Almirall, S.a.

Inke, S.a.

Juan Antonio Perez Andres

Maria Prat Quinones

Pere Dalmases Barjoan

Carlos Puig Duran

Maria Prat Quiñones

Francesc Carrera Carrera

Montserrat Julia Jane

Francesca Pajuelo Lorenzo

Joan Huguet Clotet

Jordi Bessa Belmunt

The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a dicarboxylic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.

Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both muscarinic receptor antagonist and &#x3b2;2 adrenergic receptor agonist activities

The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a hydroxycarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.

Salts of 2-amino-1-hydroxyethyl-8-hydroxyquinolin-2(1H)-one derivatives having both &#x3b2;2 adrenergic receptor agonist and M3 muscarinic receptor antagonist activities

The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency. 

Method for obtaining a pharmaceutically active compound, synthesis intermediates thereof and methods for obtaining them

This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation. 

Process for the preparation of Valsartan and precursors thereof

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Sant Feliu de Llobregat, Spain

Juan Antonio Perez Andres