Boehringer Mannheim Italia, S.p.a.

University of Vermont and State Agricultural College

F. Hoffmann-la Roche Ag

Mariella Valsecchi

Silvano Spinelli

Ernesto Menta

Nicholas P Farrell

Carlo Bugatti

Carla Manzotti

Alessandro Pasini

Marco Conti

Ferdinando C Giuliani

Paolo Pavesi

Luisa Del Greco

Fernando Giuliani

Trinuclear cationic platinum complexes having antitumor activity and

Novel bis(platinum) (IV) complexes coupled via diamine bridging agents are taught as well as methods for their preparation. These complexes are to be used as pharmaceutical agents, e.g., for the treatment of cancer and parasitic diseases.

Bis-platinum (IV) complexes as chemotherapeutic agents

##STR1## Platinum (II) complexes of formula (I) where: Am is a monodentate amine, or (Am).sub.2 is a bidentate amine, B represents a straight or branched alkyl residue or a single bond, R is selected from the group of hydrogen, (C.sub.3 -C.sub.8) cycloalkyl, phenyl or naphthyl which may be substituted by halogens (I, Br, Cl, F), trihalomethane, hydroxyl, (C.sub.1 -C.sub.4)-alkoxyl, (C.sub.1 -C.sub.7)-acylamino, (C.sub.1 -C.sub.7)-sulphamido, allyl, phenoxyl, haloalkoxyl, nitro, cyano, azido, with condition that when R is hydrogen B is different from a single bond, Q is a residue of formula --(CH.sub.2).sub.n1 --CR.sub.a R.sub.b --(CH.sub.2).sub.n2 --, 1,2- or 2,3-naphthalene, benzo-1,3-dioxolan-5,6-diyl, substituted or unsubstituted 1,2-phenylene, R.sub.a and R.sub.b are selected independently of each other from the group of hydrogen, allyl, linear or branched (C.sub.1 -C.sub.8)-alkyl, --(CH.sub.2).sub.p OH, --(CH.sub.2 CH.sub.2 O).sub.q --CH.sub.3, or taken together with the carbon atom to which they are bonded form a (C.sub.3 -C.sub.8) cycloalkyl, or heterocyclic tetrahydropyran-4,4-diyl, n.sub.1 and n.sub.2 are independently zero or the integer 1, p is an integer from 2 to 6, and q is an integer from 1-3, X.sup.- is a biocompatible anion such as chloride, bromide, iodide, nitrate, perchlorate, or one equivalent of sulphate or phosphate, or an anion of a monovalent C.sub.1 -C.sub.4 organic acid such as acetate, propionate or chloroacetate, or of an aromatic acid such as benzoate, or of a heteroaromatic acid such as nicotinate are described. The compounds are useful as anti-tumor drugs.

Cis-platinum complexes with chelating amines and sulphinyl carboxylates

Growing community of inventors

Monza, Italy

Mariella Valsecchi