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    Proteasome inhibiting beta-lactam compounds
    1.
    发明申请
    Proteasome inhibiting beta-lactam compounds 有权
    蛋白酶体抑制β-内酰胺化合物

    公开(公告)号：US20070060561A1

    公开(公告)日：2007-03-15

    申请号：US11224589

    申请日：2005-09-12

    申请人： Elias Corey ,  Philip Hogan

    发明人： Elias Corey ,  Philip Hogan

    IPC分类号： C07D205/12 ,  A61K31/407

    CPC分类号： C07D487/04

    摘要： Disclosed is a total synthesis of a biologically active β-Lactam—Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. Also disclosed are proteasome inhibiting compounds having the formula: wherein: R1 is a cyclolower alkyl group; or R1 is a lower alkyl group; and R2 is either hydrogen or a lower alkyl group; R3 is either hydrogen or a lower alkyl group; R4 a halo-lower alkyl group; and R5 is either hydrogen or a lower alkyl group.

    摘要翻译： 公开了生物活性β-内酰胺 - 化合物3的全合成，其与结构上和通过其作为蛋白酶体抑制剂的活性与Salinosporamide A和Omuralide有关。 还公开了具有下式的蛋白酶体抑制化合物：其中：R 1是环状烷基; 或R 1是低级烷基; 并且R 2是氢或低级烷基; R 3是氢或低级烷基; R 4卤代低级烷基; 并且R 5是氢或低级烷基。

    Process and intermediates for the production of 7-substituted antiestrogens
    2.
    发明申请
    Process and intermediates for the production of 7-substituted antiestrogens 有权
    用于生产7-取代的抗雌激素的方法和中间体

    公开(公告)号：US20050101583A1

    公开(公告)日：2005-05-12

    申请号：US10398924

    申请日：2001-10-09

    申请人： Robert Stevenson ,  Fraser Kerr ,  Anthony Lane ,  Eve Brazier ,  Philip Hogan ,  David Laffan

    发明人： Robert Stevenson ,  Fraser Kerr ,  Anthony Lane ,  Eve Brazier ,  Philip Hogan ,  David Laffan

    IPC分类号： C07B61/00 ,  C07J31/00 ,  C07J41/00 ,  C07J75/00 ,  A61K31/56 ,  C07J1/00

    CPC分类号： C07J31/006 ,  C07J31/00 ,  Y02P20/55

    摘要： A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4′ is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4′ to a group R4, or where R4′ is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.

    摘要翻译： 制备其中X如说明书中所定义的式（II）的中间体化合物的方法是卤代烷基，烷基，烯基，环烷基，羧基烷基，烷氧基羰基烷基，芳基或芳基烷基; R 2，R 3，R 4和R 5是说明书中定义的有机基团，该方法 包括式（III）化合物的芳构化，其中R 1，R 2，R 3，R 3，n，X和R 5 如式（II）所定义，并且R 4'是基团R 4或其前体基团，然后如果需要或需要， 进行一个或多个以下步骤：（i）除去任何羟基保护基团R; （ii）将前体基团R 4'转化成基团R 4，或其中R 4'是基团R 4 ，将其转换为不同的这样的组。 获得的化合物是例如制备氟维司群的有用的中间体。 还要求新的中间体。