Patent number: 10023539
Abstract: 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.
Type:
Grant
Filed:
December 8, 2015
Date of Patent:
July 17, 2018
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
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
Publication number: 20170342034
Abstract: 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 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.
Type:
Application
Filed:
December 8, 2015
Publication date:
November 30, 2017
Applicant:
Bayer Pharma Aktiengesellschaft
Inventors:
Jeffrey Stuart MOWAT, Timo STELLFELD, Carlo STRESEMANN, Roman HILLIG, Silke KÖHR, Detlef STÖCKIGT, Jörg WEISKE, Thomas BRUMBY, Naomi BARACK, Clara CHRIST, Antonius TER LAAK, Volker BADOCK, Rosemary Helen CRAMPTON, Ian STEFANUTI