公开(公告)号：US20180065942A1

公开(公告)日：2018-03-08

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： C07D295/104 ,  C07D295/067 ,  C07C317/04 ,  C07C309/04 ,  C07D265/30 ,  C07D471/04 ,  C07C303/28 ,  C07C309/65

CPC分类号： C07D295/104 ,  A61P9/00 ,  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.

公开(公告)号：US20230219952A1

公开(公告)日：2023-07-13

申请号：US18001834

申请日：2021-06-15

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY ,  Nadine BREMEYER ,  Markus LONGERICH ,  Thomas FRENZEL ,  Helene FABER ,  Michal SOWA ,  Joerg BROCKOB ,  Guido BECKER ,  Heike NEUMANN

IPC分类号： C07D471/04 ,  C07D295/067

CPC分类号： C07D471/04 ,  C07D295/067

摘要： The present application relates to a novel and efficient process with high yield for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate of the formula (I) in the crystalline form of modification I, wherein the x-ray diffractogram of the compound of the formula (I) in modification exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 22.7, in very high purity which is significantly more cost-effective than the process known from the art and can be performed in customary pilot- and production plant-equipment (stirred tank/devices for isolation).

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：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：US20170158652A1

公开(公告)日：2017-06-08

申请号：US15435964

申请日：2017-02-17

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY ,  Alfons GRUNENBERG ,  Donald BIERER

IPC分类号： C07D295/104

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.

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：US20190177287A1

公开(公告)日：2019-06-13

申请号：US16278778

申请日：2019-02-19

申请人： ADVERIO PHARMA GMBH

发明人： Peter FEY ,  Alfons Grunenberg ,  Donald Bierer

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.