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    Acylated derivatives of etoposide
    3.
    发明公开
    Acylated derivatives of etoposide 失效
    Acylierte Derivate von Etoposid。

    公开(公告)号：EP0401800A2

    公开(公告)日：1990-12-12

    申请号：EP90110729.2

    申请日：1990-06-06

    申请人： Bristol-Myers Squibb Company

    发明人： Ohnuma, Takeshi ,  Obata, Rika ,  Kamei, Hideo ,  Naito, Takayuki

    IPC分类号： C07H17/04 ,  A61K31/70

    CPC分类号： C07H17/04

    摘要： The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia
    wherein R² is H and R¹ is selected from the group consisting of (C₁₋₁₀)alkyl, (C₂₋₁₀)alkenyl, (C₅₋₆)cycloalkyl, 2-furyl, 2-thienyl, (C₆₋₁₀)aryl, and (C₇₋₁₄)aralkyl; or R¹ and R² are each (C₁₋₁₀)alkyl; or R¹, R² and the carbon to which they are attached together represent (C₅₋₆)cycloalkyl; one of R³ and R⁴ is H and the other is selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; or R³ and R⁴ are the same or different and are selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; R⁵ is H or a phosphate group.

    摘要翻译： 公开的表鬼臼毒素葡糖苷在本文中是一个或两个糖羟基进行酰化。 这些化合物对P388鼠白血病显示出显着的活性，其中R 2是H，R 1选自（C 1-10）烷基，（C 2-10）烯基，（C 5-6） 环烷基，2-呋喃基，2-噻吩基，（C6-10）芳基和（C7-14）芳烷基; 或R 1和R 2各自为（C 1-10）烷基; 或R 1，R 2和它们所连接的碳代表（C5-6）环烷基; R 3和R 4之一是H，另一个选自（C 1-5）烷酰基和苯甲酰基; 或R 3和R 4相同或不同，并且选自（C 1-5）烷酰基和苯甲酰基; R 5是H或磷酸基。

    Epipodophyllotoxin glycosides
    4.
    发明公开
    Epipodophyllotoxin glycosides 失效
    表鬼臼毒苷

    公开(公告)号：EP0461556A1

    公开(公告)日：1991-12-18

    申请号：EP91109356.5

    申请日：1991-06-07

    申请人： Bristol-Myers Squibb Company

    发明人： Ohnuma, Takeshi ,  Hoshi, Hideaki

    IPC分类号： C07H17/04 ,  A61K31/70

    CPC分类号： C07H17/04

    摘要： The present invention relates to novel antitumor compounds which are 4'-demethylepipodophyllotoxin derivatives. More particularly, the novel compounds are 4'-demethylepipodophyllotoxin allopyranosides, allofuranosides, and mannopyranosides.

    摘要翻译： 本发明涉及新的抗肿瘤化合物，它们是4'-去甲基表鬼臼脂素衍生物。 更具体地说，这些新化合物是4'-去甲基表鬼臼毒素异吡喃糖苷，allofuranoside和甘露吡喃糖苷。

    4'-Demethylepipodophyllotoxin glycosides
    5.
    发明公开
    4'-Demethylepipodophyllotoxin glycosides 失效
    4'-去甲表鬼臼毒甙

    公开(公告)号：EP0455159A1

    公开(公告)日：1991-11-06

    申请号：EP91106788.2

    申请日：1991-04-26

    申请人： Bristol-Myers Squibb Company

    发明人： Ohnuma, Takeshi ,  Obata, Rika

    IPC分类号： C07H17/04 ,  A61K31/70

    CPC分类号： C07H17/04

    摘要： The present invention relates to antitumor 4'-demethylepipodophyllotoxin glycosides having the formula

