Pliva-lachema A.s.

Zak, Frantisek

Frantisek Zak

Anna Poulova

Adolf Mistr

Jaroslav Turanek

Dana Zaluska

Milan Melka

Disclosed is a platinum complex of formula (I) wherein X represents a halogen atom, B represent, independently to each other, a halogen atom, a hydroxyl group or a carboxylate group containing 1 to 6 carbon atoms, and A represents a croup &mdash;NH &mdash;R wherein R is a tricyclic hydrocarbon moiety containing 10 to 14 carbon atoms which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) each containing 1 to 4 carbon atoms, and, furthermore, an inclusion complex of the above platinum complex with beta- or gamma-cyclodextrin which may be optionally substituted by hydroxyalkyl groups containing 1 to 6 carbon atoms. There is also disclosed a process for the manufacture of the complex of formula (I) based on oxidation of a complex of divalent platinum of formula (II) with hydrogen peroxide and on optional substitution of hydroxyl groups in the obtained product with carboxylate groups by action of an acylating agent. The disclosed complexes may be used as such or as a part of pharmaceutical composition in a therapy of oncologic diseases.

Platinum complex, its preparation and therapeutic application

A platinum complex of the general formula (I) wherein X represents a halogen atom and A represents a group &mdash;NH &mdash;R wherein R is a tricyclic hydrocarbon moiety containing 10 to 14 carbon atoms which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) containing 1 to 4 carbon atoms, and, furthermore, an inclusion complex of the above platinum complex with beta- or gamma-cyclodextrin which may be optionally substituted by a hydroxyalkyl group of 1 to 6 carbon atoms. There are also disclosed a method for the preparation of the complex of the formula (I) based on bringing into reaction a solution of an akaline metal salt of amminetrihalogenoplatinate (1&minus;) in a polar organic solvent or in water with a primary amine of formula R&mdash;NH , wherein R is a tricyclic hydrogen moiety containing 10 to 14 carbon atoms, which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) each containing 1 to 4 carbon atoms, at the temperature in the range of 0 to 100&deg; C., as well as a method for manufacture of the above inclusion complex. The both disclosed complexes may be used as such or as a part of pharmaceutical composition in a therapy of oncologic diseases.

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Brno, Czechia

Frantisek Zak