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    • 7. 发明授权
    • Novel platinum complexes
    • 新型铂络合物
    • US4607114A
    • 1986-08-19
    • US661433
    • 1984-10-16
    • Yuya NakayamaKenji IwataKatsutoshi Takahashi
    • Yuya NakayamaKenji IwataKatsutoshi Takahashi
    • A61K31/28A61K31/282A61P35/00C07F15/00
    • C07F15/0093
    • This invention relates to a novel platinum-diamine complexes represented by the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each represents a lower alkyl group having 1 to 3 carbon atoms or jointly represent an alkylene group having 3 to 6 carbon atoms; two X's each represents a halogen atom, ##STR2## or jointly represent a group represented by ##STR3## in which R.sub.3 is a lower alkyl group or a group represented by --OM (wherein M is an atom which can become a monovalent cation); Y is --OH or a halogen atom; and n is 0 or 1, and n is 1 when R.sub.1 and R.sub.2 jointly represent an alkylene group having 5 carbon atoms and X is chlorine. The platinum-diamine complex of this invention has an excellent antitumor activity and a lower renal toxicity than cis-Platin now widely used as a carcinostatic as clinical medicine, and is expected as a carcinostatic lowered in toxicity.
    • 本发明涉及由以下通式表示的新颖的铂 - 二胺络合物:其中R 1和R 2各自表示具有1至3个碳原子的低级烷基或共同表示具有3至6个碳原子的亚烷基; 两个X各自表示卤素原子,或者共同表示由表示的基团,其中R3是低级烷基或由-OM表示的基团(其中M是可以成为单价阳离子的原子); Y是-OH或卤素原子; 且n为0或1,当R 1和R 2共同表示具有5个碳原子的亚烷基且X为氯时,n为1。 本发明的铂 - 二胺配合物与现在广泛用作制癌剂作为临床医学的顺铂具有优异的抗肿瘤活性和较低的肾毒性,并且预期其具有降低的致癌性。