Glycolic acid type platinum complexes

C - Chemistry – Metallurgy – 07 – F

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167/119, 260/429

C07F 15/00 (2006.01) A61K 31/295 (2006.01)

Patent

CA 1226295

ABSTRACT Novel platinum complexes of glycolic acid type having potent antitumor activity and high water solubility with low nephrotoxicity and a pharmaceutical composition containing one or more said compounds together with one or more carriers, diluents or excipients are provided. They can be administered parenterally to patients suffering from malignant tumors. They are prepared by passing nitrato-platinum complexes of amines through anion exchange resins and subsequent reaction with glycolic acids. BACKGOUND OF THE INVENTION 1. FIELD OF THE INVENTION The present invention relates to novel platinum complexes of glycolic acid type which have antitumor activity comparable to or more potent than that of cisplatin. The nephrotoxicity is very low and the water solubility is high. 2. DESCRIPTION OF THE PRIOR ART Compounds analogous to cisplatin [U.S. Patent Nos. 3,892,790 and 3,904,663] have intensively been investigated since its potent antitumor activity was observed; as the result of the fact, compounds such as malonato(1,2- diaminocyclohexane)platinum(II) [U.S Patent No.4,169,846], sulfato(1,2-diaminocyclohexane)platinum(II) [U.S Patent Nos. 4,200,583 and 4,256,652], 4-carboxyphthalato(1,2- diaminocyclohexane)platinum(II) [British Patent Publication No. 2,003,468], cis-dichloro-trans-dihydroxy-bis(isopropyl- amine)platinum(IV) [U.S. Patent No. 4,394,319], and the like are known presently. The present inventors have also been studying compounds analogous to cisplatin and prepared various new types of platinum complexes having potent antitumor activity and high water solubility, for example, novel platinum complexes - 1 -

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