Abstract: A method for the qualification and selection of manufacturing processes, raw materials, intermediates and batch production of pentosan polysulfate based on the identification of acetylated monosaccharide units, including units of xylose substituted with 4-O-methyl-glucuronic which also lead the acetyl group, as structural characterizing units, is disclosed.

Abstract: The object of the present invention is an anti-xylan sulfate antiserum having an antibody titre of between 1/10000 and 1/15000, and obtainable using a specific immunization method, and use thereof in one or more ELISA methods for determining xylan sulfate levels in biological fluids.

Abstract: The present invention relates to a process for the preparation of a polysaccharide composed of D-xylose units of formula (III) linked together via beta 1,4 glycosidic bonds wherein R1 is hydrogen or acetyl, R2 is hydrogen, acetyl or a 4-O-methyl glucuronic acid unit, wherein, when R2 is a 4-O-methyl glucuronic acid unit, the R1 group on the same saccharide unit is defined as G, wherein G is hydrogen or acetyl, and wherein the sugar unit at the reducing end of sun such polysaccharide is xylose, lyxose or xylulose, said process comprising the following steps: selective deacetylation of xylan extracted from beech wood; and isomerization of the selectively deacetylated xylan achieved in step or the following steps: isomerization of xylan extracted from beech wood; and selective deacetylation of isomerized xylan achieved in step. The process is useful for the preparation of pentosan polysulfate or pharmaceutically acceptable salts thereof for pharmaceutical use.

Abstract: The present invention relates to reversed phase high-performance liquid chromatography (HPLC) methods useful for the characterisation of glatiramer acetate or similar polypeptide mixtures. The method described herein can distinguish glatiramer acetate from non-conforming copolymers and may be used to choose batches of glatiramer acetate suitable for pharmaceutical use.

Abstract: A method for the qualification and selection of manufacturing processes, raw materials, intermediates and batch production of pentosan polysulfate based on the identification of acetylated monosaccharide units, including units of xylose substituted with 4-O-methyl-glucuronic which also lead the acetyl group, as structural characterizing units, is disclosed.

Abstract: A method for the qualification and selection of manufacturing processes, raw materials, intermediates and batch production of pentosan polysulfate based on the identification of acetylated monosaccharide units, including units of xylose substituted with 4-O-methyl-glucuronic which also lead the acetyl group, as structural characterizing units, is disclosed.

Abstract: A process for the purification of L-?-glycerophosphorylcholine is described, wherein L-?-glycerophosphorylcholine is crystallized from DMSO or from a mixture of DMSO with at least another solvent, preferably selected from water, alcohol, halogenated solvents, ethers, esters and/or amides. Such a process allows to obtain L-?-glycerophosphorylcholine having a purity greater than 99.5%, preferably greater than 99.7%, even more preferably greater than or equal to 99.9%. A method for determining the purity of L-?-glycerophosphorylcholine is also described, comprising the elution of L-?-glycerophosphorylcholine through an HPLC column having an amino stationary phase, and subsequent detection of L-?-glycerophosphorylcholine itself, and any impurity thereof, by means of an Evaporative Light Scattering Detector type.

Abstract: The present invention relates to simple size exclusion chromatography (SEC) analytical methods useful for the assessment of accurate molecular weight distributions (MWDs) of certain polypeptide mixtures known as glatiramoids. The use of a SEC method based on one or more broad MWD standards furnishes the absolute (not relative) molecular weight distribution profile of complex polypeptide mixtures like, for instance, the glatiramer acetate (GA) polymer.

Abstract: The present invention relates to a process for the preparation of a polysaccharide composed of D-xylose units of formula (III) linked together via beta 1,4 glycosidic bonds wherein R1 is hydrogen or acetyl, R2 is hydrogen, acetyl or a 4-O-methyl glucuronic acid unit, wherein, when R2 is a 4-O-methyl glucuronic acid unit, the R1 group on the same saccharide unit is defined as G, wherein G is hydrogen or acetyl, and wherein the sugar unit at the reducing end of sun such polysaccharide is xylose, lyxose or xylulose, said process comprising the following steps: selective deacetylation of xylan extracted from beech wood; and isomerization of the selectively deacetylated xylan achieved in step or the following steps: isomerization of xylan extracted from beech wood; and selective deacetylation of isomerized xylan achieved in step. The process is useful for the preparation of pentosan polysulfate or pharmaceutically acceptable salts thereof for pharmaceutical use.

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

Abstract: 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° 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.

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

Abstract: 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.

Abstract: 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: a) washing with a basic aqueous solution; b) concentration of the organic phase; c) addition of a polar organic solvent and/or a mixture of polar organic solvents; d) precipitation of the pemetrexed diethyl ester 2.

Abstract: 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 “(R)-feso deacyl”, called form B.

Abstract: 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.

Abstract: 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.

Abstract: 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 “(R)-feso deacyl”, called form B.

Abstract: The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C10-C30, pure or mixed together, and X?OH or OM, where M=alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.

Abstract: 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 stability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprise 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.