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

Rostaquo S.p.a.

Silvia Armaroli

Walter Cabri

Alberto Cerri

Marco Torri

Giuseppe Bianchi

Patrizia Ferrari

Mauro Marzi

Rosamaria Micheletti

Roberto Castagnani

Fabrizio Giorgi

Simona Sputore

Giuseppe Marazzi

Giulio Carzana

Maria Pia Zappavigna

Leonardo Banfi

Rosamaria Michaeletti

Vincenzo Colangeli

Gianandrea Quattrociocchi

Elena Badaloni

The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts. 

Process for the synthesis of 7-chloro-4-(piperazin-1-yl)-quinoline

New crystalline forms of 17&#x3b2;-(3-Furyl)-5-&#x3b2;androstane-3&#x3b2;,14&#x3b2;,17&#x3b1;-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.

Crystalline rostafuroxin

Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na, K-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms. 

Amino derivatives of androstanes and androstenes as medicaments for cardiovascular disorders

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

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Gallo Poggio Renatico, Italy

Silvia Armaroli