17.beta.-substituted 4-azaandrostane derivatives, pharmaceutical
compositions containing them and process for preparing same
    2.
    发明授权
    17.beta.-substituted 4-azaandrostane derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    17β-取代的4-氮杂雄甾烷衍生物,含有它们的药物组合物及其制备方法

    公开(公告)号:US5583138A

    公开(公告)日:1996-12-10

    申请号:US406920

    申请日:1995-03-23

    IPC分类号: A61K31/58 A61P5/00 C07J73/00

    CPC分类号: C07J73/005

    摘要: The invention relates to novel 17.beta.-substituted 4-azaandrostane derivatives of general formula (I), ##STR1## wherein R means hydrogen or a C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; orR.sup.1 and R.sup.2 together means an .alpha.,.omega.-alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom;n is 4, 5, 6 or 7; and--- bond line represents a single or double bond.Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general formula (I).The compounds of general formula (I) exert a 5.alpha.-reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseases, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.

    摘要翻译: PCT No.PCT / HU93 / 00058 Sec。 371日期:1995年3月23日 102(e)1995年3月23日PCT 1993年10月1日PCT PCT。 第WO94 / 07909号公报 日本1994年4月14日本发明涉及通式(I)的新型17β-取代的4-氮杂雄甾烷衍生物,其中R表示氢或C 1-3烷基; R1和R2相同或不同,代表氢或C1-4烷基,条件是只有在n高于5的情况下,两者均可表示氢; 或R 1和R 2一起是指含有5至7个碳原子的α,ω-亚烷基,所述亚烷基的末端碳原子与相同的环碳原子结合; n为4,5,6或7; 和+ E,uns --- + EE键线代表单键或双键。 此外,本发明涉及含有这些化合物的药物组合物以及制备通式(I)化合物的方法。 通式(I)的化合物发挥5α-还原酶抑制作用,因此它们可用于治疗所有疾病,其目的是减少组织二氢睾酮水平,例如良性前列腺增生,痤疮,皮脂溢 ,女性多毛症或雄激素性脱发。