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公开(公告)号：US11427578B1
公开(公告)日：2022-08-30
申请号：US16632273
申请日：2018-07-12
发明人： Jeffrey Stuart Mowat , Bernd Buchmann , Nuria Aiguabella Font , Gabriele Leder , Rafael Carretero , Olaf Panknin , Roland Neuhaus , Robin Michael Meier , Sandra Berndt , Kirstin Petersen , Rienk Offringa
IPC分类号： C07D471/04 , A61K45/06
摘要： The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.
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公开(公告)号：US11311520B2
公开(公告)日：2022-04-26
申请号：US16983768
申请日：2020-08-03
发明人： Ulrich Klar , Rolf Bohlmann , Heike Schäcke , Detlev Sülzle , Stephan Menz , Olaf Panknin
IPC分类号： C07D471/04 , A61K31/437 , A61K31/5386 , C07D473/34 , C07D495/04 , C07D495/14 , C07D498/08 , C07D513/04 , C07D519/00
摘要： The present invention relates to substituted dihydroimidazopyridinedione compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative, angiogenesis disorders, inflammatory diseases or diseases associated with inflammatory pain, as a sole agent or in combination with other active ingredients.
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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：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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公开(公告)号：US09951027B2
公开(公告)日：2018-04-24
申请号：US15118157
申请日：2015-02-10
发明人： Hartmut Rehwinkel , Holger Siebeneicher , Sonja Anlauf , Duy Nguyen , Olaf Panknin , Sven Ring , Wolfgang Schwede , Marcus Bauser , Katja Zimmermann , Stefan Kaulfuss , Roland Neuhaus
IPC分类号： C07D235/30 , C07D409/12 , C07D401/12 , C07D405/12
CPC分类号： C07D235/30 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to benzimidazol-2-amines of general formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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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：US10414734B2
公开(公告)日：2019-09-17
申请号：US15744641
申请日：2016-07-12
发明人： Olaf Panknin , Sven Ring , Katja Zimmermann , Roland Neuhaus
IPC分类号： C07D235/30 , A61P35/00 , A61K31/4184 , A61K45/06
摘要： The present invention relates to benzimidazol-2-amines of general formula (I) in which R1, R2, R3, R4, R5, R6 and R7 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
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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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