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：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.