Antitumor antibiotic BU-3285T
    3.
    发明公开
    Antitumor antibiotic BU-3285T 失效
    抗肿瘤抗生素BU-3285T。

    公开(公告)号:EP0408336A2

    公开(公告)日:1991-01-16

    申请号:EP90307579.4

    申请日:1990-07-11

    CPC分类号: C07D309/32

    摘要: The present invention relates to the antitumor antibiotic compound BU-3285T and its preparation. The compound is obtained by culturing a new strain of Chainia rosea and demonstrates both antitumor and antifungal activity. It also relates to the desulfated derivative of BU-3285T which is obtained by treatment of BU-3285T with sulfatase enzyme. BU-3285T desulfate possesses antitumor activity.

    摘要翻译: 本发明涉及抗肿瘤抗生素化合物BU-3285T及其制备方法。 该化合物通过培养一种新的连翘蔷薇菌株获得,并表现出抗肿瘤和抗真菌活性。 它还涉及通过用硫酸酯酶处理BU-3285T获得的BU-3285T的脱硫衍生物。 BU-3285T硫酸盐具有抗肿瘤活性。

    Pradimicin derivatives
    5.
    发明公开
    Pradimicin derivatives 失效
    PRADIMICIN衍生物

    公开(公告)号:EP0432527A3

    公开(公告)日:1991-12-04

    申请号:EP90122217.4

    申请日:1990-11-20

    摘要: The present invention concerns neutral sugar derivatives (Formula I) of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
    wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid residue has the D -configuration; and R² is H or ß- D -xylosyl with the proviso that, when R¹ is methyl, R² is H; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及普拉德霉素的中性糖衍生物(式I),它们作为抗真菌剂的用途,其制备方法及其合成中间体。 其中R 1选自H,甲基和羟甲基,当R 1为甲基或羟甲基时,所得氨基酸残基具有D-构型; 且R 2为H或β-D-木糖基,条件是当R 1为甲基时,R 2为H; 或其药学上可接受的盐。

    Acylated derivatives of etoposide
    6.
    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

    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.

    Fluoro-substituted epipodophyllotoxin glucosides
    8.
    发明公开
    Fluoro-substituted epipodophyllotoxin glucosides 失效
    氟代显性表鬼臼毒素。

    公开(公告)号:EP0358197A2

    公开(公告)日:1990-03-14

    申请号:EP89116448.5

    申请日:1989-09-06

    IPC分类号: C07H17/04 A61K31/70

    CPC分类号: C07H17/04 Y02P20/55

    摘要: The present invention provides antitumor fluoro-substituted 4'-demethylepipodophyllotoxin glucosides.

    摘要翻译: 本发明提供抗肿瘤氟取代的4'-去甲表鬼臼毒素葡糖苷(I)。 其中R 2是H,R 1选自(C 1-10)烷基; (C 2-10)链烯基; (C 5-6)环烷基; 2-呋喃基; 2-噻吩基; (C 6-10)芳基; (C7-14)芳烷基; 和(C 8-14)芳烯基,其中每个芳环可以是未取代的或被一个或多个选自卤素,(C 1-8)烷基,(C 1-8)烷氧基,羟基,硝基和氨基的基团取代; 或R 1和R 2各自为(C 1-8)烷基; 或R 1和R 2和它们所连接的碳连接形成(C5-6)环烷基; R 3或R 4之一是OH,另一个是F; R 5为H或苯酚保护基; 而“IMAGE”代表α-或β-糖苷键。

    Pradimicin derivatives
    10.
    发明公开
    Pradimicin derivatives 失效
    普拉定霉素衍。

    公开(公告)号:EP0432527A2

    公开(公告)日:1991-06-19

    申请号:EP90122217.4

    申请日:1990-11-20

    摘要: The present invention concerns neutral sugar derivatives (Formula I) of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
    wherein R¹ is selected from the group consisting of H, methyl, and hydroxymethyl, and when R¹ is methyl or hydroxymethyl, the resulting amino acid residue has the D -configuration; and R² is H or ß- D -xylosyl with the proviso that, when R¹ is methyl, R² is H; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及普拉德霉素的中性糖衍生物(式I),它们作为抗真菌剂的用途,其制备方法及其合成中间体。 其中R 1选自H,甲基和羟甲基,当R 1为甲基或羟甲基时,所得氨基酸残基具有D-构型; 且R 2为H或β-D-木糖基,条件是当R 1为甲基时,R 2为H; 或其药学上可接受的盐。