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

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Domenico Alloatti

Maria Ornella Tinti

Claudio Pisano

Giuseppe Giannini

Mauro Marzi

Loredana Vesci

Franco Zunino

Sabrina Dallavalle

Sergio Penco

Lucio Merlini

Alma Dal Pozzo

Walter Cabri

Gianfranco Battistuzzi

Teresa Riccioni

Tiziana Brunetti

Vesci Loredana

Zunino Franco

Ni Minghong

Ni Ming Hong

Marcella Marcellini

Caludio Pisano

The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumors, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis. 

Retinoid derivatives endowed with cytotoxic and/or antiangiogenic properties

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 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

The present invention is related to new derivatives of Combretastatin, of Formula obtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation&#x2014;as anticancer and/or antiangiogenic activity, in a mammal&#x2014;to pharmaceutical compositions comprising these compounds.

Fluorocombretastatin and derivatives thereof

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

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Rome, Italy

Domenico Alloatti