K.u. Leuven Research & Development

Katholieke Universiteit Leuven, Ku Leuven R&d

Roche Diagnostics Operations, Inc.

Katholieke Universiteit Leuven

Imec

Piet Herdewijn

Steven De Jonghe

Christophe Pannecouque

Erik De Clercq

Bart Vanderhoydonck

Jean Herman

Ling-Jie Gao

Dieter Heindl

Thierry Louat

Joachim Hoenes

Carina Horn

Johan Neyts

Mark Jozef Albert Waer

Pieter Leyssen

Miyeon Jang

Mi-Yeon Jang

Yuan Lin

Thierry Andre Michel Louat

Herbert Von Der Eltz

Frank Bergmann

Gustaaf Regina Borghs

Qiuya Huang

Horst Donner

Mark Waer

Michal Sala

Lei Chang

Irene Lagoja

Koen De Keersmaecker

Olga Adelfinskaya

Erik De Clerq

Christophe Pannecoucque

Arthur Van Aerschot

Sona Kovachova

Chao Liu

Shrivinas Dumbre

Robert Snoeck

Dominique Schols

Min Luo

Elisabetta Groaz

Graciela Andrei

Jean Ferdinand Herman

Thierry Andre Louat

Mark Jozef Waer

Thierry André Michel Louat

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.

Prodrugs of nucleoside phosphonates

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.

Antiviral compounds, a process for their preparation, and their use for treating viral infections

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 claimor 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. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovints. 

Antiviral activity of novel bicyclic heterocycles

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.

Phosphonate nucleosides useful as active ingredients in pharmaceutical compositions for the treatment of viral infections, and intermediates for their production

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.

GAK modulators

Compounds that bind to phosphatidylinositol-4-kinase III&#x3b2; (PI4KIII&#x3b2;) and inhibit the binding of PI4KIII&#x3b2; to its substrate and/or inhibit PI4KIII&#x3b2; 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&#x3b2; activity, is also disclosed.

Autoimmune and inflammatory disorder therapy

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. These compounds can be described by the general formula (XIX) 

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 R, R, R, R, R, R, R, R, R, R, and Rare as defined in the claim. 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. 

Thiazolopyrimidine modulators as immunosuppressive agents

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 claimor 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. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral 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. 

Antiviral activity of bicyclic heterocycles

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.

Compounds, methods, complexes, apparatuses and uses relating to stabile forms of NAD/NADH

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. These compounds can be described by general formula (II) 

The present invention is related to the localized/patterned deposition and/or desorption of (bio)molecules using microelectronic structures. Often pre-existing structures needed for proper functioning of the device (e.g. sensors, . . . ) can be used as individually addressable control structures to achieve localized deposition through thermal and/or electrochemical spotting, thereby reducing the need for and simplifying additional processing steps to achieve localized/patterned deposition. If these multi-purpose structures are not available, additional control structures can be implemented, using microelectronic VLSI production technology.

Microelectronic structures for patterned deposition of molecules onto surfaces

The invention is directed to 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, as well as pharmaceutical compositions thereof. These compounds, which can be described by general formula (II), are useful for the treatment of retroviral infection, e.g., HIV (Human Immunodeficiency Virus) infection in a mammal. The invention also features synthetic intermediates for the preparation of phosphonate nucleosides. 

This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.

Phosphate modified nucleosides useful as substrates for polymerases and as antiviral agents

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Wezemaal, Belgium

Piet Herdewijn