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：US20170190719A1

公开(公告)日：2017-07-06

申请号：US15321176

申请日：2015-07-20

Applicant: BRACCO IMAGING S.P.A.

Inventor： Roberta MAZZON ,  Roberta FRETTA ,  Pier Lucio ANELLI

IPC: C07F5/00 ,  A61K49/18 ,  A61K49/10

Abstract: The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.

公开(公告)号：US20160228583A1

公开(公告)日：2016-08-11

申请号：US15130160

申请日：2016-04-15

Applicant: BRACCO IMAGING S.p.A.

Inventor： Pier Lucio ANELLI ,  Pierfrancesco MOROSINI ,  Silvia CERAGIOLI ,  Fulvio UGGERI ,  Luciano LATTUADA ,  Roberta FRETTA ,  Aurelia FERRIGATO

IPC: A61K49/18 ,  C07C213/10 ,  B29C67/24 ,  C07C227/40

CPC classification number: A61K49/1887 ,  A61K9/0019 ,  B29C67/24 ,  C07C213/10 ,  C07C227/38 ,  C07C227/40 ,  Y10T428/2982 ,  C07C229/22

Abstract: The present invention discloses a process for the preparation of gadobenate dimeglumine complex in a solid form. In particular, said solid form is conveniently obtained by spray-drying a corresponding liquid suspension at a given temperature and concentration. The present invention is particularly advantageous for the industrial scale as the solid form may be obtained by employing water as a solvent, which is a non-toxic solvent, easy to handle and basically not requiring troublesome health or safety precautions.

Abstract translation: 本发明公开了一种以固体形式制备钆酸二甲酚络合物的方法。 特别地，所述固体形式通过在给定温度和浓度下喷雾干燥相应的液体悬浮液而方便地得到。 本发明对于工业规模是特别有利的，因为固体形式可以通过使用水作为溶剂，其是无毒溶剂，易于处理并且基本上不需要麻烦的健康或安全预防措施来获得。

公开(公告)号：US20200071341A1

公开(公告)日：2020-03-05

申请号：US16678082

申请日：2019-11-08

Applicant: BRACCO IMAGING S.P.A.

Inventor： Roberta MAZZON ,  Roberta FRETTA ,  Pier Lucio ANELLI

IPC: C07F5/00 ,  A61K49/18 ,  A61K49/10 ,  C07C227/40 ,  A61K9/00 ,  A61K9/14

Abstract: The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.

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。