Fidia Farmaceutici S.p.a.

Fidia Advanced Biopolymers S.r.l.

Davide Renier

Lanfranco Callegaro

Matteo D'Este

Matteo D'este

Vittorio Crescenzi

Monica Campisi

Cristian Guarise

Stefania Panero

Fabio Bettella

Andrea Francescangeli

Gianfranco Pasut

Gianluca Abbati

Antonio Rosato

Susy Panfilo

Annalucia Serafino

Pasquale Pierimarchi

The present invention describes the new use in the oncologic field of bioconjugates as differentiating agents obtained by the conjugation between hyaluronic acid (HA) and a chemotherapeutic product (identified hereafter with the trade-name ONCOFID&#xae;) among which, in particular, Irinotecan, Doxorubicin, Paclitaxel, Cis-platinum and 5-Fluorouracyl (5-FU) for treating primary tumors and metastasis. In particular, the biological behavior is described in terms of action mechanism, efficacy and tolerability of pharmaceutical preparations of derivative of ONCOFID&#xae; soluble in water. More specifically, the invention relates to the surprising biological and pharmacological effect demonstrated by formulations based on ONCOFID-S (HA-SN38 conjugates) and ONCOFID-D (HA-Doxorubicin conjugates) in promoting the differentiation of tumoral cells towards a untransformed phenotype, compared with the reference drug Irinotecan (or CPT11 whose active form is represented by SN38) and Doxorubicin.

Therapeutic use of new pharmaceutical preparations containing antitumoral drugs bound to hyaluronic acid in the treatment of neoplasias

The object of the present invention is novel release systems comprising specific hyaluronic acid amides combined with therapeutically and/or biologically active proteins with a mainly hydrophobic nature, for sustained, slow release over time which increases the efficacy of the medicament and the patient's compliance.

Release system of hydrophobic proteins

The present invention describes a new group of bioconjugates which can be obtained by means of indirect synthesis, via a molecular spacer, between hyaluronic acid and/or its derivatives and drugs with an antitumoral activity belonging to different groups, their preparation process and use in the oncological field. The new derivatives, in relation to the type of bond and Substitution degree, have different physico-chemical properties which improve their tolerability and efficiency and allow a more accurate modulation of the dosage, exploiting an active targeting mechanism. 

Antitumoral bioconjugates of hyaluronic acid or its derivatives obtained by indirect chemical conjugation, and their use in the pharmaceutical field

This invention relates to oral and intra-articular formulations based on sulphated hyaluronic acid which are effective in the treatment of degenerative osteoarthritis.

Sulphated hyaluronic acid for treating degenerative osteoarthritis

The use is described of a conjugate between hyaluronic acid or a derivative thereof and antitumoral drugs for the preparation of pharmaceutical compositions for the topical treatment of hyperproliferative skin diseases.

Use of conjugates of hyaluronic acid in the local treatment of hyperproliferative skin diseases

The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones. An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.

Process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules, polymeric conjugates and relative uses thereof

Disclosed are hyaluronic acid derivatives functionalized with S-nitrosothiol groups of the general formula: wherein HA indicates hyaluronic acid and G indicates a suitable spacer. 

Hyaluronic acid derivatives containing groups able to release NO

Viscoelastic gels as novel fillers

The present invention concerns the preparation of composite biomaterials constituted by hyaluronic acid and the derivatives thereof in combination with polymers that have electrically conductive properties. In particular, the methods of preparing biomedical devices formed by a two- or three-dimensional polysaccharide matrix and by an electrically conductive membrane. The matrix is constituted by hyaluronic acid derivatives in the form of membranes, woven fabrics, nonwoven felts, meshes, gauzes, guide channels or sponges, while the electrically conductive membrane is constituted by a film of polypyrrole (polymer conductor) in combination with hyaluronic acid or a derivative thereof (doping agent).

Electrically conductive polymeric biomaterials, the process for their preparation and the use thereof in the biomedical and healthcare field

The present invention describes a new class of cross-linked derivatives of partially N-deacetylated hyaluronic acid or derivatives thereof, comprising at least one repeating unit of formula (I) hereinafter depicted and a process for the preparation of said cross-linked derivatives, comprising a multicomponent condensation reaction involving the carboxy groups and the amino groups originating from a partial N-deacetylation of hyaluronic acid or derivatives, together with an aldeyde and an isocyanide. The derivatives thus obtained can be used, alone or in association with biologically and/or pharmacologically active substances, for the preparation of pharmaceutical compositions, biomaterials, surgical and healthcare articles, slow release systems and for the coating of biomedical objects.

Cross-linked derivatives of hyaluronic acid

A process for preparing a hyaluronic acid fraction having an average molecular weight comprised between 5000 and 300,000 and a polydispersion index lower than 1.7, comprising treating the starting high molecular weight hyaluronic acid, contemporaneously with sodium hypochlorite and ultrasounds.

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Abano Terme, Italy

Davide Renier