公开(公告)号：US10736896B2

公开(公告)日：2020-08-11

申请号：US15981598

申请日：2018-05-16

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： C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  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.

公开(公告)号：US10364229B2

公开(公告)日：2019-07-30

申请号：US15812524

申请日：2017-11-14

申请人： ADVERIO PHARMA GMBH

发明人： Peter Fey ,  Alfons Grunenberg ,  Donald Bierer

IPC分类号： C07D239/02 ,  C07D295/104 ,  C07D265/30 ,  C07D471/04 ,  C07C309/04 ,  C07C317/04 ,  C07D295/067 ,  C07C303/28 ,  A61P9/00

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.

公开(公告)号：US20190177288A1

公开(公告)日：2019-06-13

申请号：US16278813

申请日：2019-02-19

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY

IPC分类号： C07D295/104 ,  A61P9/00 ,  C07D471/04 ,  C07D295/067 ,  C07D265/30 ,  C07C317/04 ,  C07C309/04 ,  C07C303/28

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.

公开(公告)号：US20180282329A1

公开(公告)日：2018-10-04

申请号：US16000382

申请日：2018-06-05

申请人： Adverio Pharma GmbH

发明人： Franz-Josef MAIS ,  Joachim REHSE ,  Winfried JOENTGEN ,  Konrad SIEGEL

IPC分类号： C07D471/04 ,  C07C325/02 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07C325/02 ,  C07D239/48 ,  C07D239/50 ,  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.

公开(公告)号：US20160009671A1

公开(公告)日：2016-01-14

申请号：US14796703

申请日：2015-07-10

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY

IPC分类号： C07D295/104 ,  C07D471/04 ,  C07C317/04 ,  C07D295/067

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.

摘要翻译： 本申请涉及一种制备新颖的式（Ⅵ）取代的5-氟-1H-吡唑并吡啶的新颖且有效的方法，它们适合作为制备药物和用于制备用于治疗和/或预防心血管的药物的中间体 疾病 更具体地，式（VI）的5-氟-1H-吡唑并吡啶适用于制备用于制备药物的式（I）化合物，用于制备用于治疗和/或预防心血管疾病的药物 。

公开(公告)号：US20230067593A1

公开(公告)日：2023-03-02

申请号：US17759958

申请日：2021-02-02

申请人： ADVERIO PHARMA GMBH

发明人： Elisabeth KERSTEN ,  Michael OSTENDORF ,  Werner HOHEISEL ,  Heike NEUMANN ,  Michal SOWA ,  Joerg BROCKOB ,  Peter FEY ,  Markus LONGERICH ,  Guido BECKER ,  Valentina Paula CONTY ,  Anja EHRIG

IPC分类号： C07D471/04 ,  A61K9/16 ,  A61K9/107 ,  A61K47/10

摘要： The present invention relates to stable nanosuspensions of methyl {4,6-diamino-2-[5-fluoro-1-(2- fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate (Vericiguat, compound of formula (I)), processes for preparing the stable nanosuspensions, nanoparticles comprising the compound of formula (I), and pharmaceutical compositions in solid form made from the nanosuspensions.

公开(公告)号：US20220089554A1

公开(公告)日：2022-03-24

申请号：US17424866

申请日：2020-01-15

申请人： Adverio Pharma GmbH

发明人： Peter Fey ,  Sergii Pazenok ,  Christian Funke ,  Natalya Pavlovna Kolesnik ,  Olexandr Ivanovich Guzyr ,  Yuriy Grigorievich Shermolovich

IPC分类号： C07D295/067

摘要： The present application relates to a novel, cost-saving and efficient process for preparing 4-(2,2,3,3-tetrafluoropropyl)morpholine which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

公开(公告)号：US20220073515A1

公开(公告)日：2022-03-10

申请号：US17526129

申请日：2021-11-15

申请人： Adverio Pharma GmbH

发明人： Birgit KEIL ,  Franz-Josef MAIS ,  Winfried JOENTGEN ,  Alfons GRUNENBERG

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.

公开(公告)号：US10662188B2

公开(公告)日：2020-05-26

申请号：US16119671

申请日：2018-08-31

申请人： Adverio Pharma GmbH

发明人： Birgit Keil ,  Franz-Josef Mais ,  Winfried Joentgen ,  Alfons Grunenberg

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.

公开(公告)号：US10351562B2

公开(公告)日：2019-07-16

申请号：US16000382

申请日：2018-06-05

申请人： Adverio Pharma GmbH

发明人： Franz-Josef Mais ,  Joachim Rehse ,  Winfried Joentgen ,  Konrad Siegel

IPC分类号： C07D239/48 ,  C07D239/50 ,  C07D471/04 ,  C07D487/04 ,  C07D403/04 ,  C07C325/02

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.