17alpha-fluorosteroids, pharmaceutical compositions containing 17alpha-fluorosteroids and a method of making them
    2.
    发明申请
    17alpha-fluorosteroids, pharmaceutical compositions containing 17alpha-fluorosteroids and a method of making them 失效
    17α-含氟类固醇,含有17α-荧光素的药物组合物及其制备方法

    公开(公告)号:US20050234027A1

    公开(公告)日:2005-10-20

    申请号:US11104736

    申请日:2005-04-13

    IPC分类号: A61K31/57 C07J3/00

    CPC分类号: C07J3/00

    摘要: New 17α-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5α-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.

    摘要翻译: 公开了式(I)的新的17α-荧光素类化合物:其中R 1表示H或甲基; R 2和R 3各自表示H,Cl或甲基; 并且分别存在于类固醇环体系的C-6和C-7之间以及C-9和C-10之间的双键或单键。 这些化合物具有混合特征的活性谱,因此它们作为5α-还原酶的抑制剂和作为高效力的孕激素。 公开了含有它们的药物组合物。 它们适用于治疗由器官和组织中高水平雄激素引起的病症。 这些新化合物可以与其他荷尔蒙物质(如雌激素,睾酮和其他雄激素)一起使用,作为避孕药具和其他应用。

    Methylene-4-azasteroids
    4.
    发明授权
    Methylene-4-azasteroids 失效
    亚甲基-4-azasteroids

    公开(公告)号:US07186728B2

    公开(公告)日:2007-03-06

    申请号:US10487862

    申请日:2002-08-28

    IPC分类号: A61K31/473 C07D221/18

    CPC分类号: C07J73/005

    摘要: 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl group, and R1 and R2 each denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.

    摘要翻译: 式I的17-亚甲基-4-氮杂甾族化合物:其中R 20表示氟,氯或溴R 20a表示氢,R 10和 R 4各自表示氢原子或甲基,R 1和R 2各自表示氢原子或一起表示附加键 可用于治疗由过度雄激素水平引起的疾病或病症,如痤疮,前列腺疾病,脱发和多毛症以及妇科病症。 描述了合成新的17-亚甲基-4-氮杂甾族化合物的方法。