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

Fabrizio Giorgi

Walter Cabri

Mauro Marzi

Maria Ornella Tinti

Marco Alpegiani

Paolo Carminati

Domenico Vergani

Paolo Ghetti

Giuseppe Marazzi

Silvia Armaroli

Emanuela Tassoni

Elena Badaloni

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

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Rome, Italy

Fabrizio Giorgi