Esteve Quimica S.a.

Laboratorios Del Dr. Esteve S.a.

Laboratories Del Dr. Esteve S.a.

Jorge Medrano Rupérez

Ramón Berenguer Maimó

Jordi Benet Buchholz

Laura Coppi

Julio Campon Pardo

Laura Puig Fernandez

Yolanda Gasanz Guillén

Laia Pellejà Puxeu

Laia Elías Rius

Martí Bartra Sanmartí

Martí Bartra Sanmarti

Jorge Garcia Gomez

Javier Ariza Piquer

Juan Francisco Merodio Cabanillas

Jorge García Gómez

Julio Campón Pardo

Ramon Berenguer Maimó

The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.

4-[-2-[[5-methyl-1-(2-naphtalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorphs and solvates

The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors. 

Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors

Process for removal of the amino protective group of a N-acylated {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R&#x2550;H or a (C-C)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity. 

Process for the preparation of abacavir

Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where Ris a (C-C)-alkyl radical with anhydrous hydrochloric acid/(C-C)-alcohol, and then with tri(C-C)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir. 

New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.

Solid forms of the magnesium salt of S-omeprazole and processes for their preparation

Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(&#x2212;) or (R)-(+)-[1,1'-Binaphthalene]-2,2&#x2032;-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.

Process for the preparation of optically active derivatives of 2-(2-pyridylmethylsulfinyl)-benzimidazole via inclusion complex with 1,1'-binaphthalene-2,2&#x2032;diol

An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.

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Barcelona, Spain

Jorge Medrano Rupérez