公开(公告)号：US20140221477A1

公开(公告)日：2014-08-07

申请号：US14249542

申请日：2014-04-10

Applicant: BRACCO IMAGING S.P.A.

Inventor： Pier Lucio ANELLI ,  Maria ARGESE ,  Valeria BOI ,  Livio CAVALIERI ,  Laura GALIMBERTI ,  Sonia GAZZETTO ,  Luciano LATTUADA ,  Fulvia VELLA

IPC: C07C303/24

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.

Abstract translation: 本发明涉及通过从相应的方法开始制备3,5-二碘-O- [3-碘-4-（磺酰氧基）苯基] -L-酪氨酸衍生物（T3S）的单钠盐的方法 酚类化合物，在氯磺酸和二甲基乙酰胺作为溶剂的存在下。 如此获得的T3S化合物可以方便地以纯的形式以良好的产率分离为固体。 本发明还涉及T3S制备方法，其中起始试剂是T2，并且还包含片剂中这种化合物的制剂。 此外，本发明公开了基于T3S衍生物的非放射性免疫测定法。

公开(公告)号：US20230040042A1

公开(公告)日：2023-02-09

申请号：US17784232

申请日：2020-12-09

Applicant: BRACCO IMAGING S.P.A.

Inventor： Aurelia FERRIGATO ,  Sonia GAZZETTO

IPC: C07D257/02

Abstract: The invention relates to a process for the one-step preparation and isolation of a protected DO3A such as DO3A-tri-tert-butyl ester as a solid salt.

公开(公告)号：US20180118669A1

公开(公告)日：2018-05-03

申请号：US15853506

申请日：2017-12-22

Applicant: BRACCO IMAGING S.p.A.

Inventor： Pier Lucio ANELLI ,  Maria ARGESE ,  Valeria BOI ,  Livio CAVALIERI ,  Laura GALIMBERTI ,  Sonia GAZZETTO ,  Luciano LATTUADA ,  Federico MAISANO ,  Giovanni RIVOLTA ,  Fulvia VELLA

IPC: C07C303/24 ,  C07F1/04 ,  C07D495/04 ,  A61K31/198 ,  A61K9/20 ,  C07C227/16 ,  C07C305/24 ,  C07C229/36

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.

公开(公告)号：US20250051292A1

公开(公告)日：2025-02-13

申请号：US18718945

申请日：2022-12-13

Applicant: BRACCO IMAGING S.P.A.

Inventor： Sonia GAZZETTO ,  Valeria BOI ,  Andrea BANIN ,  Andrea BARALE

IPC: C07D257/00 ,  C07F11/00

Abstract: The present invention relates to a process for the manufacturing of a mixture comprising the intermediate 1-[bis[2-hydroxy-3-[4,7,10-tris[2-(1,1-dimethylethoxy)-2-oxoethyl]-1,4,7,10-tetraazacyclododec-1-yl]propyl]amino]-1-deoxy-D-glucitol. Such intermediate is useful for the synthesis of the dimeric gadolinium complex [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]propyl]amino]-1-deoxy-D-glucitolate(6-)]]digadolinium complex, which can be employed as a contrast agent in the field of diagnostic imaging, and in particular of Magnetic Resonance Imaging (MRI).

公开(公告)号：US20240425527A1

公开(公告)日：2024-12-26

申请号：US18719054

申请日：2022-12-13

Applicant: BRACCO IMAGING S.P.A.

Inventor： Sonia GAZZETTO ,  Valeria BOI ,  Andrea BANIN ,  Andrea BARALE

IPC: C07F5/00

Abstract: The invention relates to a process for the preparation of the gadolinium dimeric contrast agent [p-[1-[bis[2-(hydroxy-KO)-3-[4,7,10-tris[(carboxy-KO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-K/V1,K/V4,K/V7,K/V10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex. Such process includes preparation steps carried out one-pot and without isolation of the obtained intermediates. The gadolinium dimeric contrast agent can be for use in diagnostic imaging, in particular in Magnetic resonance Imaging (MRI).

公开(公告)号：US20230303592A1

公开(公告)日：2023-09-28

申请号：US18017939

申请日：2021-07-26

Applicant: BRACCO IMAGING S.P.A.

Inventor： Andrea BARALE ,  Valeria BOI ,  Aurelia FERRIGATO ,  Sonia GAZZETTO ,  Daniela GIARDINA-PAPA ,  Armando MORTILLARO ,  Laura ORIO ,  Massimo VERANI

IPC: C07F5/00

CPC classification number: C07F5/003

Abstract: The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-kO)-3-[4,7,10-tris[(carboxy-kO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-kN1,kN4,kN7,kN10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot and without isolation of the obtained intermediate.