NOVEL 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 STÖCKIGT, Detlef, WEISKE, Jörg, STRESEMANN, Carlo, BARACK, Naomi, STELLFELD, Timo, STEFANUTI, Ian, BRUMBY, Thomas, BADOCK, Volker, CHRIST, Clara, KÖHR, Silke, CRAMPTON, Rosemary Helen, TER LAAK, Antonius, MOWAT, Jeffrey Stuart, HILLIG, Roman
Format Patent
LanguageEnglish
French
German
Published 18.10.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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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 CHRIST, Clara
STELLFELD, Timo
STRESEMANN, Carlo
CRAMPTON, Rosemary Helen
STEFANUTI, Ian
BADOCK, Volker
WEISKE, Jörg
BRUMBY, Thomas
KÖHR, Silke
HILLIG, Roman
MOWAT, Jeffrey Stuart
STÖCKIGT, Detlef
TER LAAK, Antonius
BARACK, Naomi
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– fullname: STRESEMANN, Carlo
– fullname: BARACK, Naomi
– fullname: STELLFELD, Timo
– fullname: STEFANUTI, Ian
– fullname: BRUMBY, Thomas
– fullname: BADOCK, Volker
– fullname: CHRIST, Clara
– fullname: KÖHR, Silke
– fullname: CRAMPTON, Rosemary Helen
– fullname: TER LAAK, Antonius
– fullname: MOWAT, Jeffrey Stuart
– fullname: HILLIG, Roman
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NOUVEAUX COMPOSÉS D'ARYL-CYANOGUANIDINE
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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
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
Title NOVEL ARYL-CYANOGUANIDINE COMPOUNDS
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