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    • 5. 发明公开
    • SENSITIVITY ENHANCER FOR ANTINEOPLASIC AGENT
    • WIRKSTOFF ZUR VERBESSERUNG DES EMPFINDLICHKEITFÜRANTINEOPLASTISCHE WIRKSTOFFE。
    • EP0643966A1
    • 1995-03-22
    • EP94907663.2
    • 1994-02-23
    • KYOWA HAKKO KOGYO CO., LTD.
    • MURAKATA, ChikaraSAITHO, YutakaAKINAGA, ShiroOKABE, Masami
    • A61K31/475C07D498/22
    • C07D498/22
    • The invention provides a sensitivity enhancer for antineoplastic agents which contains as the active ingredient an indolocarbazole derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R¹ represents hydrogen, lower alkyl or lower alkanoyl; A represents a group represented by general formula (1) (wherein R² represents hydrogen, lower alkyl or lower alkanoyl, and R³ represents hydrogen or lower alkyl) when one of W¹ and W² represents hydrogen and the other thereof represents hydrogen or hydroxy, or alternatively W¹ and W² are combined together to represent oxygen, excluding the case where all of the R¹, R², W¹ and W² are hydrogen atoms and R³ is methyl; or A represents a group represented by general formula (2) [wherein X represents a single bond or -CO-; m represents an integer of 0 to 6; and Y represents hydrogen, OR⁴ (wherein R⁴ represents hydrogen, lower alkyl, aralkyl or CONR⁵R⁶, wherein R⁵ and R⁶ represent each independently hydrogen or lower alkyl, or alternatively R⁵ and R⁶ are combined together to form a heterocyclic group together with the nitrogen atom to which they are bonded), NR⁷R⁸ (wherein R⁷ and R⁸ represent each independently hydrogen or lower alkyl, or alternatively R⁷ and R⁸ are combined together to form a heterocyclic group together with the nitrogen atom to which they are bonded), or (un)substituted aryl] when R¹ represents lower alkyl or lower alkanoyl and one of W¹ and W² represents hydrogen while the other thereof represents hydrogen or hydroxy, or when R¹ represents hydrogen and one of W¹ and W² represents hydrogen while the other thereof represents hydroxy. The invention also provides another indolocarbazole derivative represented by general formula (II) or a pharmacologically acceptable salt thereof, wherein R 1a represents lower alkyl or lower alkanoyl; W represents hydrogen or hydroxy; and R 4a represents lower alkyl.
    • 本发明提供了抗肿瘤剂的敏感性增强剂,其含有作为活性成分的通式(I)表示的吲哚并咔唑衍生物或其药理学上可接受的盐,其中R 1表示氢,低级烷基或低级烷酰基; 当W 1和W 2之一表示通式(1)表示的基团(其中R 2表示氢,低级烷基或低级烷酰基,R 3表示氢或低级烷基)表示 氢,另一个表示氢或羟基,或者W 1和W 2组合在一起代表氧,不包括所有R 1,R 2,W 1和 W 2是氢原子,R 3是甲基; 或A表示由通式(2)表示的基团[其中X表示单键或-CO-; m表示0〜6的整数, 并且Y代表氢,OR 4(其中R 4表示氢,低级烷基,芳烷基或CONR 5 R 6,其中R 5和R 6各自独立地表示氢或低级烷基, 或者R 5和R 6结合在一起形成与它们所键合的氮原子一起的杂环基),NR 7 R 8(其中R 7和R 8) 独立地表示氢或低级烷基,或者R 7和R 8可以结合在一起形成杂环基以及它们所键合的氮原子),或(未取代的芳基),当R 1 >表示低级烷基或低级烷酰基,W 1和W 2中的一个表示氢,而另一个表示氢或羟基,或当R 1表示氢且W 1和W 2中的一个表示氢时, 代表氢,而另一个代表羟基。 本发明还提供另一种由通式(II)表示的吲哚并咔唑衍生物或其药学上可接受的盐,其中R 1a表示低级烷基或低级烷酰基; W表示氢或羟基; R 4a表示低级烷基。