Patents by Inventor Koen Augustyns
Koen Augustyns has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 11638712Abstract: 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.Type: GrantFiled: October 6, 2021Date of Patent: May 2, 2023Assignee: Universiteit AntwerpenInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Paul Cos, Cedric Joossen, Benedicte Yvonne De Winter, Hannah Ceuleers, Hanne Van Spaendonk
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Patent number: 11339124Abstract: 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.Type: GrantFiled: February 5, 2019Date of Patent: May 24, 2022Assignees: UNIVERSITEIT ANTWERPEN, VIB VZW, UNIVERSITEIT GENTInventors: Peter Vandenabeele, Tom Vanden Berghe, Koen Augustyns, Sam Hofmans, Pieter Van Der Veken, Lars Devisscher
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Publication number: 20220023320Abstract: 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.Type: ApplicationFiled: October 6, 2021Publication date: January 27, 2022Applicant: Universiteit AntwerpenInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Paul Cos, Cedric Joossen, Benedicte Yvonne De Winter, Hannah Ceuleers, Hanne Van Spaendonk
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Patent number: 11166967Abstract: 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.Type: GrantFiled: May 18, 2017Date of Patent: November 9, 2021Assignee: Universiteit AntwerpenInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Paul Cos, Cedric Joossen, Benedicte Yvonne De Winter, Hannah Ceuleers, Hanne Van Spaendonk
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Publication number: 20210094909Abstract: 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.Type: ApplicationFiled: February 5, 2019Publication date: April 1, 2021Applicants: VIB VZW, Universiteit Antwerpen, Universiteit GentInventors: Peter VANDENABEELE, Tom VANDEN BERGHE, Koen AUGUSTYNS, Sam HOFMANS, Pieter VAN DER VEKEN, Lars DEVISSCHER
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Patent number: 10738002Abstract: 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.Type: GrantFiled: November 24, 2017Date of Patent: August 11, 2020Assignees: UNIVERSITAIR ZIEKENHUIS ANTWERPEN, UNIVERSITEIT ANTWERPENInventors: Koen Augustyns, Matthias Cleenewerck, Guido R. Y. De Meyer, Jurgen Joossens, Ammar Kurdi, Pieter Van Der Veken, Christel Vangestel, Sigrid Stroobants, Wim Martinet
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Publication number: 20190284130Abstract: 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.Type: ApplicationFiled: November 24, 2017Publication date: September 19, 2019Inventors: Koen Augustyns, Matthias Cleenewerck, Guido R.Y. De Meyer, Jurgen Joossens, Ammar Kurdi, Pieter Van Der Veken, Christel Vangestel, Sigrid Stroobants, Wim Martinet
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Publication number: 20190175629Abstract: 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.Type: ApplicationFiled: May 18, 2017Publication date: June 13, 2019Applicant: Universiteit AntwerpenInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Paul Cos, Cedric Joossen, Benedicte Yvonne De Winter, Hannah Ceuleers, Hanne Van Spaendonk
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Patent number: 10017527Abstract: 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.Type: GrantFiled: March 30, 2015Date of Patent: July 10, 2018Assignee: UNIVERSITEIT ANTWERPENInventors: Jurgen Joossens, Koen Augustyns, Anne-Marie Lambeir, Pieter Van Der Veken, Jeroen Van Soom, Viktor Magdolen
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Patent number: 9862678Abstract: 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.Type: GrantFiled: November 16, 2015Date of Patent: January 9, 2018Assignees: VIB VZW, Universiteit Gent, Universiteit AntwerpenInventors: Peter Vandenabeele, Tom Vanden Berghe, Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Sam Hofmans
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Publication number: 20170313653Abstract: 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.Type: ApplicationFiled: November 16, 2015Publication date: November 2, 2017Inventors: Peter VANDENABEELE, Tom VANDEN BERGHE, Koen AUGUSTYNS, Jurgen JOOSSENS, Pieter VAN DER VEKEN, Sam HOFMANS
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Patent number: 9650348Abstract: 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.Type: GrantFiled: March 18, 2013Date of Patent: May 16, 2017Assignees: Universiteit Antwerpen, Shakturana CVInventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi
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Publication number: 20170101427Abstract: 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.Type: ApplicationFiled: March 30, 2015Publication date: April 13, 2017Applicant: UNIVERSITEIT ANTWERPENInventors: Jurgen JOOSSENS, Koen AUGUSTYNS, Anne-Marie LAMBEIR, Pieter VAN DER VEKEN, Jeroen VAN SOOM, Viktor MAGDOLEN
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Patent number: 9346814Abstract: 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.Type: GrantFiled: January 17, 2013Date of Patent: May 24, 2016Assignees: Universiteit Antwerp, Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Publication number: 20150126510Abstract: 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.Type: ApplicationFiled: March 18, 2013Publication date: May 7, 2015Applicants: Universiteit Antwerpen, Shakturana CVInventors: Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Kevin Karel Florentina Arien, Guido Louis Emile Vanham, Paulus Lewi (deceased)
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Publication number: 20140357650Abstract: 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.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Publication number: 20140323488Abstract: 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.Type: ApplicationFiled: November 9, 2012Publication date: October 30, 2014Inventors: Venkatraj Muthusamy, Louis Maes, Jan Heeres, Koen Augustyns, Pieter Van Der Veken, Jurgen Joossens, Paulas Joannes Lewi
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Publication number: 20140079632Abstract: The present invention relates to selective trypsine-like serine protease activity-based probes, in particular urokinase plasminogen activator-activity based probes, the use thereof and methods for detecting selective urokinase activity by making use of said probes.Type: ApplicationFiled: May 9, 2012Publication date: March 20, 2014Applicant: UNIVERSITEIT ANTWERPENInventors: Koen Augustyns, Pieter Van Der Veken, Jonas Messagie, Jurgen Joossens, Anne-Marie Lambeir
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Patent number: 8003627Abstract: 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.Type: GrantFiled: October 20, 2006Date of Patent: August 23, 2011Assignee: Universiteit AntwerpenInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Anne-Marie Virginie Renée Lambeir, Simon Scharpé, Achiel Haemers
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Publication number: 20080312191Abstract: 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.Type: ApplicationFiled: October 20, 2006Publication date: December 18, 2008Applicant: UNIVERSITEIT ANTWERPENInventors: Koen Augustyns, Jurgen Joossens, Pieter Van Der Veken, Anne-Marie Virginie Renee Lambeir, Simon Scharpe, Achiel Haemers