Chemi S.p.a.

Biovail Laboratories International S.r.l.

Recordati S.a. Chemical and Pharmaceutical Company

Valeant International Bermuda

Italfarmaco Spa

Biovail Laboratories, Inc.

Valeant Pharmaceuticals Luxembourg S.à.r.l.

Valeant International Srl

Stefano Turchetta

Maurizio Zenoni

Pietro Massardo

Umberto Ciambecchini

Lorenzo De Ferra

Paul Maes

Werner Oberegger

Mohammad Ashty Saleh

Graham Jackson

Fang Zhou

Elio Ullucci

Paolo Brandi

Mauro Anibaldi

Giorgio Berardi

Vincenzo De Sio

Valentina Aromatario

Renzo Rossi

Maria Donnarumma

Angela Tuozzi

Ettore Ammirati

Giovanni Frare

Gianfranco Piccoli

Silvana Cappelletti

Paolo Casellato

Sabina Pucci

Nakia Maulucci

Stefania Cocciolo

Paola Annoni

Alessandra Celona

Lorenzo Cappellini

Barbara Simonelli

A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl[4-(hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%. An HPLC method for determining the purity of the product and possible impurities thereof is also described.

Process for preparing {6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate having high purity

The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.

Modified release formulations of a bupropion salt

New formulations of bendamustine hydrochloride having HPLC purity higher than 99% obtained through the lyophilization of aqueous solutions without organic solvents, are described.

Lyophilized formulations of bendamustine hydrochloride

A process is described for preparing fesoterodine fumarate comprising the salification reaction of fesoterodine with fumaric acid in an organic solvent, preferably a ketone, at a temperature not greater than 45&#xb0; C. Such process allows obtaining products with high yields and purities, and in particular a product having a content of (2E)-4-[(3-(3-diisopropylamino-1-phenylpropyl)-4-(2-isobutyroyloxyphenyl)methoxy]-4-oxobut-2-enoic acid less than or equal to 0.15% by mole.

Method for preparing high-purity fesoterodine fumarate

Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.

Process for the synthesis of azacitidine and decitabine

Bortezomib esters with tartaric acid wherein the molar ratio between bortezomib and tartaric acid is 2:1 and formulations containing them are described.

Bortezomib esters and formulations thereof

A process for the preparation of a prodrug of 5-aminosalicylic acid, namely 2-butanoyloxy-5-amino-benzoic acid, and solid forms of such compound are described.

Prodrug of an anti-inflammatory active ingredient

The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 by purifying the mixture obtainable by reacting compounds 1 and 1a in the presence of a chemical agent capable of promoting the formation of a peptide bond in an aprotic organic solvent characterized in that the mixture is subjected to the following steps:

Process for the synthesis of pemetrexed disodium salt

The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called 'feso chromenyl' and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called '(R)-feso deacyl', which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate &#x201c;(R)-feso deacyl&#x201d;, called form B.

Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl

Polymorphous and amorphous forms of bupropion hydrobromide are described.

Bupropion hydrobromide polymorphs

Herein described is a novel crystalline form of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester. In particular, herein described is a polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphtalenyl) ester, characterized by a Powder X Ray Diffraction spectrum as indicated in FIG., and/or by a DSC profile as indicated in FIG., and/or by a TGA profile as indicated in FIG.and/or by an IR spectrum as indicated in FIG.

Polymorph of the hydrochloride of the (4-hydroxycarbamoyl-phenyl)-carbamic acid (6-dimethylamino methyl-2-naphthalenyl) ester

A process is described for preparing fesoterodine and/or fesoterodine fumarate comprising the esterification of (R)-feso deacyl with isobutyric acid or a precursor thereof, such as an isobutyryl halide or the isobutyric acid anhydride to give fesoterodine, in a mixture of water at alkaline pH and/or at least one organic solvent. This process allows obtaining products with high yields and purities, and in particular a product having a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-isobutyroyloxymethyl-phenyl isobutyrate less than 1% by mole and a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol less than 0.05% by mole.

Method for preparing fesoterodine and/or fesoterodine fumarate

Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy -4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater ability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprises the steps of: a) suspending 1-cyclopropyl-7-(S,S)-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro -8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating the product which is separated, (form A) and, additionally, e), reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.5% and 0.01% by weight, f) isolating the product (form B).

Polymorphs of 1-cyclopropy1-7-([s,s])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride and methods for the preparation thereof

Described is a new process for producing temozolomide, comprising the reaction between 5-aminoimidazole-4-carboxamide and N-succinimidyl-N'-methyl carbamate and the subsequent reaction of the thus obtained carbamoyl 5-aminoimidazole-4-carboxamide with sodium nitrite. Temozolomide is then purified by chromatography on adsorbent polymeric resin and subsequent crystallization from water and acetone.

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Rome, Italy

Stefano Turchetta