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    PROCESS FOR THE PRODUCTION OF ESTETROL
    2.
    发明公开
    PROCESS FOR THE PRODUCTION OF ESTETROL 有权
    用于生产雌四醇

    公开(公告)号：EP2764008A1

    公开(公告)日：2014-08-13

    申请号：EP12778664.8

    申请日：2012-10-05

    Applicant: Estetra S.P.R.L.

    Inventor： PASCAL, Jean-Claude

    IPC: C07J75/00

    CPC classification number: C07J1/0066 ,  C07J51/00 ,  C07J75/00 ,  Y02P20/55

    Abstract: The present invention relates to a process for the preparation of a compound of formula (I), hydrates or solvates thereof; (I) said process comprising the steps of a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), (II) (III) wherein P
    1 is a protecting group selected from R
    1 CO-, or R
    2 Si(R
    3 )(R
    4 )-, P
    2 is a protecting group selected from (R
    6 R
    5 R
    7 )C-CO-, or (R
    2 )Si(R
    3 )(R
    4 )-, wherein R
    1 is a group selected from C
    1-6 alkyl or C
    3-6 cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C
    1-4 alkyl; R
    2 , R
    3 and R
    4 are each independently a group selected from C
    1-6 alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C
    1-4 alkyl; R
    5 is a group selected from C
    1-6 alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C
    1-4 alkyl; R
    6 and R
    7 are each independently hydrogen or a group selected from C
    1-6 alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C
    1-4 alkyl; b) reacting the compound of formula (III) in the presence of at least one oxidizing agent selected from permanganate salt, osmium oxide, hydrogen peroxide, or iodine and silver acetate to produce compound of formula (IV); and (IV)5 c) deprotecting the compound of formula (IV) to produce compound of formula (I).

    16-Hydroxyestratriene als selektiv wirksame Estrogene
    7.
    发明公开
    16-Hydroxyestratriene als selektiv wirksame Estrogene 审中-公开

    公开(公告)号：EP1580192A2

    公开(公告)日：2005-09-28

    申请号：EP05075149.4

    申请日：2000-02-09

    Applicant: Schering AG

    Inventor： Künzer, Hermann, Dr. ,  Knauthe, Rudolf, Dr. ,  Lessl, Monika, Dr. ,  Fritzemeier, Karl-Heinrich, Dr. ,  Hegele-Hartung, Christa, Dr. ,  Bömer, Ulf, Dr. ,  Müller, Gerd, Dr. ,  Kosemund, Dirk, Dr.

    IPC: C07J53/00 ,  C07J1/00 ,  A61K31/565 ,  C07J31/00 ,  C07J41/00 ,  C07J33/00 ,  C07J15/00

    CPC classification number: C07J41/0094 ,  C07J1/0055 ,  C07J1/0066 ,  C07J15/00 ,  C07J31/006 ,  C07J33/002 ,  C07J53/004

    Abstract: Die Erfindung beschreibt neue Verbindungen als pharmazeutische Wirkstoffe, die in vitro eine höhere Affinität an Estrogenrezeptorpräparationen von Rattenprostata als an Estrogenrezeptorpräparationen von Rattenuterus und in vivo eine präferentielle Wirkung am Knochen im Vergleich zum Uterus und/oder ausgeprägte Wirkung hinsichtlich Stimulierung der Expression von 5HT2a-Rezeptor und -transporter aufweisen, deren Herstellung, ihre therapeutische Anwendung und pharmazeutischen Darreichungsformen, die die neuen Verbindungen enthalten.
    Bei den neuen Verbindungen handelt es sich um 16α- und 16β-Hydroxy-estra,1,3,5(10)-estratriene, die am Steroid-Gerüst weitere Substituenten tragen sowie in den B-, C-und/oder D-Ringen eine oder mehrere zusätzliche Doppelbindungen aufweisen können.

