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    • 2. 发明授权
    • Platinum(II) complex and processes for preparing the same
    • 铂(II)络合物及其制备方法
    • US5395947A
    • 1995-03-07
    • US117096
    • 1993-09-14
    • Dae-Kee KimGanghyeok KimJongsik GamYong B. ChoHun T. KimJoo H. TaiKey H. Kim
    • Dae-Kee KimGanghyeok KimJongsik GamYong B. ChoHun T. KimJoo H. TaiKey H. Kim
    • C07D317/28A61K31/555C07D317/32C07D317/72C07F15/00C07D317/00
    • C07F15/0093
    • Disclosed herein are novel platinum(II) complexes having a potent anti-tumor activity which are represented by the formula (1), ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cycloalkane group together with the carbon atom attached thereto; two Xs jointly form a group represented by formula (a) or (b) wherein, R.sub.3 is a hydrogen atom or a methyl group; R.sub.4 and R.sub.5, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cyclobutane together with the carbon thereto; and the absolute configurations at the respective chiral centers in the 4,5-bis(aminomethyl)-1,3-dioxolane moiety are (4R,5R) or (4S,5S); processes for the preparing the same; and their use for treating animal or human cancer. Further, disclosed herein are novel intermediates useful for the preparation of the platinum(II) complexes and processes for preparing said intermediates.
    • 本文公开了具有有效抗肿瘤活性的新颖的铂(II)络合物,其由式(1),(IMA)(1)表示:其中R1和R2,其中R1和R2, 可以相同或不同,分别为氢原子或C1-4烷基,或与其连接的碳原子一起共同形成环烷烃基; 两个X共同形成由式(a)或(b)表示的基团,其中R3是氢原子或甲基; R4和R5可以相同或不同,分别为氢原子或C1-4烷基,或与其一起共同形成环丁烷; 并且4,5-双(氨基甲基)-1,3-二氧戊环部分各手性中心的绝对构型为(4R,5R)或(4S,5S); 制备方法; 及其用于治疗动物或人类癌症的用途。 此外,本文公开了可用于制备铂(II)络合物的新中间体和用于制备所述中间体的方法。