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    KOMBINATIONSPRÄPARATE AUS EINEM ER-BETA-SELEKTIVEN ESTROGEN UND EINEM SERM ODER ANTIESTROGEN
    3.
    发明公开
    KOMBINATIONSPRÄPARATE AUS EINEM ER-BETA-SELEKTIVEN ESTROGEN UND EINEM SERM ODER ANTIESTROGEN 审中-公开
    复方制剂从ER-β选择性雌激素和SERM

    公开(公告)号：EP1307229A1

    公开(公告)日：2003-05-07

    申请号：EP01974107.3

    申请日：2001-08-03

    申请人： Schering Aktiengesellschaft

    发明人： FRITZEMEIER, Karl-Heinrich ,  KOLLENKIRCHEN, Uwe ,  HEGELE-HARTUNG, Christa

    IPC分类号： A61K45/06

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/565

    摘要： A novel medicament for the treatment of estrogen-deficient disease states is disclosed. Said medicament is a combination preparation comprising an ERß-selective estrogen and an ERα-selective antiestrogen or SERM (Selective Estrogen Receptor Modulator). The antiestrogen or SERM which is a component of the combination preparation is preferably selective for the periphery. The preparation is suitable for an organ-specific estrogen therapy and has clear advantages over conventional therapies. Due to the combination of ERα-selective SERM and ERß-estrogen the preparation permits a complete protection against bone loss caused by estrogen deficiency. The components of the medicament also have a synergistic effect with respect to the inhibition of inflammation inducing genes, in particular in inflammatory disorders such as atherosclerosis and arthritis, or neurodegenerative diseases such as Alzheimers and multiple sclerosis. Furthermore, positive effects on cognition and mood may be expected. The protective estrogen-like effects are achieved, with no expectation of proliferation effects on breasts or uterus.

    11$g(b)-ARYLSUBSTITUIERTE 14,17-ETHANO ESTRATRIENE, VERFAHREN ZUR HERSTELLUNG DIESER VERBINDUNGEN, SOWIE IHRE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
    6.
    发明公开
    11$g(b)-ARYLSUBSTITUIERTE 14,17-ETHANO ESTRATRIENE, VERFAHREN ZUR HERSTELLUNG DIESER VERBINDUNGEN, SOWIE IHRE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN 失效
    11 $克（b）中的芳基取代的14,17-乙醇雌三烯，PROCESS用于生产这些化合物，以及它们在药物的生产

    公开(公告)号：EP0986574A1

    公开(公告)日：2000-03-22

    申请号：EP98937433.5

    申请日：1998-06-02

    申请人： Schering Aktiengesellschaft

    发明人： BOHLMANN, Rolf ,  FRITZEMEIER, Karl-Heinrich ,  HEGELE-HARTUNG, Christa ,  KNAUTHE, Rudolf ,  PARZCYK, Karsten

    IPC分类号： C07J41/00 ,  A61K31/565 ,  C07J53/00

    CPC分类号： C07J41/0083 ,  C07J53/002

    摘要： The invention relates to 11β-aryl-substituted 14,17-ethano-oestratriens of general formula (I), in which R1 is a hydrogen atom, a C¿1?-C12-alkanoyl-, a benzoyl-, a straight-chain or branched C1-C12-alkyl-, a C3-C7-cycloalkyl- or a C4-C8-alkyl cycloalkyl group, which can all optionally be substituted; R?2¿ is a hydrogen atom or an optionally substituted C¿1?-C12-alkanoyl group; R?3¿ stands for a group in which n = 4, 5, 6, or 7; m = 0, 1 or 2; R4 or R5 are, independently of each other, a hydrogen atom or a straight-chain or branched, optionally substituted C¿1?-C8-alkyl group, which can also be partially or completely fluorinated, or R?4 and R5¿ together mean a methylene to pentamethylene group -(CH¿2?)p-(p=1-5); and R?6¿ is the same as R4 or R5, or is an optionally substituted aryl or aryl alkyl radical, whereby said alkyl radical can have up to 6 carbon atoms, and the aryl radical, on its own or in the aryl alkyl radical, is a 5 or 6-link monocyclic ring or a condensed 8-10-link ring system, and the aryl radical can have one or more heteroatoms selected from oxygen, nitrogen, and sulphur. The new compounds are selective oestrogens whose effect is tissue-selective. In particular, the oestrogenic effect occurs on bone, in the cardiovascular system and in the central nervous system. However, it has little or no oestrogenic effect on the uterus and the liver. The compounds are suitable for producing medicaments which are used in many indications (for example, for hormone replacement therapy, prevention and treatment of osteoporosis).

