Patents by Inventor Piet Herdewijn
Piet Herdewijn 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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Publication number: 20230104311Abstract: The present invention relates to the synthesis of 6-substituted 7-deazapurines and their corresponding nucleosides by coupling aryl or alkyl Grignard reagents with halogenated purine nucleosides in the presence of iron or an iron/copper mixture such as Fe(acac)3/CuI. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.Type: ApplicationFiled: February 17, 2020Publication date: April 6, 2023Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Piet HERDEWIJN, Elisabetta GROAZ, Li QINGFENG
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Patent number: 11040047Abstract: The present invention relates to novel phosphonoamidate prodrugs. The invention also relates to the use of these novel phosphonate-modified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses such as the herpes simplex virus 1, herpes simplex virus 2, human cytomegalovirus, varicella zoster virus, vaccinia virus and adenovirus.Type: GrantFiled: March 21, 2018Date of Patent: June 22, 2021Assignee: Katholieke Universiteit LeuvenInventors: Graciela Andrei, Steven De Jonghe, Elisabetta Groaz, Piet Herdewijn, Min Luo, Dominique Schols, Robert Snoeck
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Publication number: 20200016180Abstract: The present invention relates to novel phosphonoamidate prodrugs. The invention also relates to the use of these novel phosphonate-modified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses such as the herpes simplex virus 1, herpes simplex virus 2, human cytomegalovirus, varicella zoster virus, vaccinia virus and adenovirus.Type: ApplicationFiled: March 21, 2018Publication date: January 16, 2020Inventors: Graciela Andrei, Steven De Jonghe, Elisabetta Groaz, Piet Herdewijn, Min Luo, Dominique Schols, Robert Snoeck
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Publication number: 20190388441Abstract: The present invention relates to novel prodrugs of mizoribine, and a method for their preparation, as well as to pharmaceutical compositions comprising these prodrugs and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel prodrugs as biologically active ingredients, specifically in combination with other biologically active drugs such as immunosuppressants and/or immunomodulatory drugs, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and autoimmune disorders, organ and cells transplant rejection.Type: ApplicationFiled: January 22, 2018Publication date: December 26, 2019Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Piet Herdewijn, Ling-Jie Gao, Yuan Lin, Mark Waer
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Patent number: 10087209Abstract: The present invention relates to novel pro-drugs of L-2?-deoxythreose nucleoside phosphonates, such as phosphoramidate, phosphorodiamidate and phospho-diester pro-drugs. The invention also relates to a process for preparing these novel prodrugs of nucleoside phosphonates. The invention also relates to the use of these novel phosphonate-modified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the HBV family.Type: GrantFiled: April 27, 2016Date of Patent: October 2, 2018Assignee: KU LEUVEN RESEARCH & DEVELOPMENTInventors: Piet Herdewijn, Steven De Jonghe, Shrivinas Dumbre, Chao Liu
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Publication number: 20180105552Abstract: The present invention relates to novel pro-drugs of L-2?-deoxythreose nucleoside phosphonates, such as phosphoramidate, phosphorodiamidate and phospho-diester pro-drugs. The invention also relates to a process for preparing these novel prodrugs of nucleoside phosphonates. The invention also relates to the use of these novel phosphonate-modified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the HBV family.Type: ApplicationFiled: April 27, 2016Publication date: April 19, 2018Applicant: KU LEUVEN RESEARCH & DEVELOPMENTInventors: Piet HERDEWIJN, Steven DE JONGHE, Shrivinas DUMBRE, Chao LIU
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Patent number: 9730944Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.Type: GrantFiled: October 16, 2015Date of Patent: August 15, 2017Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
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Patent number: 9522932Abstract: The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.Type: GrantFiled: September 28, 2015Date of Patent: December 20, 2016Assignee: K.U. Leuven Research & DevelopmentInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
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Patent number: 9518066Abstract: The present invention relates to a class of novel isothiazolo[4,3-b]pyridine derivatives and a method for their preparation, as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel isothiazolo[4,3-b]pyridine derivatives as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, cell-proliferative and neurodegenerative diseases.Type: GrantFiled: July 4, 2014Date of Patent: December 13, 2016Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Sona Kovachova, Lei Chang, Michal Sala
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Publication number: 20160122364Abstract: The present invention relates to a class of novel isothiazolo[4,3-b]pyridine derivatives and a method for their preparation, as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel isothiazolo[4,3-b]pyridine derivatives as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, cell-proliferative and neurodegenerative diseases.Type: ApplicationFiled: July 4, 2014Publication date: May 5, 2016Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Piet Herdewijn, Steven De Jonghe, Sona Kovachova, Lei Chang, Michal Sala
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Patent number: 9301961Abstract: Compounds that bind to phosphatidylinositol-4-kinase III? (PI4KIII?) and inhibit the binding of PI4KIII? to its substrate and/or inhibit PI4KIII? activity may be used in the treatment and/or prevention of an autoimmune or inflammatory disorder, or organ or cell transplant rejection. A new assay for identifying compounds for use in treating and/or preventing those pathological conditions, which comprises measuring the inhibition of PI4KIII? activity, is also disclosed.Type: GrantFiled: September 7, 2012Date of Patent: April 5, 2016Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Jean Herman, Thierry Louat, Qiuya Huang, Bart Vanderhoydonck, Mark Waer, Piet Herdewijn
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Publication number: 20160030447Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HN2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.Type: ApplicationFiled: October 16, 2015Publication date: February 4, 2016Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&DInventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
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Patent number: 9249177Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.Type: GrantFiled: June 27, 2014Date of Patent: February 2, 2016Assignee: K.U. Leuven Research & DevelopmentInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
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Publication number: 20160009750Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.Type: ApplicationFiled: September 28, 2015Publication date: January 14, 2016Inventors: Piet HERDEWIJN, Christophe PANNECOUQUE, Tongfei WU, Erik DE CLERCQ
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Patent number: 9221822Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: GrantFiled: October 20, 2014Date of Patent: December 29, 2015Assignee: Katholieke Universiteit Leuven, K. U. Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Patent number: 9193741Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.Type: GrantFiled: May 20, 2011Date of Patent: November 24, 2015Assignee: Katholieke Universiteit Leuven, K. U. Leuven R&DInventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
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Patent number: 9139572Abstract: The invention concerns stable nicotinamide adenine dinucleotide (NAD/NADH) and nicotinamide adenine dinucleotide phosphate (NADP/NADPH) derivatives, enzyme complexes of these derivatives and their use in biochemical detection methods and reagent matrices.Type: GrantFiled: May 26, 2009Date of Patent: September 22, 2015Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Joachim Hoenes, Carina Horn, Piet Herdewijn
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Publication number: 20150038494Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Patent number: 8901132Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: GrantFiled: March 15, 2010Date of Patent: December 2, 2014Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Publication number: 20140316127Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.Type: ApplicationFiled: June 27, 2014Publication date: October 23, 2014Inventors: Piet HERDEWIJN, Christophe PANNECOUQUE, Tongfei WU, Erik DE CLERCQ