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    PROCESS FOR THE PRODUCTION OF ESTETROL INTERMEDIATES
    57.
    发明申请
    PROCESS FOR THE PRODUCTION OF ESTETROL INTERMEDIATES 审中-公开
    生产中间体的方法

    公开(公告)号：US20140107091A1

    公开(公告)日：2014-04-17

    申请号：US14122892

    申请日：2012-06-01

    申请人： ESTETRA S.A.

    发明人： Jean-Claude Pascal

    IPC分类号： C07J1/00 ,  A61K31/565

    CPC分类号： C07J1/0018 ,  A61K31/565 ,  C07J1/0059 ,  C07J1/007 ,  C07J51/00 ,  Y02P20/55

    摘要： The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of the compound of formula (IV) to produce compound of formula (V); and d) reacting the compound of formula (V) with a reducing agent to produce compound of formula (I).

    摘要翻译： 本发明涉及一种制备式（I）化合物的方法，包括以下步骤：a）使式（II）化合物与甲硅烷基化或酰化剂反应制备式（III）化合物，其中P1 是选自R2Si-R3R4或R1CO-的保护基，R1是选自C1-6烷基或C3-6环烷基的基团，每个基团任选被一个或多个独立地选自氟或C 1-4烷基的取代基取代; R 2，R 3和R 4各自独立地为选自C 1-6烷基或苯基的基团，每个基团任选被一个或多个独立地选自氟或C 1-4烷基的取代基取代; b）式（III）化合物的卤化或亚硫酰化以制备式（IV）化合物; 其中X是卤素或-O-SO-R 5，R 5是选自C 6-10芳基或杂芳基的基团，每个基团任选被一个或多个独立地选自氯或C 1-4烷基的取代基取代; c）式（Ⅳ）化合物的脱卤或脱亚甲基化，制得式（Ⅴ）化合物; 和d）使式（V）的化合物与还原剂反应以制备式（I）的化合物。

    MODIFIED, HYDROXY-SUBSTITUTED AROMATIC STRUCTURES HAVING CYTOPROTECTIVE ACTIVITY
    58.
    发明申请
    MODIFIED, HYDROXY-SUBSTITUTED AROMATIC STRUCTURES HAVING CYTOPROTECTIVE ACTIVITY 审中-公开
    改性，羟基取代的具有抗肿瘤活性的芳香结构

    公开(公告)号：US20110015165A1

    公开(公告)日：2011-01-20

    申请号：US12888560

    申请日：2010-09-23

    申请人： Douglas F. Covey

    发明人： Douglas F. Covey

    IPC分类号： A61K31/566 ,  A61K31/565 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  A61P27/02 ,  A61P9/10 ,  A61P27/06 ,  A61P27/12

    CPC分类号： C07J1/00 ,  A61K31/565 ,  C07J1/0059 ,  C07J1/007

    摘要： The present invention is directed to a process for conferring cytoprotection on a population of cells which comprises administering to that population of cells a compound comprising a hydroxy-substituted aromatic ring structure and a non-fused polycyclic, hydrophobic substituent attached thereto. In particular, the present invention is directed to such a process wherein the administered compound is phenolic, such as a steriod (e.g., estrogen), and has a non-fused polycyclic, hydrophobic substituent attached to the hydroxy-substituted A-ring thereof.

    摘要翻译： 本发明涉及对细胞群赋予细胞保护作用的方法，其包括向所述细胞群施用包含羟基取代的芳环结构和与其连接的非稠合多环疏水性取代基的化合物。 特别地，本发明涉及这样的方法，其中所施用的化合物是酚类，例如steriod（例如雌激素），并且具有与其羟基取代的A环连接的非稠合的多环疏水性取代基。

    Method and intermediates for preparing 2-alkoxy and 2-aryloxy estrogen compounds
    59.
    发明申请
    Method and intermediates for preparing 2-alkoxy and 2-aryloxy estrogen compounds 有权
    制备2-烷氧基和2-芳氧基雌激素化合物的方法和中间体

    公开(公告)号：US20100099141A1

    公开(公告)日：2010-04-22

    申请号：US12285901

    申请日：2008-10-16

    申请人： Paolo Lombardi ,  Franco Buzzetti

    发明人： Paolo Lombardi ,  Franco Buzzetti

    IPC分类号： C12P33/00 ,  C07J51/00

    CPC分类号： C07J1/0059 ,  C07J1/007 ,  C07J41/0005

    摘要： The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

    摘要翻译： 本发明涉及一种制备2-烷氧基和2-芳氧基雌激素化合物的方法，以及在该方法的使用中制备的中间体化合物，该中间体化合物是制备某些生理活性化合物的有用中间体。