Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Sigma-tau Research Switzerland S.a.

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Alfasigma S.p.a.

Loredana Vesci

Claudio Pisano

Giuseppe Giannini

Franco Zunino

Sergio Penco

Lucio Merlini

Sabrina Dallavalle

Maria Ornella Tinti

Mauro Marzi

Walter Cabri

Claudio Cavazza

Marco Alpegiani

Domenico Alloatti

Gianfranco Battistuzzi

Maria Di Marzo

Alma Dal Pozzo

Paolo Carminati

Richard William Versace

Maurizio Taddei

Nicola Fanto'

Davide Vignola

Ni Ming Hong

Ni Minghong

Riccardo Pezzi

Maria Luisa Cervoni

Serena Ferrini

Sara Zaknoen

Margaret Ma Woo

Ni Ming Hong Hong

Elena Marastoni

Tamara Danelli

Martin Gomez Patricio

The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds. 

Aryl triazole compounds with antitumoural activity

The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.

Anticancer combination of artemisinin-based drugs and other chemotherapeutic agents

A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.

Combinations of therapeutic agents for treating cancer

The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds. 

Thio derivatives bearing lactams as potent HDAC inhibitors and their uses as medicaments

A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma.

Broad-spectrum anti-cancer treatment based on iminocamptothecin derivatives

A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma.

Treatment of pediatric tumors

Are described compounds of Formula (I) in which R, R', R&#x2033;, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterized by altered angiogenesis and as antitumorals.

Retinoid derivatives with antiangiogenic, antitumoral and proapoptotic activities

Indole derivatives of Formula (I+A) having antitumor and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumors. 

Indole derivatives having antitumor activity

A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I.

Treatment of drug-resistant tumors

Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.

Cinnamic, phenylpropiolic and phenylpropanoic acid derivatives useful as anti-tumor agents

Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumor, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumors.

Biphenyl and Naphthyl-Phenyl Hydroxamic Acid Derivatives

Compounds of Formula (I) are described in which the Rgroup is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents

The use of a substance belonging to the class of atypical retinoids for the topical treatment of acne is described. In particular the effects on an animal model for this skin disease of a pharmaceutical or cosmetic compound for topical use containing adamantyl methoxydiphenyl propenoic acid formulated in a gel are demonstrated.

Use of adamatyl methoxydiphenyl propenoic acid for the treatment of acne

Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumors and viral and parasite infections.

7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups

Compounds of Formula (I) are described: in which the Rgroup is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors &#x3b1;&#x3b2;and &#x3b1;&#x3b2;and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.

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Rome, Italy

Loredana Vesci