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    • 6. 发明授权
    • Platinum (IV) complex and pharmaceutical composition comprising the same
    • 铂(IV)复合物和包含其的药物组合物
    • US5902826A
    • 1999-05-11
    • US997061
    • 1997-12-23
    • Kinichi MogiHidehiko KoyaMari OhtsukaHiroyuki MizunoSusumu Sato
    • Kinichi MogiHidehiko KoyaMari OhtsukaHiroyuki MizunoSusumu Sato
    • A61K31/55C07F15/00A61K31/28
    • C07F15/0093
    • A diamine-platinum (IV) complex represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 together represent R.sup.5 O--CH(CH.sub.2 NH.sub.2).sub.2 (R.sup.5 represents hydrogen, acetyl, trifluoroacetyl, benzoyl, cycloalkylcarbonyl or methanesulfonyl) or a C.sub.5-8 1,2-cycloalkanediamine; R.sup.3 and R.sup.4 each represents hydrogen or R.sup.6 CO-- (R.sup.6 represents alkyl, halogenoalkyl, cycloalkyl, aryl or aralkyl); and two X's together represent a malonic acid residue or glycolic acid residue which may have a substituent capable of coordinating to the platinum in formula (1) by an O,O-coordination or an N-acylamino acid residue coordinating to the platinum in formula (1) by an O,N-coordination; and a pharmaceutical composition comprising as an active ingredient the above-described diamine-platinum (IV) complex.
    • 由下式(1)表示的二胺 - 铂(IV)络合物:其中R1和R2一起表示R5O-CH(CH2NH2)2(R5代表氢,乙酰基,三氟乙酰基,苯甲酰基,环烷基羰基或甲磺酰基)或C5-8 1,2-环烷二胺; R3和R4各自表示氢或R6CO-(R6表示烷基,卤代烷基,环烷基,芳基或芳烷基); 两个X一起代表丙二酸残基或乙醇酸残基,其可以具有能够通过与式(1)中的铂配位的O,O-配位体或N-酰基氨基酸残基与式(1)中的铂配位的取代基, 1)通过O,N-配位; 以及包含上述二胺 - 铂(IV)络合物作为活性成分的药物组合物。