Aryl-cyanoguanidine compounds

US10023539B2 · kind B2 · utility

Assignee

• Bayer Pharma Aktiengesellschaft · DE

Inventors

• Jeffrey Stuart MOWAT · Berlin, DE
• Timo Stellfeld · Berlin, DE
• Carlo STRESEMANN · Berlin, DE
• Roman Hillig · Berlin, DE
• Silke Köhr · Teltow, DE
• Detlef STÖCKIGT · Potsdam, DE
• Jörg WEISKE · Berlin, DE
• Thomas Brumby · Berlin, DE
• Naomi Barak · Berlin, DE
• Clara Christ · Leverkusen, DE
• Antonius Ter Laak · Berlin, DE
• Volker BADOCK · Berlin, DE
• Rosemary Helen CRAMPTON · Bollington, GB
• Ian STEFANUTI · Chapel-en-le-Frith, GB

Key dates

• Filing date: Dec 8, 2015
• Grant date: Jul 17, 2018
• Expiry date: Dec 8, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.