Proter S.p.a.

Augusto De Barbieri

A pharmaceutical composition for use in the treatment of malignant tumor cells in laboratory animals is disclosed. The pharmaceutical composition uses a pharmaceutically acceptable excipient with a tripeptide compound as the active ingredient. The tripeptide compound is formed from dichlorodiethylaminophenylalanine, parafluorophenylalanine, and methione.

Intravenous or intraperitoneal administration of a tripeptide compound

Compounds with high anti-tumor activity and of moderate toxicity are described which are constituted by tripeptides formed from dichlorodiethylaminophenylalanine, para-fluorophenylalanine and methionine bonded together by peptide links. The tripeptides of the invention are particularly useful in the treatment of malignant tumors.

Compounds of dichlorodiethylaminophenylalanine with anti-tumor activity

N-acyl derivatives of D-hexosamine made by linking an oligopeptide having a m-di(2-chloroethyl)amino-L-phenylalanyl residue to the amino groups of two hexosamine molecules by a peptide bond, are endowed with strong antitumor action against transplanted neoplasms in animals. Compounds according to the present invention are: ##STR1## and its salts with organic or inorganic acids physiologically tolerated. The antineoplastic activity of the compounds of the present invention is not affected in the gastrointestinal tract and hence they can be effectively administered orally.

N-Acyl derivatives of glucosamine having antitumor chemotherapeutic

N-Acyl derivatives of glucosamines made by linking an amino acid or oligopeptide having a m-di(2-chloroethyl)amino-L-phenylalanyl group, to the amino group of the glucosamines by a peptide bond, are endowed with strong anti-tumor action against transplanted neoplasma in animal. The compounds according to the present invention are of the general formula (I): ##STR1## where R.sub.1 is a hydrogen atom or an acetyl group,

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Milan, Italy

Augusto De Barbieri