Aryl-cyanoguanidine compounds

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...

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Main Authors Köhr, Silke, Christ, Clara, Badock, Volker, Hillig, Roman, Ter Laak, Antonius, Stellfeld, Timo, Crampton, Rosemary Helen, Stöckigt, Detlef, Brumby, Thomas, Weiske, Jörg, Stresemann, Carlo, Mowat, Jeffrey Stuart, Stefanuti, Ian, Barak, Naomi
Format Patent
LanguageEnglish
Published 17.07.2018
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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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 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.
AbstractList 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 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.
Author Weiske, Jörg
Ter Laak, Antonius
Badock, Volker
Crampton, Rosemary Helen
Stöckigt, Detlef
Köhr, Silke
Stresemann, Carlo
Stellfeld, Timo
Christ, Clara
Hillig, Roman
Mowat, Jeffrey Stuart
Brumby, Thomas
Stefanuti, Ian
Barak, Naomi
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– fullname: Ter Laak, Antonius
– fullname: Stellfeld, Timo
– fullname: Crampton, Rosemary Helen
– fullname: Stöckigt, Detlef
– fullname: Brumby, Thomas
– fullname: Weiske, Jörg
– fullname: Stresemann, Carlo
– fullname: Mowat, Jeffrey Stuart
– fullname: Stefanuti, Ian
– fullname: Barak, Naomi
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Snippet The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory...
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SubjectTerms CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Title Aryl-cyanoguanidine compounds
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