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公开(公告)号：EP3458072B1
公开(公告)日：2020-09-30
申请号：EP17729390.9
申请日：2017-05-18
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2.发明公开
公开(公告)号：EP3218357A1
公开(公告)日：2017-09-20
申请号：EP15797953.5
申请日：2015-11-16
发明人： VANDENABEELE, Peter , VANDEN BERGHE, Tom , AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , HOFMANS, Sam
IPC分类号： C07D239/26 , C07C311/39 , C07C311/40 , C07D295/26 , C07D213/38 , A61K31/18 , A61K31/4409 , A61K31/495 , A61K31/535 , A61P25/28
CPC分类号： C07C311/39 , C07C311/40 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D213/38 , C07D239/26 , C07D295/26
摘要： This disclosure relates to a novel class of compounds having the structure of formula I as defined herein and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. This disclosure also comprises methods of treating a subject by administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof to the subject. These compounds are useful for the conditions disclosed herein. This disclosure further comprises methods for making the compounds of formula I and corresponding intermediates.
摘要翻译： 本发明涉及具有式（I）结构的新型化合物和包含式（I）化合物或其药学上可接受的盐的药物组合物。 这些化合物抑制或减少非细胞凋亡性细胞死亡形式的铁浓化和/或氧化，使它们可用于治疗本文公开的各种病症。
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公开(公告)号：EP1940856A1
公开(公告)日：2008-07-09
申请号：EP06806436.9
申请日：2006-10-20
发明人： AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , LAMBEIR, Anne-Marie Virginie Renée , SCHARPÉ, Simon , HAEMERS, Achiel
IPC分类号： C07F9/40
CPC分类号： C07F9/4006 , C07F9/4084
摘要： The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to the use of said uPA inhibitor compounds as a medicament and the use of said uPA inhibitor compounds for the preparation of a medicament for the treatment of conditions chosen from the group comprising cancer, tumour growth, tumour invasion, tumour metastasis, diabetic retinopathy, hemorrhagic atherosclerosis and inflammatory conditions, such as rheumatoid arthritis and psoriasis.
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公开(公告)号：EP3544952A1
公开(公告)日：2019-10-02
申请号：EP17801477.5
申请日：2017-11-24
发明人： AUGUSTYNS, Koen , CLEENEWERCK, Matthias , DE MEYER, Guido R.Y. , JOOSSENS, Jurgen , KURDI, Ammar , VAN DER VEKEN, Pieter , VANGESTEL, Christel , STROOBANTS, Sigrid , MARTINET, Wim
IPC分类号： C07C69/757 , C07C62/38 , C07C235/82 , A61K31/167 , A61K31/215 , A61P35/00
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5.发明公开
公开(公告)号：EP3458072A1
公开(公告)日：2019-03-27
申请号：EP17729390.9
申请日：2017-05-18
发明人： AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , COS, Paul , JOOSSEN, Cedric , DE WINTER, Benedicte Yvonne , CEULEERS, Hannah , VAN SPAENDONK, Hanne
摘要： The present invention relates to compounds for use in the prevention and/or treatment of PAR-related diseases, such as for example: pain and ocular disorders. More in particular, the present invention provides bis(acetamidophenyl) guanidinophenylethylphosphonates for use in the prevention and/or treatment of pancreatitis-related pain, IBS (irritable bowel syndrome), IBD (inflammatory bowel disease), dry eye disease and conjunctivitis sicca. These inhibitors were found to have a different inhibitory profile compared to diphenyl guanidinophenylethylphosphonates leading to a more pronounced effect on these conditions.
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公开(公告)号：EP2804859B1
公开(公告)日：2019-06-12
申请号：EP13701410.6
申请日：2013-01-17
发明人： JANSEN, Koen , DE MEESTER, Ingrid , HEIRBAUT, Leen , CHENG, Jonathan D , JOOSSENS, Jurgen , AUGUSTYNS, Koen , VAN DER VEKEN, Pieter
IPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/401 , A61P35/00
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公开(公告)号：EP3122758A1
公开(公告)日：2017-02-01
申请号：EP15722454.4
申请日：2015-03-30
发明人： JOOSSENS, Jurgen , AUGUSTYNS, Koen , LAMBEIR, Anne-Marie , VAN DER VEKEN, Pieter , VAN SOOM, Jeroen , MAGDOLEN, Viktor
IPC分类号： C07F9/6539 , C07F9/6561
CPC分类号： C07F9/6561 , A61K49/0052 , C07F9/4087 , C07F9/588 , C07F9/650964 , C07F9/650988 , C07F9/65182 , C07F9/6539 , C07F9/65515 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C12Q1/37 , G01N2333/96433
摘要： The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.
摘要翻译： 本发明涉及具有获得对KLK4的有效抑制活性所必需的共同化学结构和/或可用于检测KLK4肽及其活性的新型化合物和探针。 它还涉及这些化合物和方法在体外和体内通过利用所述探针或抑制剂来抑制和/或检测KLK4活性的用途。 本发明的化合物至少在苯胍（而不是例如苄基胍）和/或尾组中存在杂原子的情况下与现有技术化合物不同，它们的组合存在意外地导致有效和选择性的KLK4抑制活性 。
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公开(公告)号：EP1940856B1
公开(公告)日：2014-10-08
申请号：EP06806436.9
申请日：2006-10-20
发明人： AUGUSTYNS, Koen , JOOSSENS, Jurgen , VAN DER VEKEN, Pieter , LAMBEIR, Anne-Marie Virginie Renée , SCHARPÉ, Simon , HAEMERS, Achiel
IPC分类号： C07F9/40
CPC分类号： C07F9/4006 , C07F9/4084
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9.发明授权TRIAZINES WITH SUITABLE SPACERS FOR TREATMENT AND/OR PREVENTION OF HIV INFECTIONS 有权TRITZINES具有适合治疗和/或预防HIV感染的间隔物
公开(公告)号：EP2828244B1
公开(公告)日：2017-11-15
申请号：EP13714873.0
申请日：2013-03-18
发明人： HEERES, Jan , VAN DER VEKEN, Pieter , JOOSSENS, Jurgen , MUTHUSAMY, Venkatraj , AUGUSTYNS, Koen , ARIËN, Kevin Karel Florentina , VANHAM, Guido Louis Emile
IPC分类号： C07D251/70 , A61K31/53 , A61P31/18
CPC分类号： C07D251/70 , A61K31/18 , A61K31/53 , C07D251/52
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10.发明公开TRIAZINES WITH SUITABLE SPACERS FOR TREATMENT AND/OR PREVENTION OF HIV INFECTIONS 有权与用于治疗和/或预防感染艾滋病毒APPROPRIATE SPACERS三嗪
公开(公告)号：EP2828244A1
公开(公告)日：2015-01-28
申请号：EP13714873.0
申请日：2013-03-18
发明人： HEERES, Jan , VAN DER VEKEN, Pieter , JOOSSENS, Jurgen , MUTHUSAMY, Venkatraj , AUGUSTYNS, Koen , ARIËN, Kevin Karel Florentina , VANHAM, Guido Louis Emile
IPC分类号： C07D251/70 , A61K31/53 , A61P31/18
CPC分类号： C07D251/70 , A61K31/18 , A61K31/53 , C07D251/52
摘要： The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.
摘要翻译： 本发明涉及HIV-1感染的领域，并且具体提供了含有三嗪环和合适的间隔基的新型化合物。 化合物gemäß本发明非常适合于HIV-1感染的预防和/或治疗和抗HIV-1的NNRTI抗性病毒特别表现出改进的活性。
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