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    • 1. 发明授权
    • Camptothecin derivative, and preparation method thereof, and pharmaceutical composition and application
    • 喜树碱衍生物及其制备方法,药物组合物及应用
    • US09266911B2
    • 2016-02-23
    • US14134346
    • 2013-12-19
    • Wenqiang ZhouJing Deng
    • Wenqiang ZhouJing Deng
    • C07F9/6533C07F9/6561C07D491/22A61K31/675A61P35/00C07F7/08
    • C07F9/65335C07D491/22C07F7/0812C07F7/0814C07F9/6561
    • The present invention relates to a camptothecin derivative having a structure as represented by Formula (II), in which Xn+ is selected from H+, K+, Na+, Li+, Mg2+, Ca2+, Zn2+, Fe3+, and ammonium ion, while R1, R2, R3, and R4 independently represent a hydrogen, a hydroxyl group, a nitro group, a cyano group, a halogen, a carboxyl group, an optionally substituted amino group, a silicon-containing group, a monocyclic aryloxy group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkylcarbonyl group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C3-C6 cycloalkyl group; alternatively, R1 and R2 are connected via one to three other atoms to form a heterocyclic ring; and in another embodiment, R3 and R4 are oxygen atoms and connected via —O—(CH2)n—O—, forming a ring, in which n=I or 2. The compound has great water-solubility, chemical stability, and great efficacy in treatment on cancer.
    • 本发明涉及具有由式(II)表示的结构的喜树碱衍生物,其中Xn +选自H +,K +,Na +,Li +,Mg2 +,Ca2 +,Zn2 +,Fe3 +和铵离子,而R1,R2, R 3和R 4独立地表示氢,羟基,硝基,氰基,卤素,羧基,任选取代的氨基,含硅基团,单环芳氧基,任选取代的C1- C6烷氧基,任选取代的C 1 -C 6烷基羰基,任选取代的C 1 -C 6烷基或任选取代的C 3 -C 6环烷基; 或者,R1和R2通过一至三个其它原子连接形成杂环; 在另一个实施方案中,R 3和R 4是氧原子并通过-O-(CH 2)n -O-取代,形成环,其中n = 1或2.该化合物具有很高的水溶性,化学稳定性和良好的 治疗癌症的疗效。