Abstract: The invention relates to a method of Magnetic Resonance (MR) detection, in particular 13C-MR detection, by using a diagnostic medium comprising a hyperpolarized ester, in particular ethyl acetoacetate. The method comprises the detection of the MR signal of a hyperpolarized 13C carboxylic ester and of its respective hyperpolarized metabolite.
Type:
Application
Filed:
January 30, 2014
Publication date:
December 31, 2015
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Pernille Rose JENSEN, LERCHE H. Mathilde, Magnus KARLSSON, Claudia CABELLA, Sonia COLOMBO SERRA, Luigi MIRAGOLI, Luca VENTURI, Fabio TEDOLDI
Abstract: The present invention relates to a process for the preparation of iodinated phenols, —in particular, it relates to a process including the electrochemical iodination of 3,5-disubstituted phenols of formula (1) to the corresponding 3,5-disubstituted-2, 4,6-triiodophenols of formula (2), which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. Furthermore, the present invention includes the electrochemical iodination of 3, 5- disubstituted anilines of formula (6) to the corresponding 3,5-disubstituted-2,4,6-triiodoanilins of formula (7).
Type:
Grant
Filed:
February 16, 2009
Date of Patent:
November 24, 2015
Assignee:
BRACCO IMAGING S.P.A.
Inventors:
Giovanni Battista Giovenzana, Camilla Cavallotti, Luciano Lattuada, Fulvio Uggeri
Abstract: The present invention relates to a continuous method for the preparation of (S)-2-acetyloxypropionic acid from an aqueous solution of lactic acid and acetic anhydride, in acetic acid. (S)-2-acetyloxypropionic acid is used for the preparation of (S)-2-acetyloxypropionic acid chloride, an essential intermediate compound for the preparation of lopamidol and has to be industrially produced with high purity and suitable quality for producing lopamidol according to the Pharmacopoeia requirements. The continuous process according to the invention, comprises therefore also the chlorination steps of (S)-2-acetyloxypropionic acid with thionyl chloride to give the corresponding (S)-2-acetyloxypropionic acid chloride which is further distilled to give the suitable purity characteristics for its use for the preparation of non-ionic iodinated contrast agents as lopamidol.
Type:
Application
Filed:
December 4, 2013
Publication date:
November 19, 2015
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Silvia CERAGIOLI, Pietro DELOGU, Armando MORTILLARO, Alfonso NARDELLI, Stefano SGUASSERO, Rosario VELARDI, Carlo Felice VISCARDI
Abstract: The present invention describes a process for the synthesis of a iodinating agent, being said iodinating agent iodine chloride (ICI.) In particular, the present invention relates to a process for the electrochemical preparation of ICI, as a useful iodinating agent in the preparation of iodinated organic compounds for use as contrast agents or their precursors in the synthesis of the same.
Type:
Grant
Filed:
July 6, 2010
Date of Patent:
October 13, 2015
Assignee:
Bracco Imaging S.P.A.
Inventors:
Pier Lucio Anelli, Carlo Felice Viscardi, Pietro Delogu, Fabrizio Goffredi, Alfonso Nardelli, Giovanni Battista Giovenzana
Abstract: Hyperpolarized 1-13C-2-oxoglutarate as contrast agent in 13C Magnetic Resonance diagnostic technique (13C-MRI) for use in the diagnosis of cancer. In particular, upon administration of said 1-13C-2-oxoglutarate, signals of 1-13C-glutamate are detected. More in particular, different MR signals from 13C nuclei are detected and compared, said comparison being useful to determine a difference between tumor and non-tumor tissues, to determine the aggressiveness of a tumor or the efficacy of an anti-tumor therapy.
Type:
Application
Filed:
October 24, 2013
Publication date:
October 1, 2015
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Claudia Cabella, Lara Caminiti, Sonia Colombo Serra, Pernille Rose Jensen, Magnus Karlsson, Mathilde H. Lerche, Luigi Miragoli, Luisa Poggi, Fabio Tedoldi, Luca Venturi
Abstract: The present invention relates to paramagnetic solid lipid nanoparticles (pSLNs) comprising an amphiphilic paramagnetic metal chelating moiety selected from: a diazepine derivative of Formula I and a tetraazocyclododecane derivative of Formula (II): being said chelating moiety complexed to a paramagnetic metal ion selected from the group consisting of: Gd(III), Mn(II), Cr(III), Cu(II), Fe(III), Pr(III), Nd(III), Sm(III), Tb(III), Yb(III), Dy(III), Ho(III) and Er(III), or salts thereof. The invention further relates to the process for preparation of said solid lipid nanoparticles comprising amphiphilic complexes of paramagnetic metals (pSLNs) and to the use of pSLNs as MRI contrast agents in the diagnostic field.
Abstract: 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 ?-hydroxyacid or a salt thereof.
Type:
Grant
Filed:
March 12, 2010
Date of Patent:
August 4, 2015
Assignee:
Bracco Imaging S.P.A.
Inventors:
Pier Lucio Anelli, Marino Brocchetta, Roberta Fretta, Luciano Lattuada, Armando Mortillaro
Abstract: The present invention generally relies on a process for the preparation of chelated compounds, comprising the selective interaction between a solid matrix and a chelating agent. In more details, the present invention enables the preparation of chelated compounds useful as diagnostic agents, in high yields and in a reliable way.
