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1.发明申请SUBSTITUTED CYCLOALKENOPYRAZOLES AS BUB1 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开作为治疗癌症的BUB1抑制剂的替代环孢噻嗪公开(公告)号：US20150141372A1
公开(公告)日：2015-05-21
申请号：US14400315
申请日：2013-05-08
发明人： Marion Hitchcock , Christoph-Stephan Hilger , Anne Mengel , Hans Briem , Simon Holton , Vera Pütter , Gerhard Siemeister , Stefan Prechtl , Amaury Ernesto Fernández-Montalván , Christian Stegmann , Cornelia Preuße , Mark Jean Gnoth
IPC分类号： C07D401/14 , A61K31/506 , A61K31/695 , A61K31/5377 , C07D405/14 , C07F7/18 , C07D403/04 , A61K45/06
CPC分类号： C07D401/14 , A61K31/506 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D403/04 , C07D405/14 , C07F7/1804 , C07F7/188
摘要： Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
摘要翻译： 式（I）化合物，其生产方法及其作为Bub1激酶抑制剂用于治疗对细胞死亡诱导反应的过度增殖性疾病和/或病症的用途。
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公开(公告)号：US10975060B2
公开(公告)日：2021-04-13
申请号：US16463076
申请日：2017-11-24
发明人： Markus Berger , Jessica Lohrke , Christoph-Stephan Hilger , Gregor Jost , Thomas Frenzel , Olaf Panknin , Hubertus Pietsch
IPC分类号： C07D403/14 , C07D257/02 , A61K49/10
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.
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公开(公告)号：US10137209B2
公开(公告)日：2018-11-27
申请号：US15578687
申请日：2016-05-30
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.
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公开(公告)号：US20190083659A1
公开(公告)日：2019-03-21
申请号：US16192185
申请日：2018-11-15
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.
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公开(公告)号：US09416125B2
公开(公告)日：2016-08-16
申请号：US14400315
申请日：2013-05-08
发明人： Marion Hitchcock , Christoph-Stephan Hilger , Anne Mengel , Hans Briem , Simon Holton , Vera Pütter , Gerhard Siemeister , Stefan Prechtl , Amaury Ernesto Fernández-Montalván , Christian Stegmann , Cornelia Preuβe , Mark Jean Gnoth
IPC分类号： A61K31/506 , C07D401/14 , C07D405/14 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D403/04 , C07F7/18
摘要： Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
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公开(公告)号：US11814369B2
公开(公告)日：2023-11-14
申请号：US17218907
申请日：2021-03-31
发明人： Markus Berger , Jessica Lohrke , Christoph-Stephan Hilger , Gregor Jost , Thomas Frenzel , Olaf Panknin , Hubertus Pietsch
IPC分类号： C07D403/14 , A61K49/10 , C07D257/02
CPC分类号： C07D403/14 , A61K49/106 , 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.
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公开(公告)号：US11491245B2
公开(公告)日：2022-11-08
申请号：US16947272
申请日：2020-07-27
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.
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公开(公告)号：US10722601B2
公开(公告)日：2020-07-28
申请号：US16192185
申请日：2018-11-15
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.
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