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公开(公告)号：US11339124B2
公开(公告)日：2022-05-24
申请号：US16967871
申请日：2019-02-05
发明人： Peter Vandenabeele , Tom Vanden Berghe , Koen Augustyns , Sam Hofmans , Pieter Van Der Veken , Lars Devisscher
IPC分类号： C07C311/39 , C07D227/02 , C07D295/027 , C07D221/00 , C07D241/04 , C07D227/04
摘要： The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate.
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公开(公告)号：US09862678B2
公开(公告)日：2018-01-09
申请号：US15525480
申请日：2015-11-16
发明人： Peter Vandenabeele , Tom Vanden Berghe , Koen Augustyns , Jurgen Joossens , Pieter Van Der Veken , Sam Hofmans
IPC分类号： C07C311/39 , C07C311/40 , C07D295/26 , C07D213/38 , C07D239/26
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.
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3.发明申请DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES 审中-公开用于治疗和/或预防感染性疾病的分离的TRIAZINE二聚体公开(公告)号：US20140323488A1
公开(公告)日：2014-10-30
申请号：US14356762
申请日：2012-11-09
申请人： Wim LEWI , Universiteit Antwerpen , Shakturana CV
发明人： Venkatraj Muthusamy , Louis Maes , Jan Heeres , Koen Augustyns , Pieter Van Der Veken , Jurgen Joossens , Paulas Joannes Lewi
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , C07D251/52 , C07D251/70
摘要： The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.
摘要翻译： 本发明涉及包含通过有机接头共价连接的两个二取代三嗪环的新化合物（I），从而产生二聚体。 这些化合物显示针对感染性疾病如非洲锥虫病，恰加斯病，利什曼病，疟疾和艾滋病毒的致病感染因子的活性。 本发明还涉及这些疾病的预防和/或治疗。
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公开(公告)号：US09346814B2
公开(公告)日：2016-05-24
申请号：US14372798
申请日：2013-01-17
发明人： Koen Jansen , Ingrid De Meester , Leen Heirbaut , Jonathan D Cheng , Jurgen Joossens , Koen Augustyns , Pieter Van Der Veken
IPC分类号： C07D401/12 , C07D487/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
CPC分类号： C07D487/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
摘要翻译： 本发明涉及对FAP（成纤维细胞活化蛋白）具有高选择性和特异性的新型抑制剂。 所述抑制剂可用作人和/或兽医药物，特别是用于治疗和/或预防FAP相关疾病，例如但不限于增殖性疾病。
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公开(公告)号：US20220023320A1
公开(公告)日：2022-01-27
申请号：US17495447
申请日：2021-10-06
发明人： Koen Augustyns , Jurgen Joossens , Pieter Van Der Veken , Paul Cos , Cedric Joossen , Benedicte Yvonne De Winter , Hannah Ceuleers , Hanne Van Spaendonk
IPC分类号： A61K31/688 , A61P27/04 , A61P25/04
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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6.发明申请公开(公告)号：US20190175629A1
公开(公告)日：2019-06-13
申请号：US16301240
申请日：2017-05-18
发明人： Koen Augustyns , Jurgen Joossens , Pieter Van Der Veken , Paul Cos , Cedric Joossen , Benedicte Yvonne De Winter , Hannah Ceuleers , Hanne Van Spaendonk
IPC分类号： A61K31/688 , A61P25/04 , A61P27/04
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：US10017527B2
公开(公告)日：2018-07-10
申请号：US15128446
申请日：2015-03-30
发明人： Jurgen Joossens , Koen Augustyns , Anne-Marie Lambeir , Pieter Van Der Veken , Jeroen Van Soom , Viktor Magdolen
IPC分类号： C07F9/6561 , C07F9/40 , A61K49/00 , C07F9/58 , C07F9/655 , C07F9/6553 , C07F9/6509 , C07F9/6558 , C12Q1/37
CPC分类号： C07F9/6561 , A61K49/0052 , C07F9/4087 , C07F9/58 , C07F9/650952 , C07F9/6518 , 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.
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公开(公告)号：US20190284130A1
公开(公告)日：2019-09-19
申请号：US16463544
申请日：2017-11-24
发明人： Koen Augustyns , Matthias Cleenewerck , Guido R.Y. De Meyer , Jurgen Joossens , Ammar Kurdi , Pieter Van Der Veken , Christel Vangestel , Sigrid Stroobants , Wim Martinet
IPC分类号： C07C235/82 , C07C69/757 , C07C62/38
摘要： The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
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公开(公告)号：US09650348B2
公开(公告)日：2017-05-16
申请号：US14385843
申请日：2013-03-18
发明人： Jan Heeres , Koen Augustyns , Pieter Van Der Veken , Jurgen Joossens , Venkatraj Muthusamy , Kevin Karel Florentina Arien , Guido Louis Emile Vanham , Paulus Lewi
IPC分类号： C07D251/70 , C07D251/52 , A61K31/53 , A61P31/18 , A61K31/18
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.
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公开(公告)号：US20140357650A1
公开(公告)日：2014-12-04
申请号：US14372798
申请日：2013-01-17
发明人： Koen Jansen , Ingrid De Meester , Leen Heirbaut , Jonathan D. Cheng , Jurgen Joossens , Koen Augustyns , Pieter Van Der Veken
IPC分类号： C07D487/04 , C07D471/04 , C07D417/12 , C07D413/12 , C07D401/12 , C07D403/12
CPC分类号： C07D487/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
摘要翻译： 本发明涉及对FAP（成纤维细胞活化蛋白）具有高选择性和特异性的新型抑制剂。 所述抑制剂可用作人和/或兽医药物，特别是用于治疗和/或预防FAP相关疾病，例如但不限于增殖性疾病。
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