Glucocorticoids
    4.
    发明授权
    Glucocorticoids 失效
    糖皮质激素

    公开(公告)号:US5616573A

    公开(公告)日:1997-04-01

    申请号:US530352

    申请日:1995-10-06

    CPC分类号: C07J41/005 C07J43/003

    摘要: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.

    摘要翻译: PCT No.PCT / EP94 / 00937 371日期1995年10月6日 102(e)日期1995年10月6日PCT 1994年3月24日PCT公布。 出版物WO94 / 22898 日期:1994年10月13日描述了通式IR-Val-O-GC(II)的糖皮质激素,其中O-GC是具有抗炎作用的21-羟基皮质激素的基团,Val表示21位的缬氨酸基团 皮质激素和R表示氢原子或具有多至32个碳原子的烃基,其任选被羟基,氨基,氧代基和/或卤素原子取代和/或被氧原子,SO2基团和 /或NH基及其盐。

    14.alpha., 16.alpha.-ethanoand 14.alpha., 16.alpha.-etheno-estratrienes
    7.
    发明授权
    14.alpha., 16.alpha.-ethanoand 14.alpha., 16.alpha.-etheno-estratrienes 失效
    14α,16α-乙基和14α,16α-异 - 异三烯

    公开(公告)号:US5439902A

    公开(公告)日:1995-08-08

    申请号:US140053

    申请日:1994-03-18

    CPC分类号: C07J53/002

    摘要: The new 14.alpha.,16.alpha.-ethano- and 14.alpha.,16.alpha.-etheno-estratrienes of general formula I, ##STR1## are described, in which A-B means a C-C single bond or C-C double bond,R.sub.1 means a hydrogen atom, a methyl or acyl group with 1-12 carbon atoms andX means oxygen or ##STR2## in which R.sub.2 represents a hydrogen atom or an acyl group with 1-12 carbon atoms,and a process for their production. The new compounds are very strong estrogens and are suitable for the production of pharmaceutical agents.

    摘要翻译: PCT No.PCT / EP92 / 00945 Sec。 371日期:1994年3月18日 102(e)1994年3月18日PCT提交1992年4月30日PCT公布。 WO92 / 19641 PCT出版物 日期为1992年11月12日。描述了通式I,IMAGE(I)的新的14α,16α-乙烯和14α,16α-异 - 异三烯,其中AB表示CC单键或 CC双键,R1表示氢原子,具有1-12个碳原子的甲基或酰基,X表示氧或,其中R2表示氢原子或具有1-12个碳原子的酰基, 为他们的生产。 新化合物是非常强的雌激素,适用于生产药剂。

    18-nor steroids as selectively active estrogens
    10.
    发明申请
    18-nor steroids as selectively active estrogens 审中-公开
    18-或类固醇作为选择性活性雌激素

    公开(公告)号:US20050282791A1

    公开(公告)日:2005-12-22

    申请号:US11184784

    申请日:2005-07-20

    IPC分类号: A61K31/56 A61K31/58

    CPC分类号: C07J1/0051

    摘要: This invention describes the new 18-nor steroids (gonatrienes) of general formula (I), in which R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15, R16, R17 and R17′ have the meanings that are indicated in the description, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo a preferential action on bone in comparison to the uterus, and/or pronounced action relative to the stimulation of the expression of 5HT2a-receptors and transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention further describes the use of steroids, on which the gonatriene skeleton is based, for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of the gonatriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bone in comparison to the uterus.

    摘要翻译: 本发明描述了通式(I)的新的18-或类固醇(高碳二烯),其中R 1,R 2,R 3,R 3, R 6,R 7,R 8,R 9,R 11, ,R 11,R 14,R 15,R 15,R 16, R 17和R 17具有在说明书中指出的含义,作为具有体外对大鼠前列腺的雌激素受体制剂具有更高亲和力的药物活性成分 而不是雌激素受体制剂的大鼠子宫和体内与子宫相比优于骨骼的优势,和/或相对于刺激5HT2a受体和转运蛋白表达的显着作用,其生产,其治疗用途和药物分配 包含新化合物的形式。 本发明进一步描述了用于治疗雌激素缺乏诱导的疾病和病症以及在有兴趣解离的化合物的总体结构中使用三烯结构部分的用途, 与子宫相比,它们对骨骼的雌激素作用。