    Abstract translation: 3,16-二羟基-1,3,5（10） - 三亚甲基衍生物（I）是新的。 式（I）的3,16-二羟基-1,3,5（10） - 三亚甲基衍生物是新的：[Image]环中的粗黑线=单键或双键; R 1> H，卤素，OH，Me，CF 3，OMe或OEt; R 2> H，卤素，OH或1-6C任选饱和的烷氧基; R 4> H，卤素，1-10C任选饱和的烷基，CF 3，C 2 F 5或1-6 C任选饱和的烷氧基; R 7> H，卤素，1-10C任选饱和的烷基（任选完全或部分氟化），1-6C任选饱和的烷氧基或任选取代的芳基或杂芳基; R 8> H，，1-10 C任选饱和烷基（任选完全或部分氟化）或CN; R 9> H，Me，Et，CF 3或C 2 F 5; R 1> H，ONO 2，OH，SH，卤素，CH 2 Cl，1-10C任选饱和的烷基（任选完全或部分氟化），1-6C任选的饱和烷氧基，1-6C任选饱和的烷硫基或任选取代的芳基 或杂芳基; Me 3，Et，CF 3或C 2 F 5; H或1-10C任选饱和的烷基（任选地全部或部分氟化）; 任选饱和的烷基（任选地完全或部分氟化并且任选被O，S，SO，SO 2或NR 5''中断）; H或1-3C烷基; R 16>任选饱和的1-10C烷基（任选部分或完全氟化），CF 3或五氟乙基，CN或H; H，OH，卤素或1-10C任选饱和的烷基（任选地全部或部分氟化）; 或R 1> 4> R 5>任选的单或二卤代亚甲基; 波浪线= alpha或beta配置。 不包括：1,3,5（10） - 三烯-3,16α-二醇（Ia）; 1,3,5（10） - 三亚甲基-3,16-二醇（Ib）; 1,3,5（10），7-雌四烯-3β-二醇（Ic）; 和1,3,5（10），7-雌四烯-316-二醇（Id）。 还包括以下独立权利要求：（1）使用化合物（I），包括（Ia） - （Id），用于治疗妇女和男性由雌激素缺乏引起的疾病; （2）使用式（II）的部分结构作为有利于子宫上的骨的雌激素活性解离的化合物的总体结构的组分。 活动：妇科; uropathic; 抗溃疡; 止血; 骨科; cardiant; 抗动脉硬化; 促智; 神经保护; 抗炎; antiinfertility; 免疫调节。 作用机制：雌激素受体配体。 （Ia）对于大鼠前列腺和子宫雌激素受体的相对结合亲和力（雌二醇= 100）分别为50和9，并且其对于人雌激素受体α和β的相对结合亲和力的比例为6（雌二醇= 1）。

    9-ALPHA-SUBSTITUIERTE ESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE
    8.
    发明公开
    9-ALPHA-SUBSTITUIERTE ESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE 有权
    9-α-取代三烯作为选择性雌激素有效

    公开(公告)号：EP1517914A2

    公开(公告)日：2005-03-30

    申请号：EP03757065.2

    申请日：2003-06-11

    Applicant: Schering Aktiengesellschaft

    Inventor： KOSEMUND, Dirk ,  MÜLLER, Gerd ,  HILLISCH, Alexander ,  FRITZEMEIER, Karl-Heinrich ,  MUHN, Peter

    IPC: C07J1/00

    CPC classification number: C07J1/0055 ,  C07J1/0066 ,  C07J41/0072 ,  C07J63/008

    Abstract: The invention relates to novel 9 alpha -substituted estratrienes of general formula (I) - wherein R3, R7, R7', R13, R16, R17 and R17' have the designations cited in the description, and R9 represents a linear-chain or branched-chain, optionally partially or fully halogenated alkenyl radical comprising between 2 and 6 carbon atoms, or an ethinyl radical or a prop-1-inyl radical - as pharmaceutical active ingredients which have, in vitro, a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparation of the rat uterus, and, in vivo, preferably a preferential action on the ovary compared to the uterus. The invention also relates to the production of said estratrienes, to the therapeutic application thereof and to pharmaceutical forms of administration containing the novel compounds. The invention further relates to the use of said compounds for treating illnesses and states related to estrogen deficiency.

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