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公开(公告)号：EP3601267A1
公开(公告)日：2020-02-05
申请号：EP18717840.5
申请日：2018-03-19
发明人： WORTMANN, Lars , SAUTIER, Brice , EIS, Knut , BRIEM, Hans , BÖHNKE, Niels , VON NUSSBAUM, Franz , HILLIG, Roman , BADER, Benjamin , SCHRÖDER, Jens , PETERSEN, Kirstin , LIENAU, Philip , WENGNER, Antje, Margret , MOOSMAYER, Dieter , WANG, Qiuwen , SCHICK, Hans
IPC分类号： C07D403/12 , C07D405/14 , C07D401/12 , C07D403/04 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D239/94 , C07D417/12 , C07D487/04 , C07D495/04 , A61P35/00 , A61K31/517
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公开(公告)号：EP3230274B1
公开(公告)日：2019-01-30
申请号：EP15807653.9
申请日：2015-12-08
发明人： MOWAT, Jeffrey Stuart , STELLFELD, Timo , STRESEMANN, Carlo , HILLIG, Roman , KÖHR, Silke , STÖCKIGT, Detlef , WEISKE, Jörg , BRUMBY, Thomas , BARACK, Naomi , CHRIST, Clara , TER LAAK, Antonius , BADOCK, Volker , CRAMPTON, Rosemary Helen , STEFANUTI, Ian
IPC分类号： C07D403/12 , C07D231/06 , C07D401/12 , C07D413/12 , A61K31/506 , A61P35/00
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公开(公告)号：EP3230274A1
公开(公告)日：2017-10-18
申请号：EP15807653.9
申请日：2015-12-08
发明人： MOWAT, Jeffrey Stuart , STELLFELD, Timo , STRESEMANN, Carlo , HILLIG, Roman , KÖHR, Silke , STÖCKIGT, Detlef , WEISKE, Jörg , BRUMBY, Thomas , BARACK, Naomi , CHRIST, Clara , TER LAAK, Antonius , BADOCK, Volker , CRAMPTON, Rosemary Helen , STEFANUTI, Ian
IPC分类号： C07D403/12 , C07D231/06 , C07D401/12 , C07D413/12 , A61K31/506 , A61P35/00
CPC分类号： C07D231/06 , C07D401/12 , C07D403/12 , C07D413/12
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, 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.
摘要翻译： 本发明涉及蛋白质 - 赖氨酸N-甲基转移酶SMYD2（含SET和MYND结构域的蛋白质2）抑制剂，特别是通式（I）的SMYD2抑制性取代的氰基胍 - 吡唑啉，其中R 1，R 2，R 3，R 4，R 5，X和r具有本文所述和定义的含义，以及包含本发明化合物的药物组合物，以及它们对过度增殖性疾病，特别是对于癌症和肿瘤疾病的预防和治疗用途。 本发明还涉及SMYD2抑制剂用于良性增生，动脉粥样硬化病症，败血症，自身免疫病症，血管病症，病毒感染，神经变性病症，炎性病症，动脉粥样硬化病症和男性生育力的控制中的用途。
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公开(公告)号：EP3390387A1
公开(公告)日：2018-10-24
申请号：EP16829402.3
申请日：2016-12-15
发明人： SCHULZE, Volker , HEINRICH, Tobias , PRINZ, Florian , LEFRANC, Julien , SCHRÖDER, Jens , MENGEL, Anne , BONE, Wilhelm , BÁLINT, Joszef , WENGNER, Antje Margret , EIS, Knut , IRLBACHER, Horst , KOPPITZ, Marcus , BÖMER, Ulf , BADER, Benjamin , BRIEM, Hans , LIENAU, Philip , CHRIST, Clara , STÖCKIGT, Detlef , HILLIG, Roman , EHEIM, Ashley , KOSEMUND, Dirk , MÖNNING, Ursula , HARB, Hassan, Y.
IPC分类号： C07D401/14 , C07D405/14 , C07D401/12 , C07D409/14 , C07D451/14 , C07D471/08 , C07D487/08 , A61K31/407
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D451/14 , C07D471/08 , C07D487/08
摘要： The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.
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公开(公告)号：EP3283480A1
公开(公告)日：2018-02-21
申请号：EP16716211.4
申请日：2016-04-14
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
IPC分类号： C07D403/12 , C07D231/06 , C07D401/12 , A61K31/444 , A61K31/4155 , A61P35/00 , A61P29/00 , A61P15/16 , A61P9/10 , A61P31/12
CPC分类号： C07D231/06 , A61P35/00 , C07D401/12 , C07D403/12
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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公开(公告)号：EP3283478A1
公开(公告)日：2018-02-21
申请号：EP16716549.7
申请日：2016-04-14
发明人： STELLFELD, Timo , STRESEMANN, Carlo , HILLIG, Roman , KÖHR, Silke , STÖCKIGT, Detlef , WEISKE, Jörg , BARAK, Naomi , CHRIST, Clara , TER LAAK, Antonius , BADOCK, Volker
IPC分类号： C07D403/04 , A61K31/415 , A61P35/00 , A61K31/45
CPC分类号： C07D403/04 , A61P35/00 , C07C267/00 , C07D207/12 , C07D231/06
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, R3, R4, R5 and n 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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