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

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Boehringer Biochemia Robin S.p.a.

Other

Boehringer Mannheim Italia, S.p.a.

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Istituo Nazionale Per Lo Studio E La Cura Dei Tumori

Istituto Nazional Per Lo Studio E La Cura Dei Tumori

Franco Zunino

Sergio Penco

Maria Ornella Tinti

Walter Cabri

Marco Alpegiani

Claudio Pisano

Loredana Vesci

Lucio Merlini

Giuseppe Giannini

Sabrina Dallavalle

Mauro Marzi

Domenico Alloatti

Alessandro Pasini

Silvano Spinelli

Paolo Carminati

Carmelo A Gandolfi

Sergio Tognella

Odoardo Tofanetti

Gianfranco Battistuzzi

Maria Di Marzo

Alma Dal Pozzo

Ernesto Menta

Riccardo Pezzi

Ni Minghong

Ni Ming Hong

Sergio Tongnella

Elena Marastoni

Tamara Danelli

Martin Gomez Patricio

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

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

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

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.

7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists

Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors. 

Esters in position 20 of camptothecins

Camptothecin derivatives of camptothecin of formula (I) wherein the groups R, Rand Rare as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodiumare also disclosed.

7-imino derivatives of camptothecin having antitumor activity

Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.

Camptothecin derivatives having antitumor activity

Compounds of formula (I), wherein: R,is &mdash;CN, &mdash;CH(CN)&mdash;R,, &mdash;CH&boxH;C(CN)&mdash;R,, &mdash;CH,&mdash;CH(CN)&mdash;R,, &mdash;C(&boxH;NOH)&mdash;NH,, &mdash;C(&boxH;NH)&mdash;NH,, &mdash;CH&boxH;C(NO,)&mdash;R,, &mdash;CH(CN)&mdash;R,, &mdash;CH(CH,NO,)&mdash;R,; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R,is hydrogen; R,is hydrogen, OR,; R,is hydrogen, C,-C,linear or branched alkyl, CN, COOR,; R,is hydrogen, OR,; R,is hydrogen, C,-C,linear or branched alkyl, (C,-C,) aryl (C,-C,) alkyl, (C,-C,) alkoxy (C,-C,) alkyl, (C,-C,) alkyl (C,-C,) aryl, (C,-C,) aryl (C,-C,) acyl, (C,-C,) acyl, amino (C,-C,) alkyl, amino (C,-C,) acyl, glycosyl; R,is hydrogen, C,-C,linear or branched alkyl, (C,-C,) aryl (C,-C,) alkyl, (C,-C,) alkoxy (C,-C,) alkyl, (C,-C,) alkyl (C,-C,) aryl; R,has the same meanings of R,, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives

Camptothecin derivatives of camptothecin of formula (I)

7-Substituted camptothecin derivatives and methods for inhibiting the

Amino anthracenediones-bis platinum complexes, useful as antitumoral

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Milan, Italy

Franco Zunino