Shionogi Company Limited

Tetsushi Totani

Katsutoshi Aono

Osamu Shiratori

Kenji Yamaguchi

Yoshihiro Muraoka

Yasuko Adachi

Michihiro Komura

Naomi Uchida

Novel platinum complexes of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each identically of differently is lower alkyl, or R.sup.1 and R.sup.2 taken together form --(CH.sub.2)m--, and m is an integer from 2 to 5, and antitumor agents comprising the compound (I), which are effective against cisplatin-resistant ascitic murine leukemia, murine leukemia, and solid tumor, with slight hemotoxicity and nephrotoxicity.

Platinum complexes and antitumor agents containing them as an active

A compound of the formula (I): ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, hydroxy, carboxy, C.sub.1 -C.sub.6 alkoxy, halogen or oxo; m is an integer from 2 to 7; X and Y each is chlorine or nit-rato ligand, or taken together form --OCOCH(R.sup.1)O--, OCOCOO--, ##STR2## R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, hydroxymethyl, halogmethyl or phenyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.5 alkyl; and n is an integer from 2 to 5), being useful as antitumor agents is provided.

Ammine-alicyclic amine-platinum complexes and antitumor agents

Novel platinum (IV) complexes having potent antitumor and antibacterial activities and high water solubility with low toxicity and pharmaceutical and/or veterinarily compositions containing one or more compounds together with one or more carriers are provided. They can be prepared by reacting a corresponding platinum (II) complex with hydrogen peroxide or halogen.

Platinum complexes

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.

Glycolic acid type platinum complexes

Platinum complexes of the following formula useful as antitumor agents with less nephro-toxicity and higher water solubility than cisplatin: ##STR1## wherein X and Y respectively or taken together represent a mono- or di-valent residue of hydroxycarboxylic acids.

Novel water-soluble glycolic acid platinum complexes which have more potent antitumor activity with lower nephrotoxicity than cisplatin are provided. They can be administered parenterally to mice attacked by malignant tumors. Prepared from dinitrato-platinum complexes of amines on treatment with anion exchange resins and subsequent reaction with glycolic acid.

Glycolic acid platinum complexes

Organo-platinum complexes of the following formula having excellent antitumor actions: ##STR1## X and Y each or taken together is a mono- or bi-functional ligand selected from the group consisting of halogeno, nitrato, sulfonato, monocarboxylato (mono-functional), sulfato, and dicarboxylato (bi-functional); and each of n and m is an integer of 1 or 2.

Growing community of inventors

Hyogo, Japan

Tetsushi Totani