Dibra S.p.a.

Bracco Imaging S.p.a.

Bracco International Bv

Marino Brocchetta

Pier Lucio Anelli

Fulvio Uggeri

Massimo Visigalli

Ornella Gazzotti

Enrico Cappelletti

Giovanna Lux

Giuseppe Manfredi

Franco Fedeli

Daniela Palano

Luciano Lattuada

Christoph De Haen

Pierfrancesco Morosini

Chiara Gallotti

Giorgio Ripa

Maria Argese

Roberta Fretta

Mario Virtuani

Luisella Calabi

Fabrizio Rebasti

Michele Serleti

Marco Lolli

Armando Mortillaro

Lino Paleari

Pierlucio Anelli

Lucio Pier Anelli

The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available &#x3b1;-hydroxyacid or a salt thereof.

Process for the preparation of triiodinated carboxylic aromatic derivatives

The present invention relates to a process for the preparation of 5-[(2-hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives comprising the Smiles rearrangement of a suitable precursor, by contact of an aqueous solution of this latter with an anion exchanger solid phase.

Process for the preparation of contrast agents

A process for the preparation of (S)-N,N'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starting from 5-amino-N,N&#x2032;-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein Ris a hydrogen atom, a C&#xf7;Cstraight or branched alkoxy group, Ris hydrogen, a C&#xf7;Cstraight or branched alkoy group and R3 ?is a C&#xf7;Cstraight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions. The invention also refers to the new intermediates of formula (III) and (IV) wherein &#x2014;R is a group A.

Process for the preparation of iopamidol and the new intermediates therein

The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein Rrepresents a straight or branched (C-C)-alkyl group, with at least the stoichiometric amount of an amine of formula HNR.

Process for the preparation of N,N-substituted 5-amino-1,3-benzenedicarboxamides

A process for the preparation of (S)-N,N'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starting from 5-amino-N,N&#x2032;-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein Ris a hydrogen atom, a C&#xf7;Cstraight or branched alkoxy group, Ris hydrogen, a C&#xf7;Cstraight or branched alkoxy group and R3 ?is a C&#xf7;Cstraight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions. The invention also refers to the new intermediates of formula (III) and (IV) wherein &#x2014;R is a group A.

Process for the preparation of iopamidol and the new intermediated therein

A process for the preparation of compound of formula (I A), decahydro-2a,4a,6a,8a-tetraazacyclopent[fg]accnaphthylene and the corresponding functionalized compounds of general formula (I), intermediates for the preparation of 1,4,7,10-tetraazacyclododecane (II A) and corresponding derivatives (II), by preparation of compounds of general formula (III) and subsequent reduction thereof.

Process for the preparation of decahydro-2a,4a,6a,8a-tetraazacyclopent[fg]acenaphthylene and functionalized derivatives

Bile acid salts

Blood pool imaging contrast agents containing paramagnetic bi- and tri-valent metal ion chelates of bile acid conjugates with molecules having chelating activity are used in magnetic resonance imaging of the vascular system and particularly the coronaries.

Use of bile acid conjugates, derivatives thereof with metal complexes as blood pool agents for nuclear magnetic resonance diagnostics

Diagnostic imaging contrast agent with improved in serum relaxivity

Compounds of formula (I) both in the racemic and optically active forms, are used in MRI diagnostic imaging.

Manganese chelates with high relaxivity in serum

A process for the preparation of the compounds of general formula (I)

Process for the preparation of bile acid derivatives

Process for the manufacturing of iodinated contrast agents

A process for the preparation of compounds of general formula (I) ##STR1## characterized in that the corresponding derivatives of general formula (II) ##STR2## are reacted with the compounds of general formula (III) ##STR3## wherein Z is halogen atom or a reactive residue of a sulfonic acid or a --N.sup.+ (R.sub.9).sub.3 cation wherein R.sub.9 is a (C.sub.1 -C.sub.6) alkyl group and

This invention relates to novel compounds able to chelate paramagnetic bi- or trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI).

Macrocyclic chelants, their chelates and uses thereof in the diagnostic

The invention relates to novel contrast media particularly useful for X-ray diagnostic investigations of human and animal body.

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Milan, Italy

Marino Brocchetta