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![Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain](/abs-image/US/2024/01/23/US11878967B2/abs.jpg.150x150.jpg)
公开(公告)号：US11878967B2
公开(公告)日：2024-01-23
申请号：US17252804
申请日：2019-06-17
申请人： Merck Patent GmbH
发明人： Michael Lange , Clemens Kuehn , Tobias Schlueter , Werner Mederski , David Maillard , Edoardo Burini
IPC分类号： C07D401/12 , A61P35/00 , A61P37/00 , A61K31/506
CPC分类号： C07D401/12 , C07B2200/13
摘要： A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methy}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.
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公开(公告)号：US09932337B2
公开(公告)日：2018-04-03
申请号：US15528116
申请日：2015-11-19
申请人： Merck Patent GmbH
IPC分类号： C07D487/04 , C07D471/04 , C07D217/14 , C07C59/64 , C07C59/84
CPC分类号： C07D471/04 , C07B2200/07 , C07C59/64 , C07C59/84 , C07D217/14
摘要： The present invention relates to methods for the production of enantiopure or enantioenriched Praziquantel precursors and to methods for the production of enantiopure or enantioenriched Praziquantel comprising the methods for the production of the Praziquantel precursors. The present invention further relates to compounds or intermediates useful in such methods.
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公开(公告)号：US11465964B2
公开(公告)日：2022-10-11
申请号：US16967781
申请日：2019-02-05
申请人： Merck Patent GmbH
发明人： Camille Correia , Renaud Poli , Serge Gerbaut , Marc Dittmann , David Maillard , Sebastian Haertner
IPC分类号： C07C277/08 , C07C279/26
摘要： The present invention relates to an improved process for the preparation of metformin hydrochloride, an important drug in the first line treatment of Type II Diabetes.
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公开(公告)号：US10160758B2
公开(公告)日：2018-12-25
申请号：US15528282
申请日：2015-11-17
申请人： MERCK PATENT GMBH
IPC分类号： C07D471/04 , C07C31/30 , C07B55/00 , C07B57/00
摘要： The present invention relates to a method for the racemization of enantiomerically pure or enantiomerically enriched Praziquantel under basic conditions and a method for the production of (R)-Praziquantel in enantiopure or enantiomerically enriched form, which comprises the racemization method.
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![Crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol](/abs-image/US/2021/08/31/US11103512B2/abs.jpg.150x150.jpg)
公开(公告)号：US11103512B2
公开(公告)日：2021-08-31
申请号：US16498873
申请日：2018-03-28
申请人： Merck Patent GmbH
发明人： Michael Lange , Clemens Kuehn , Thomas Fuchss , David Maillard , Marcel Breuning , Marco Poma , Edoardo Burini
IPC分类号： A61K31/5375 , C07D413/00 , A61P35/00 , A61K31/5377 , A61K45/06 , A61N5/10 , C07D403/10
摘要： A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.
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公开(公告)号：US10273213B2
公开(公告)日：2019-04-30
申请号：US15756267
申请日：2016-08-10
申请人： Merck Patent GmbH
IPC分类号： C07D217/14 , C07B53/00 , B01J31/12 , B01J31/24 , C07D401/04
摘要： The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound and subsequent cyclization.
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![NOVEL CRYSTALLINE FORMS OF 1-(4-{[6-AMINO-5-(4-PHENOXY-PHENYL)-PYRIMIDIN-4-YLAMINO]-METHYL}-4-FLUORO-PIPERIDIN-1-YL)-PROPENONE, SALT FORMS THEREOF, AND PROCESSES TO OBTAIN](/abs-image/US/2024/04/25/US20240132472A1/abs.jpg.150x150.jpg)
公开(公告)号：US20240132472A1
公开(公告)日：2024-04-25
申请号：US18532710
申请日：2023-12-07
申请人： Merck Patent GmbH
发明人： Michael LANGE , Clemens Kuetin , Tobias Schiueter , Werner Mederski , David Maillard , Edoardo Burini
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07B2200/13
摘要： A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.
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![NOVEL CRYSTALLINE FORMS OF 1-(4-{[6-AMINO-5-(4-PHENOXY-PHENYL)-PYRIMIDIN-4-YLAMINO]-METHYL}-4-FLUORO-PIPERIDIN-1-YL)-PROPENONE, SALT FORMS THEREOF, AND PROCESSES TO OBTAIN](/abs-image/US/2021/08/26/US20210261525A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210261525A1
公开(公告)日：2021-08-26
申请号：US17252804
申请日：2019-06-17
申请人： Merck Patent GmbH
发明人： Michael LANGE , Clemens Kuehn , Tobias Schlueter , Werner Mederski , David Maillard , Edoardo Burini
IPC分类号： C07D401/12
摘要： A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methy}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.
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![Crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol](/abs-image/US/2021/07/20/US11065255B2/abs.jpg.150x150.jpg)
公开(公告)号：US11065255B2
公开(公告)日：2021-07-20
申请号：US16498873
申请日：2018-03-28
申请人： Merck Patent GmbH
发明人： Michael Lange , Clemens Kuehn , Thomas Fuchss , David Maillard , Marcel Breuning , Marco Poma , Edoardo Burini
IPC分类号： A61K31/5375 , C07D413/00 , A61P35/00 , A61K31/5377 , A61K45/06 , A61N5/10 , C07D403/10
摘要： A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.
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![Solid form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol](/abs-image/US/2021/07/06/US11053233B2/abs.jpg.150x150.jpg)
公开(公告)号：US11053233B2
公开(公告)日：2021-07-06
申请号：US16498905
申请日：2018-03-28
申请人： Merck Patent GmbH
发明人： Michael Lange , Clemens Kuehn , Thomas Fuchss , David Maillard , Marcel Breuníng , Marco Poma , Edoardo Burini
IPC分类号： C07D413/14 , B01D9/00
摘要： An anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be used in pharmaceutical compositions.
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