4-Azasteroids for treatment of hyperandrogenic conditions
    72.
    发明授权
    4-Azasteroids for treatment of hyperandrogenic conditions 失效
    4-Azasteroids用于治疗雄激素过多的病症

    公开(公告)号:US6001844A

    公开(公告)日:1999-12-14

    申请号:US029926

    申请日:1998-03-11

    CPC分类号: C07J73/005 A61K31/435

    摘要: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

    摘要翻译: PCT No.PCT / US96 / 14564 Sec。 371日期1998年3月11日 102(e)1998年3月11日PCT PCT 1996年9月11日PCT公布。 出版物WO97 / 10217 日期1997年3月20日结构式(I)及其药理学上可接受的盐和酯的化合物具有5种α-还原酶抑制活性。 这些化合物抑制1型和2型5型α-还原酶。结构式I的化合物可用于全身,包括口服和肠胃外,包括局部治疗和预防高雄激素病症,包括前列腺癌,良性前列腺增生症,寻常痤疮 ,皮脂溢,雄激素性脱发(也称为雄性激素性脱发),包括男性和女性型秃发,女性多毛症和前列腺炎。 一类本发明的化合物也是有效的抗雄激素。 本发明还涉及含有这些化合物的新型组合物,其用途及其制备方法。

    4-Oxa and 4-thia steroids
    73.
    发明授权
    4-Oxa and 4-thia steroids 失效
    4-Oxa和4-thia类固醇

    公开(公告)号:US5998464A

    公开(公告)日:1999-12-07

    申请号:US65112

    申请日:1998-04-23

    摘要: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.

    摘要翻译: PCT No.PCT / US96 / 16883 Sec。 371日期:1998年4月23日 102(e)1998年4月23日PCT PCT 1996年10月22日PCT公布。 出版物WO97 / 15564 日期1997年5月1日本发明化合物为结构式(I)的化合物,其中X为氧或硫。 公开了化合物在治疗雄激素过度症状中的药物组合物和使用方法。 此外,公开了化合物与其他活性剂如非那雄胺,米诺地尔和视黄酸或其衍生物的组合。

    4-oxa and 4-thia steriods
    75.
    发明授权
    4-oxa and 4-thia steriods 失效
    4-氧杂和4-硫杂异构体

    公开(公告)号:US5777134A

    公开(公告)日:1998-07-07

    申请号:US738545

    申请日:1996-10-24

    CPC分类号: C07D311/94 C07D335/04

    摘要: The novel compounds of the present invention are those of structural formula I: ##STR1## wherein X is selected from O and S, or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, and are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostatic 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 finasteride, 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X选自O和S,或其药学上可接受的盐,酯或立体异构体,并且是5α-还原酶的抑制剂。 式I化合物可用于口服,全身,胃肠外或局部治疗雄激素过多症状,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(例如与非那雄胺)或钾通道开放剂如米诺地尔或视黄酸组合使用或 还教导了其衍生物,其中这样的组合可用于一种或多种上述治疗方法或药物组合物。