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49 条记录 (耗时 0.037 秒)

    Epothilone derivatives and methods for making and using the same
    4.
    发明授权
    Epothilone derivatives and methods for making and using the same 有权
    埃坡霉素衍生物及其制备和使用方法

    公开(公告)号：US07176235B2

    公开(公告)日：2007-02-13

    申请号：US10845467

    申请日：2004-05-12

    申请人： Gary Ashley ,  John R. Carney ,  Brian Metcalf

    发明人： Gary Ashley ,  John R. Carney ,  Brian Metcalf

    IPC分类号： A61K31/335 ,  C07D225/04 ,  C07D491/00 ,  C07D225/02

    CPC分类号： C07D405/06 ,  C07D313/00 ,  C07D413/06 ,  C07D417/06 ,  C07D491/04 ,  C12N1/20 ,  C12N9/00 ,  C12N15/52 ,  C12N15/74 ,  C12P17/16 ,  C12P17/181 ,  C12R1/01

    摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

    摘要翻译： 本发明涉及式（I）化合物及其药用盐和溶剂合物，其中R 1，R 2，R 3， R 4，R 5，W，X，Y和Ar如本文所定义。 式（I）化合物可用于治疗以细胞过度增殖为特征的疾病或病症。 本发明还涉及制备式（I）化合物的方法; 含有式（I）化合物的制剂; 以及在治疗以细胞过度增殖为特征的疾病或病症（包括癌症）中使用所述化合物和制剂的方法。

    Laulimalide derivatives
    5.
    发明授权
    Laulimalide derivatives 有权
    酸性衍生物

    公开(公告)号：US06815463B2

    公开(公告)日：2004-11-09

    申请号：US10364111

    申请日：2003-02-10

    申请人： Gary Ashley ,  Brian Metcalf

    发明人： Gary Ashley ,  Brian Metcalf

    IPC分类号： C07D41706

    CPC分类号： C07D493/08

    摘要： Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.

    Epothilone derivatives and methods for making and using the same
    7.
    发明授权
    Epothilone derivatives and methods for making and using the same 有权
    埃坡霉素衍生物及其制备和使用方法

    公开(公告)号：US06489314B1

    公开(公告)日：2002-12-03

    申请号：US09825856

    申请日：2001-04-03

    申请人： Gary Ashley ,  Brian Metcalf

    发明人： Gary Ashley ,  Brian Metcalf

    IPC分类号： A61K3133

    CPC分类号： C07D405/06 ,  C07D313/00 ,  C07D413/06 ,  C07D417/06 ,  C07D491/04 ,  C12N1/20 ,  C12N9/00 ,  C12N15/52 ,  C12N15/74 ,  C12P17/16 ,  C12P17/181 ,  C12R1/01

    摘要： The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.

    摘要翻译： 本发明涉及16元大环化合物。 在本发明的一个方面，提供下列化合物，其中：R1，R2，R3和R5各自独立地为氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; R4为氢 卤素，C 1 -C 10烷基，C 1 -C 10羟基烷基，C 1 -C 10卤代烷基，芳基，-C（= O）R 6，-C（= O）OR 6，-NR 6 R 7，其中R 6和R 7各自独立地为氢， 脂族，芳基或烷基芳基; W是O，NR8，其中R8是氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; X是O，CH2或碳 - 碳双键; Y是 不存在或C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基; 且Ar为芳基; 条件是排除了10,11-脱氢抗坏血酸酮C.