    8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
    7.
    发明授权
    8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE 有权
    8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5（10）-TRIENDERIVATE

    公开(公告)号：EP1272505B1

    公开(公告)日：2005-08-24

    申请号：EP01940331.0

    申请日：2001-04-12

    申请人： Schering Aktiengesellschaft

    发明人： PETERS, Olaf ,  BRAEUER, Nico ,  HILLISCH, Alexander ,  HEGELE-HARTUNG, Christa ,  FRITZEMEIER, Karl-Heinrich

    IPC分类号： C07J1/00 ,  A61K31/565 ,  C07J41/00 ,  A61P5/30

    CPC分类号： C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

    摘要： The present invention relates to the novel 8β-substituted estradienes of general formula (I), wherein R?2, R3, R6, R6", R7, R7", R14, R15, R15", R16, R16", R17 and R17"¿ have the meanings given in the description, R8 means a straight-chain or branched-chain, optionally partially or entirely halogenated alkyl or alkenyl radical having up to 5 carbon atoms, an ethynyl or prop-1-inyl radical and R11 means an n-pentyl- or n-hexyl radical. Said estradienes are used as pharmaceutical active agents which, in vitro, are provided with a higher affinity of estrogen receptor preparations of rat prostate than of estrogen receptor preparations of rat uterus and, in vivo, preferably act in a preferential contraceptive manner on the ovary without stimulating the uterus. The invention also relates to the production thereof, the therapeutic use thereof and pharmaceutical administration forms which contain the novel compounds. The invention further relates to the use of said compounds for male contraception and to the use of non-malignant or malignant proliferate diseases of the ovary, such as ovarian carcinoma or granulosa cell tumours for instance.

    摘要翻译： 本发明涉及通式（I）的新的8β-取代的雌甾烯，其中R 2，R 3，R 6，R 6“，R 7，R 7”，R 14，R 15，R 15“，R 16，R 16”，R 17和R 17 “具有在说明书中给出的含义，R 8表示具有至多5个碳原子的直链或支链，任选部分或完全卤化的烷基或烯基，乙炔基或丙-1-烯基，并且R 11表示 所述雌甾烯被用作药物活性剂，其在体外与大鼠子宫的雌激素受体制剂相比对大鼠前列腺的雌激素受体制剂具有较高的亲和力，并且在体内优选地 在不刺激子宫的情况下以优先避孕方式作用，本发明还涉及其生产，其治疗用途和含有该新化合物的药物给药形式，本发明进一步涉及所述化合物在雄性收缩期 例如卵巢癌或颗粒细胞瘤的非恶性或恶性增殖性疾病的应用。

    18-NOR-STEROIDE ALS SELEKTIV WIRKSAME ESTROGENE
    8.
    发明公开
    18-NOR-STEROIDE ALS SELEKTIV WIRKSAME ESTROGENE 有权
    18-NOR类固醇AS选择性有效的雌激素

    公开(公告)号：EP1226155A2

    公开(公告)日：2002-07-31

    申请号：EP00981233.0

    申请日：2000-11-02

    申请人： Schering Aktiengesellschaft

    发明人： HILLISCH, Alexander ,  BOIDOL, Werner ,  SCHWEDE, Wolfgang ,  ESPERLING, Peter ,  SAUER, Gerhard ,  HEGELE-HARTUNG, Christa ,  KOLLENKIRCHEN, Uwe ,  FRITZEMEIER, Karl-Heinrich

    IPC分类号： C07J1/00 ,  A61K31/565

    CPC分类号： C07J1/0062 ,  A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  C07J1/007 ,  C07J1/0088 ,  C07J1/0096

    摘要： The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R?1, R2, R3, R6, R7, R8, R9, R11, R11", R14, R15, R15", R16, R17 and R17"¿ have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus.