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

Istituto Nazionale Per Lo Studio E La Cura Dei Tumori

Sigma-tau

Instituto Nazionale Per Lo Studio E La Cura Dei Tumori

Mauro Marzi

Maria Ornella Tinti

Patrizia Minetti

Claudio Pisano

Walter Cabri

Giuseppe Giannini

Francesco De Angelis

Fabrizio Giorgi

Fabio Giannessi

Piero Foresta

Arduino Arduini

Piero Chiodi

Marco Alpegiani

Paolo Carminati

Loredana Vesci

Franco Zunino

Domenico Vergani

Domenico Alloatti

Paolo Ghetti

Maria Di Marzo

Gianfranco Battistuzzi

Vesci Loredana

Zunino Franco

Sergio Penco

Domenico Misiti

Gian Piero Moretti

Silvia Armaroli

Giuseppe Marazzi

Teresa Riccioni

Emanuela Tassoni

Romano Di Fabio

Licia Pacifici

Carla Franceschelli

Massimo Castorina

Enrico Garattini

Caludio Pisano

Penco Sergio

Gomez Patricio Martin

Danelli Tamara

Vergani Domenico

Alpegiani Marco

Cabri Walter

Elena Marastoni

Marcella Marcellini

Riccardo Pezzi

Elena Badaloni

Fabio Giannesi

Martin Gomez Patricio

The present invention relates to a new crystalline form of R-4-trimethylammonium-3-(tetradecylcarbamoyl)-amino butyrate (also named crystalline Form I of ST 1326 or teglicar), a process for its preparation and pharmaceutical compositions containing same.

Crystalline teglicar

This invention relates to a process for preparing a crystalline form of (4S)-11(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3'4&#x2032;:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing from methanol.

Crystalline form II of 7-(dimethoxy-methyl) camptothecin, its use as intermediate and products obtained therefrom

A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.

Stereoselective process and crystalline forms of a camptothecin

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 process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.

Synthesis of deoxybiotinyl hexamethylenediamine-dota

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

Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase

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

Compounds of formula (I)wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

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

Compounds of formula (I) or (II) are described: 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.

Camptothecins with a modified lactone ring

Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and cheomsensitising agents.

Bis-heterocyclic compounds with antitumour and chemosensitising activity

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Rome, Italy

Mauro Marzi