Fresenius Kabi Ipsum S.r.l.

Wayne State University

Universitá Degli Studi Di Padova

Centro Di Riferimento Oncologico

I.r.a. Istituto Ricerche Applicate S.p.a.

Fernando Formaggio

Walter Cabri

Jacopo Zanon

Antonio Ricci

Andrea Orlandin

Ivan Guryanov

Dario Visentini

Barbara Biondi

Q Ping Dou

Ugo Raffaello Citernesi

Lorenzo Beretta

Lorenzo Citernesi

Dolores Fregona

Luca Ronconi

Donatella Aldinucci

Rosa Di Liddo

Monica Piccione

Andrea Cividini

Emanuele Giuseppe De Marni

Gloria Andolina

Cristina Peggion

The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Process for the manufacture of degarelix and its intermediates

The invention concerns Au(III) complexes of the type [AuX(Pdtc)] (X=halogen, pseudo-halogen; pdtc=peptide-/esterified peptidedithiocarbamato) which are able to both maintain the antitumor properties and the lack of nephrotoxic side-effects of the previously reported Au(III)-dithiocarbamato complexes, together with an improved bioavailability through the peptide-mediated cellular internalization. The Au(III) complexes described have shown a significant biological activity on human tumor cell lines and, thus, they can be advantageously used as antineoplastic agents. The preparation method and use for the treatment of tumor pathologies of the Au(III) complexes of the invention are further described.

Gold (III) complexes with oligopeptides functionalized with sulfur donors and use thereof as antitumor agents

Growing community of inventors

Noventa Vicentina, Italy

Fernando Formaggio