    wherein R is a pentose selected from the group consisting of
    β-D-ribopyranosyl, peracyl β-D-ribopyranosyl,
    β-D-xylopyranosyl, peracyl β-D-xylopyranosyl,
    α-D-xylopyranosyl, peracyl α-D-xylopyranosyl,
    α-D-arabinopyranosyl,
    3,4-O-(C₁₋₄)alkylidene-D-ribopyranosyl,
    2-O-acyl-3,4-O-(C₁₋₄)alkylidene-D-ribopyranosyl, and β-D-ribofuranosyl; P is hydrogen, or -PO₃H₂ or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及具有下式的抗肿瘤4'-去甲基表鬼臼脂素糖苷：其中R是选自β-D-吡喃核糖基，戊酰基β-D-吡喃核糖基，β-D-吡喃木糖基，过酰基β-D-吡喃木糖基 ，α-D-吡喃木糖基，过酰基α-D-吡喃木糖基，α-D-阿拉伯吡喃糖基，3,4-O-（C 1-4）亚烷基-D-吡喃核糖基，2-O-酰基-3,4-0- C 1-4）亚烷基-D-吡喃核糖基和β-D-呋喃核糖基; P是氢或-PO 3 H 2或其药学上可接受的盐。

    Alkoxymethylidene epipodophyllotoxin glucosides
    6.
    发明公开
    Alkoxymethylidene epipodophyllotoxin glucosides 失效
    葡萄糖苷von烷氧基亚甲基 - 表鬼臼毒素。

    公开(公告)号：EP0433678A1

    公开(公告)日：1991-06-26

    申请号：EP90122095.4

    申请日：1990-11-19

    申请人： Bristol-Myers Squibb Company

    发明人： Ohnuma, Takeshi ,  Naito, Takayuki ,  Kamei, Hideo

    IPC分类号： C07H17/04 ,  A61K31/70

    CPC分类号： C07H17/04

    摘要： Novel cyclic orthoesters and orthocarbonates of 4′-demethylepipodophyllotoxin glucoside of formula I are disclosed in the present invention. These compounds are active against experimental murine P388 leukemia.
    wherein one of R¹ and R² is C₁₋₅ alkoxy and the other is selected from the group consisting of hydrogen, C₁₋₅ alkyl, and C₁₋₅ alkoxy; R³ is hydrogen or -P(O)(OM)₂ wherein M is hydrogen or an alkali metal cation.

    摘要翻译： 在本发明中公开了式I的4分钟的新型环状原酸酯和原碳酸酯 - 式I的甲氧基表鬼臼毒素葡糖苷。 这些化合物对实验鼠P388白血病具有活性。 其中R 1和R 2之一是C 1-5烷氧基，另一个选自氢，C 1-5烷基和C 1-5烷氧基; R 3是氢或-P（O）（OM）2，其中M是氢或碱金属阳离子。

    Acylated derivatives of etoposide
    9.
    发明公开
    Acylated derivatives of etoposide 失效
    ETOPOSIDE的衍生物衍生物

    公开(公告)号：EP0401800A3

    公开(公告)日：1991-04-10

    申请号：EP90110729.2

    申请日：1990-06-06

    申请人： Bristol-Myers Squibb Company

    发明人： Ohnuma, Takeshi ,  Obata, Rika ,  Kamei, Hideo ,  Naito, Takayuki

    IPC分类号： C07H17/04 ,  A61K31/70

    CPC分类号： C07H17/04

    摘要： The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia
    wherein R² is H and R¹ is selected from the group consisting of (C₁₋₁₀)alkyl, (C₂₋₁₀)alkenyl, (C₅₋₆)cycloalkyl, 2-furyl, 2-thienyl, (C₆₋₁₀)aryl, and (C₇₋₁₄)aralkyl; or R¹ and R² are each (C₁₋₁₀)alkyl; or R¹, R² and the carbon to which they are attached together represent (C₅₋₆)cycloalkyl; one of R³ and R⁴ is H and the other is selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; or R³ and R⁴ are the same or different and are selected from the group consisting of (C₁₋₅)alkanoyl and benzoyl; R⁵ is H or a phosphate group.