3-메칠-(O-치환된 옥시이미노)-피라졸린-5-온 유도체를함유하는 항암제
    7.
    发明公开
    3-메칠-(O-치환된 옥시이미노)-피라졸린-5-온 유도체를함유하는 항암제 失效
    3-甲基 - (O-取代的氧代) - 吡唑啉-5-酮衍生物作为抗肿瘤剂

    公开(公告)号:KR1020050031716A

    公开(公告)日:2005-04-06

    申请号:KR1020030067964

    申请日:2003-09-30

    CPC classification number: A61K31/4152 A61K9/0053

    Abstract: An anticancer composition comprising 3-methyl-(O-substituted oximino)-pyrazolin-5-one derivatives is provided, which derivatives inhibit activity of CDC25B enzyme which participates in cell differentiation and is overexpressed in cancer cells. The anticancer composition comprises 3-methyl-(O-substituted oximino)-pyrazolin-5-one derivatives represented by formula (1), and pharmaceutically acceptable salts thereof, wherein R1 is C1-C4 alkyl or substituted phenyl with a substituent that is one or more selected from hydrogen, halogen atom, C1-C4 alkyl, C1-C4 alkoxy, C2-C4 acyl and nitro; and R2 is C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C2-C4 acyl, methanesulfonyl, toluenesulfonyl, C1-C4 alkoxycarbonylmethyl, carboxymethyl or inorganic metal or organic amine salts of carboxymethyl.

    Abstract translation: 提供包含3-甲基 - (O-取代的肟基) - 吡唑啉-5-酮衍生物的抗癌组合物,该衍生物抑制参与细胞分化且在癌细胞中过表达的CDC25B酶的活性。 抗癌组合物包含由式(1)表示的3-甲基 - (O-取代的肟基) - 吡唑啉-5-酮衍生物及其药学上可接受的盐,其中R1是C1-C4烷基或具有取代基的取代苯基 或更多选自氢,卤素原子,C 1 -C 4烷基,C 1 -C 4烷氧基,C 2 -C 4酰基和硝基; R2为C1-C4烷基,C2-C4烯基,C2-C4炔基,C2-C4酰基,甲磺酰基,甲苯磺酰基,C1-C4烷氧基羰基甲基,羧甲基或羧甲基的无机金属或有机胺盐。

    로다닌계 화합물 또는 이의 약제학적으로 허용가능한 염을함유하는 항암제
    8.
    发明授权
    로다닌계 화합물 또는 이의 약제학적으로 허용가능한 염을함유하는 항암제 失效
    包含罗丹明衍生物或其药物可接受的药物的药物

    公开(公告)号:KR100844131B1

    公开(公告)日:2008-07-04

    申请号:KR1020070000624

    申请日:2007-01-03

    Abstract: A rhodanine-based compound or a pharmaceutically acceptable salt thereof is provided to show excellent inhibitory activity on CDC25B phosphatase acting on cell cycle decisively, thereby showing high anticancer activity on cancer cells. A rhodanine-based compound is represented by a formula(1), wherein each Ar1 and Ar2 is independently phenyl or pyridine, which may be substituted by at least two substituents selected from the group consisting of C1-4 alkyl, halogen, C1-7 alkoxy, C3-4 alkenyloxy, C2-4 acyl, cyano or nitro. An anti-cancer agent composition comprises the rhodanine-based compound or a pharmaceutically acceptable salt thereof as an effective ingredient.

    Abstract translation: 提供了一种绕丹宁类化合物或其药学上可接受的盐,对于对细胞周期起决定性作用的CDC25B磷酸酶具有优异的抑制活性,从而对癌细胞表现出高的抗癌活性。 绕丹宁类化合物由式(1)表示,其中每个Ar 1和Ar 2独立地是苯基或吡啶,其可以被至少两个选自C 1-4烷基,卤素,C 1-7的取代基取代 烷氧基,C3-4链烯氧基,C2-4酰基,氰基或硝基。 抗癌剂组合物含有绕丹宁类化合物或其药学上可接受的盐作为有效成分。

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