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公开(公告)号：US20220409618A1
公开(公告)日：2022-12-29
申请号：US17820667
申请日：2022-08-18
申请人： Adverio Pharma GmbH
发明人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Walter Kroh , Andreas Knorr , Eva-Maria Becker , Frank Wunder , Volkhart Min-Jian Li , Elke Hartmann , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat , Donald Bierer
IPC分类号： A61K31/506 , A61K45/06 , C07D471/04 , C07C57/145 , C07C309/04 , C07C309/05
摘要： The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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公开(公告)号：US11508483B2
公开(公告)日：2022-11-22
申请号：US16423371
申请日：2019-05-28
申请人： ADVERIO PHARMA GMBH
IPC分类号： G16H50/30 , G16H50/50 , G16H50/70 , G16H50/20 , G01N33/564
摘要： The present invention relates to a method of identifying a subgroup of patients suffering from diffuse cutaneous systemic sclerosis (dcSSc) which subgroup of patients benefits from a treatment with at least one sGC stimulator and/or sGC activator in a higher degree than patients not belonging to this subgroup.
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![FORMS OF METHYL {4,6-DIAMINO-2-[1 (2-FLUOROBENZYL)-1H-PYRAZOLO[3-4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE](/abs-image/US/2020/07/30/US20200239469A1/abs.jpg.150x150.jpg)
3.发明申请公开(公告)号：US20200239469A1
公开(公告)日：2020-07-30
申请号：US16848249
申请日：2020-04-14
申请人： Adverio Pharma GmbH
IPC分类号： C07D471/04 , A61K31/519
摘要： This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
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![PROCESS FOR PREPARING METHYL{4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}METHYLCARBAMATE AND ITS PURIFICATION FOR USE AS PHARMACEUTICALLY ACTIVE COMPOUND](/abs-image/US/2019/09/19/US20190284186A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190284186A1
公开(公告)日：2019-09-19
申请号：US16433743
申请日：2019-06-06
申请人： ADVERIO PHARMA GmbH
IPC分类号： C07D471/04 , C07C325/02 , C07D403/04 , C07D487/04
摘要： The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
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公开(公告)号：US09845300B2
公开(公告)日：2017-12-19
申请号：US15435964
申请日：2017-02-17
申请人： ADVERIO PHARMA GMBH
发明人： Peter Fey
IPC分类号： C07D265/30 , C07D295/104 , C07D471/04 , C07C309/04 , C07C317/04 , C07D295/067 , C07C303/28
CPC分类号： C07D295/104 , C07B2200/13 , C07C303/28 , C07C309/04 , C07C317/04 , C07D265/30 , C07D295/067 , C07D471/04 , C07C309/65
摘要： The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
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公开(公告)号：US11439642B2
公开(公告)日：2022-09-13
申请号：US16919385
申请日：2020-07-02
申请人： Adverio Pharma GmbH
发明人： Markus Follmann , Johannes-Peter Stasch , Gorden Redlich , Jens Ackerstaff , Nils Griebenow , Walter Kroh , Andreas Knorr , Eva-Maria Becker , Frank Wunder , Volkhart Min-Jian Li , Elke Hartmann , Joachim Mittendorf , Karl-Heinz Schlemmer , Rolf Jautelat , Donald Bierer
IPC分类号： A61K31/506 , A61K45/06 , C07D471/04 , C07C57/145 , C07C309/04 , C07C309/05
摘要： The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
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![Process for preparing methyl{4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate and its purification for use as pharmaceutically active compound](/abs-image/US/2020/02/25/US10570130B2/abs.jpg.150x150.jpg)
公开(公告)号：US10570130B2
公开(公告)日：2020-02-25
申请号：US16433743
申请日：2019-06-06
申请人： ADVERIO PHARMA GmbH
IPC分类号： C07D487/04 , C07D471/04 , C07D403/04 , C07C325/02 , C07D239/48 , C07D239/50
摘要： The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
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![FORMS OF METHYL {4,6-DIAMINO-2-[1 (2-FLUOROBENZYL)-1H-PYRAZOLO[3-4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE](/abs-image/US/2018/12/27/US20180370970A1/abs.jpg.150x150.jpg)
8.发明申请公开(公告)号：US20180370970A1
公开(公告)日：2018-12-27
申请号：US16119671
申请日：2018-08-31
申请人： Adverio Pharma GmbH
IPC分类号： C07D471/04
摘要： This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and 1/4-ethyl acetate solvate.
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![Forms of methyl {4,6-diamino-2-[1 (2-fluorobenzyl)-1h-pyrazolo[3-4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate](/abs-image/US/2018/10/02/US10087183B2/abs.jpg.150x150.jpg)
公开(公告)号：US10087183B2
公开(公告)日：2018-10-02
申请号：US15672921
申请日：2017-08-09
申请人： Adverio Pharma GmbH
IPC分类号： A61K31/506 , C07D471/04
摘要： This present invention relates to forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I, Modification II, mono-DMSO solvate, sesqui-DMSO solvate and ¼-ethyl acetate solvate.
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![FORMS OF METHYL {4,6-DIAMINO-2-[1 (2-FLUOROBENZYL)-1H-PYRAZOLO[3-4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE](/abs-image/US/2017/11/23/US20170334910A1/abs.jpg.150x150.jpg)
10.发明申请公开(公告)号：US20170334910A1
公开(公告)日：2017-11-23
申请号：US15672921
申请日：2017-08-09
申请人： Adverio Pharma GmbH
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： This present invention relates to forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I, Modification II, mono-DMSO solvate, sesqui-DMSO solvate and ¼-ethyl acetate solvate.
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