公开(公告)号：US11427578B1

公开(公告)日：2022-08-30

申请号：US16632273

申请日：2018-07-12

申请人： Bayer Pharma Aktiengesellschaft ,  Bayer Aktiengesellschaft ,  Deutsches Krebsforschungszentrum

发明人： Jeffrey Stuart Mowat ,  Bernd Buchmann ,  Nuria Aiguabella Font ,  Gabriele Leder ,  Rafael Carretero ,  Olaf Panknin ,  Roland Neuhaus ,  Robin Michael Meier ,  Sandra Berndt ,  Kirstin Petersen ,  Rienk Offringa

IPC分类号： C07D471/04 ,  A61K45/06

摘要： The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

公开(公告)号：US10023539B2

公开(公告)日：2018-07-17

申请号：US15534404

申请日：2015-12-08

申请人： Bayer Pharma Aktiengesellschaft

发明人： Jeffrey Stuart Mowat ,  Timo Stellfeld ,  Carlo Stresemann ,  Roman Hillig ,  Silke Köhr ,  Detlef Stöckigt ,  Jörg Weiske ,  Thomas Brumby ,  Naomi Barak ,  Clara Christ ,  Antonius Ter Laak ,  Volker Badock ,  Rosemary Helen Crampton ,  Ian Stefanuti

IPC分类号： C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R1, R2, R3, R4, R5, X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyper-proliferative disorders, in particular for cancer, respectively tumor disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.