：US5756480A

    公开(公告)日：1998-05-26

    申请号：US738546

    申请日：1996-10-24

    申请人： Herb G. Bull ,  Georgianna Harris ,  Robert W. Myers

    发明人： Herb G. Bull ,  Georgianna Harris ,  Robert W. Myers

    IPC分类号： C07H19/04 ,  C07H19/048 ,  A61K31/705

    CPC分类号： A61K31/7076

    摘要： The invention concerns the treatment of hyperandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5.alpha.-reductase enzymes from 3-oxo-4-oxa end 4-thiasteroids having a 1,2-double bond and the pyridine-nucleotide cofactor of the 5.alpha.-reductase enzyme, NADPH. The invention further relates to the isolated inhibitor-cofactor complex.

    摘要翻译： 本发明涉及通过从具有1,2-双键的3-氧代-4-氧杂末端4-硫代甾烷醇形成人类5α-还原酶的基于机制的新型不可逆抑制剂来治疗人类中雄激素过多的病症， 5α-还原酶，NADPH的吡啶核苷酸辅因子。 本发明还涉及分离的抑制剂 - 辅因子复合物。