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公开(公告)号：USRE49860E1
公开(公告)日：2024-03-05
申请号：US17087659
申请日：2020-11-03
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/13
摘要： The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)
and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).-
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：US20220153701A1
公开(公告)日：2022-05-19
申请号：US17435607
申请日：2020-02-28
发明人： Johannes Platzek
IPC分类号： C07D213/81
摘要： The present invention provides a method for preparing the process intermediate 4-amino-5-methylpyridone of the formula (I), characterized in that the intermediate 4-hydroxy-5-methyl-1H-pyridin-2-one of the formula (III) is reacted with ammonia in an autoclave with addition of an ammonium bromide salt.
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公开(公告)号：US20220153699A1
公开(公告)日：2022-05-19
申请号：US17435606
申请日：2020-02-28
发明人： Johannes Platzek , Kai Lovis
IPC分类号： C07D213/73
摘要： The present invention relates to a novel and improved method for preparing 4-amino-5-methylpyridone of the formula (I) which is an intermediate in the preparation of the MR antagonist finerenone.
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公开(公告)号：US10793532B2
公开(公告)日：2020-10-06
申请号：US16336217
申请日：2017-09-11
IPC分类号： C07D257/02
摘要： A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.
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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：US10399977B2
公开(公告)日：2019-09-03
申请号：US16114198
申请日：2018-08-27
IPC分类号： C07D471/04
摘要： The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).
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公开(公告)号：US12054481B2
公开(公告)日：2024-08-06
申请号：US17050303
申请日：2019-04-23
发明人： Johannes Platzek , Kai Lovis , Winfried Joentgen
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)
and also to the preparation of the enantiomer (Ia) by racemate resolution using chiral substituted tartaric acid esters of the general formulae (IIIa) and (IIIb)
where Ar represents a substituted or unsubstituted aromatic or heteroaromatic radical.-
公开(公告)号：US10392384B2
公开(公告)日：2019-08-27
申请号：US15753406
申请日：2016-08-18
IPC分类号： C25B3/02 , C25B3/04 , C25B15/08 , C07D471/04
摘要： The present invention relates to a novel process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and recovering (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) proceeding from (4R)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula ent-(I)
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公开(公告)号：US10336749B2
公开(公告)日：2019-07-02
申请号：US15753849
申请日：2016-08-18
发明人： Johannes Platzek
IPC分类号： C07D471/04
摘要： The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)
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