Timo STELLFELD,Jeffrey Stuart MOWAT,Carlo STRESEMANN,Roman HILLIG,Silke KÖHR,Detlef STÖCKIGT,Jörg WEISKE,Ingo HARTUNG,Naomi BARAK,Clara CHRIST,Antonius TER LAAK,Volker BADOCK,Rosemary Helen CRAMPTON,I
申请号:
US15567059
公开号:
US20180099937A1
申请日:
2016.04.14
申请国别(地区):
US
年份:
2018
代理人:
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 and R5 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 hyperproliferative disorders, in particular for cancer, respectively tumour 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.