17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase
inhibitors
    1.
    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

    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。

    4-Azasteroids for treatment of hyperandrogenic conditions
    4.
    再颁专利
    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:USRE39056E1

    公开(公告)日:2006-04-04

    申请号:US10020740

    申请日:1996-09-11

    CPC分类号: C07J73/005 A61K31/435

    摘要: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-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: 结构式(I)的化合物及其药理学上可接受的盐和酯具有5α-还原酶抑制活性。 这些化合物抑制1型和2型5α-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症状,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(也称雄激素性脱发),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-Azasteroids for treatment of hyperandrogenic conditions
    10.
    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。