Abstract: New radical compounds, useful in the field of MRI imaging of formula (I). The radical compounds are in particular new triarylmethyl (“trityl”) radicals which can be used as polarizing agents for polarizing a molecule in the DNP process.
Type:
Application
Filed:
July 4, 2013
Publication date:
June 4, 2015
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Pernille Rose Jensen, Magnus Karlsson, Mathilde H. Lerche, Roberta Napolitano, Fabio Tedoldi, Massimo Visigalli
Abstract: Method for manufacturing a hyperpolarized amino acid, in particular glutamine, which substantially limits the formation of by-products, with respect to conventional aqueous preparations of sodium hydroxide with amino acids. The amino acid is in particular admixed with the hydroxide in the substantial absence of water and the dry mixture is dissolved in an anhydrous solvent in the presence of a polarizing agent. The obtained mixture is then subjected to a DNP process and can be used in metabolic MR imaging.
Type:
Application
Filed:
March 28, 2013
Publication date:
April 30, 2015
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Pernille Rose Jensen, Magnus Karlsson, Mathilde H. Lerche
Abstract: The present invention discloses the use of L-Histidine to reduce Gadolinium accumulation into target organs, preventing its toxic effects, after administration of gadolinium based contrast agents. The invention thus, also disclose the use of L-Histidine to prevent the NSF syndrome in patients with renal functionality impairment. A kit of part is also disclosed by the use of which toxicity associated to free Gd3+, deriving from GDBCA, is prevented by oral administration of L-histidine before administration of the contrast agent. A method for the prevention of toxic metal accumulation which consists in the administration, preferably by the oral route, of L-Histidine is also disclosed. L-Histidine is preferably administered as a single oral dose comprised from 0.2-20 g.
Abstract: The present invention generally relies on a process for the preparation of chelated compounds, comprising the selective interaction between a solid matrix and a chelating agent. In more details, the present invention enables the preparation of chelated compounds useful as diagnostic agents, in high yields and in a reliable way.
Abstract: The invention relates to a one-step process for the preparation of aqueous solutions of hyperpolarized molecules in which, in a single step, the said hyperpolarized molecules are separated from the crude solution by means of a fast phase-transfer extraction and isolated in an impurity-free aqueous solution, ready for use in the MRI diagnostic imaging of organs, region or tissues of the human or animal body.
Type:
Grant
Filed:
September 30, 2009
Date of Patent:
February 24, 2015
Assignee:
Bracco Imaging S.p.A.
Inventors:
Francesca Reineri, Alessandra Viale, Giovanni Battista Giovenzana, Daniela Santelia, Walter Dastru′, Roberto Gobetto, Silvio Aime, Fulvio Uggeri
Abstract: The invention provides MRI detectable species of formula (I) Dp-Sn-Nm??(I) wherein D is a MRI detectable moiety S is a spacer N is a molecule of a nutrient or pseudo-nutrient n is 0 or an integer m is an integer and p is an integer. These compounds are useful for internalizing into tumor cells an amount of the MRI detectable moiety that is distinguishably higher than the amount internalized in normal healthy cells thus allowing the diagnosis of tumors. The internalization of the MRI detectable moiety involves the nutrients or pseudo-nutrients transporting system. Preferred compounds of formula (I) are those wherein D is the chelated complex of a paramagnetic metal ion.
Abstract: The present invention relates to a new class of diazepine-derivatives as chelating agents for paramagnetic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
Abstract: The present invention generally relates to a composition comprising acetic anhydride, a DNP agent and a gadolinium complex and its use for the preparation of hyperpolarised imaging agent for MR diagnostic analysis.
Type:
Application
Filed:
December 3, 2012
Publication date:
November 20, 2014
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Silvio Aime, Sonia Colombo Serra, Pernille Rose Jensen, Magnus Karlsson, Mathilde H. Lerche, Fabio Tedoldi, Massimo Visigalli
Abstract: 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.
Type:
Grant
Filed:
July 14, 2011
Date of Patent:
September 16, 2014
Assignee:
Bracco Imaging S.p.A.
Inventors:
Pier Lucio Anelli, Marino Brocchetta, Enrico Cappelletti, Ornella Gazzotti
Abstract: The present invention relates to a process for the preparation of aqueous solutions of hyperpolarized carboxylic organic acids ready for use in in-vivo MR diagnostic imaging, and the use of the corresponding anhydrides or esters as glass-forming agents.
Type:
Application
Filed:
October 11, 2012
Publication date:
September 11, 2014
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Silvio Aime, Sonia Colombo Serra, Giovanni Battista Giovenzana, Pernille Rose Jensen, Magnus Karlsson, Mathilde H. Lerche, Fabio Tedoldi
Abstract: The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.
Type:
Application
Filed:
April 10, 2014
Publication date:
August 7, 2014
Applicant:
BRACCO IMAGING S.P.A.
Inventors:
Pier Lucio ANELLI, Maria ARGESE, Valeria BOI, Livio CAVALIERI, Laura GALIMBERTI, Sonia GAZZETTO, Luciano LATTUADA, Fulvia VELLA
Abstract: The present invention relates to a method for the in vivo, ex vivo, or in vitro determination of physical or chemical parameters of diagnostic interest by use of a slow tumbling paramagnetic agent that is responsive to changes of said physical or chemical parameter through changes in the R2p/R1p ratio allowing the determination of the said parameter in a manner that is independent on the actual agent concentration.