公开(公告)号：US10137209B2

公开(公告)日：2018-11-27

申请号：US15578687

申请日：2016-05-30

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Markus Berger ,  Jessica Lohrke ,  Christoph-Stephan Hilger ,  Gregor Jost ,  Thomas Frenzel ,  Detlev Suelzle ,  Johannes Platzek ,  Olaf Panknin ,  Hubertus Pietsch

IPC分类号： A61K49/10 ,  C07D257/02

摘要： The present invention relates to a new class of high relaxivity extracellular gadolinium chelate complexes, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents.

公开(公告)号：US11491245B2

公开(公告)日：2022-11-08

申请号：US16947272

申请日：2020-07-27

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Markus Berger ,  Jessica Lohrke ,  Christoph-Stephan Hilger ,  Gregor Jost ,  Thomas Frenzel ,  Detlev Suelzle ,  Johannes Platzek ,  Olaf Panknin ,  Hubertus Pietsch

IPC分类号： A61K49/10 ,  C07D257/02

摘要： A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[({2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl}amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

公开(公告)号：US10722601B2

公开(公告)日：2020-07-28

申请号：US16192185

申请日：2018-11-15

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Markus Berger ,  Jessica Lohrke ,  Christoph-Stephan Hilger ,  Gregor Jost ,  Thomas Frenzel ,  Detlev Suelzle ,  Johannes Platzek ,  Olaf Panknin ,  Hubertus Pietsch

IPC分类号： A61K49/10 ,  C07D257/02

摘要： A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[{2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl} amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.

公开(公告)号：US20190083659A1

公开(公告)日：2019-03-21

申请号：US16192185

申请日：2018-11-15

申请人： Bayer Pharma Aktiengesellschaft

发明人： Markus Berger ,  Jessica Lohrke ,  Christoph-Stephan Hilger ,  Gregor Jost ,  Thomas Frenzel ,  Detlev Suelzle ,  Johannes Platzek ,  Olaf Panknin ,  Hubertus Pietsch

IPC分类号： A61K49/10 ,  C07D257/02

摘要： A compound having the formula of tetragadolinium [4,10-bis(carboxylatomethyl)-7-{-3,6,12,15-tetraoxo-16-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]-9,9-bis({[{2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]propanoyl} amino)acetyl]amino}methyl)-4,7,11,14-tetraazaheptadecan-2-yl}-1,4,7,10-tetraazacyclo dodecan-1-yl]acetate wherein the stereochemistry at the chiral carbon of the four alanine substituents is selected from the group consisting of RRRR, SSSS, RSSS, RRSS, and RRRS stereoisomers, and racemic and diastereomeric mixtures of any thereof, or a tautomer, a hydrate, a solvate, or a salt thereof, or a mixture of same is described. The compounds may be used as an MRI contrast imaging agent.