Other

Euticals Spa

Prime European Therapeucials S.p.a.

Solar Chemical S.a.

Amri Italy S.r.l.

Giuseppe Guazzi

Maria Argese

Paride Grisenti

Tiberio Bruzzese

Elahi Shahrzad Reza

Roberto Scrocchi

Alessandro Livieri

Alberto Varalli

Paolo Anesa

Marco Rognoni

Giuliano Marcon

A process for the preparation of the amorphous form of Regadenoson of formula is disclosed together with new crystalline polymorphic forms E, F and G and methods for their preparation. Regadenoson amorphous form can be prepared in mild reaction conditions with high chemical purity (&#x3e;99.6%) and high stability to the heating. A particularly thermodynamically stable anhydrous crystalline form of Regadenoson (form G) is also disclosed, provided with high stability not when exposed to 90% RH at 25&#xb0; C. for 96 hour, but also to the heating up to 200&#xb0; C.

Stable solid forms of regadenoson

A cocrystal of tiotropium bromide and lactose monohydrate is herein disclosed. In the cocrystal the components tiotropium bromide and lactose are preferably present in an almost stoichiometric ratio. Said cocrystal has a single endothermic event at about 191-193&#xb0; C. determined by DSC. A process for the preparation of the cocrystal is also disclosed. Preferably, the cocrystal has a particle size distribution of D90&#x3c;10 &#x3bc;m. The cocrystal is also disclosed for use as medicament, in particular for the treatment of a respiratory complaint, such as chronic obstructive pulmonary disease (COPD), bronchitis, emphysema and asthma. A pharmaceutical composition comprising the cocrystal as active ingredient is also disclosed, in particular for administration by inhalation. In the latter case, said cocrystal has a mean particle size of 0.5 to 10 &#x3bc;m, preferably 1 to 6 &#x3bc;m, more preferably 1.5 to 5 &#x3bc;m.

Crystalline form of tiotropium bromide with lactose

Disclosed is the preparation of 2-deoxy-D-erythro-2,2-difluoro-ribofuranose-3,5-dibenzoate, a known intermediate for the preparation of Gemcitabine, by means of a reduction process; further disclosed is the purification of Gemcitabine by chromatography and the purification of Gemcitabine hydrochloride by crystallization techniques from ternary solvent mixtures. The main advantage of the invention is providing Gemcitabine hydrochloride with purity in conformity with the Pharmacopoeia requirements, as well as a process particularly convenient from the industrial point of view.

Process for the preparation of gemcitabine hydrochloride

A process for the synthesis of 9-(2-hydroxyethoxy methyl) guanine in which guanine, or its salts, is reacted with 2-4 moles of hexamethyldisilazane, in the presence of an aprotic solvent and of ammonium sulfate. Thereafter, the trimethylsilyl derivative, without being isolated, is reacted with a stoichiometric quantity of an acyloxyethoxy methyl halide and hydrolyzed with aqueous sodium acetate or sodium hydroxyde to give 9-(2-hydroxyethyoxy methyl) guanine.

Process for the synthesis of 9-(2-hydroxyethoxy methyl) guanine

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Milan, Italy

Giuseppe Guazzi