- 专利标题： NOVEL ARYL-CYANOGUANIDINE COMPOUNDS
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申请号： EP16716211.4申请日： 2016-04-14
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公开(公告)号： EP3283480A1公开(公告)日： 2018-02-21
- 发明人: STELLFELD, Timo , MOWAT, Jeffrey Stuart , STRESEMANN, Carlo , HILLIG, Roman , KÖHR, Silke , STÖCKIGT, Detlef , WEISKE, Jörg , HARTUNG, Ingo , BARAK, Naomi , CHRIST, Clara , TERLAAK, Antonius , BADOCK, Volker , CRAMPTON, Rosemary Helen , STEFANUTI, Ian
- 申请人： Bayer Pharma Aktiengesellschaft
- 申请人地址： Müllerstrasse 178 13353 Berlin DE
- 专利权人： Bayer Pharma Aktiengesellschaft
- 当前专利权人： Bayer Pharma Aktiengesellschaft
- 当前专利权人地址： Müllerstrasse 178 13353 Berlin DE
- 代理机构： BIP Patents
- 优先权： EP15163997 20150417
- 国际公布： WO2016166186 20161020
- 主分类号： C07D403/12
- IPC分类号： C07D403/12 ; C07D231/06 ; C07D401/12 ; A61K31/444 ; A61K31/4155 ; A61P35/00 ; A61P29/00 ; A61P15/16 ; A61P9/10 ; A61P31/12
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.
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