K.u. Leuven Research & Development

Gilead Sciences, Inc.

Other

Toray Industries, Inc.

University College Cardiff Consultants Limited

Rega Foundation

Gerhard Puerstinger

Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic

Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic

Pürstinger, Gerhard

Erik De Clercq

Piet Herdewijn

Tongfei Wu

Christophe Pannecouque

Jan Balzarini

Johan Neyts

Christopher McGuigan

Zeger Debyser

Gerhard Pürstinger

Petr Cherepanov

Masanori Baba

Dominique Schols

Christopher John Yarnold

Marcela Krecmerova

Antonin Holy

Alois Piskala

Rudi Pauwels

Garry Jones

Christophe Pannecoucque

Irene Lagoja

Arthur Van Aerschot

Lieve Naesens

Robert Snoeck

Graciela Andrei

Peter Cherepanov

Marcela Krecmerová

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 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 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 relates to imidazo[4,5-c]pyridine compounds and pharmaceutical compositions for the treatment or prevention of viral infections, wherein the imidazo[4,5-c]pyridine compounds have the formula: 

Viral inhibitors

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. 

The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

Azacytosine derivatives useful as antiviral agents

The present invention provides nucleic acid molecules which include a region specifically interacting with the nucleic acid encoding the LEDGF/P75 protein or the nucleic acid encoding a fragment of a LEDGF/P75 protein and methods and uses of such nucleic acid molecules.

Integrase cofactor

The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine derivative having the general formula (Z): (formula). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections. 

The present invention provides integrase interacting proteins including cofactors which promote strand transfer activity of viral integrase, more particularly HIV integrase, and methods and uses relating thereto. The present invention also relates to methods of identifying molecules interacting with integrase interacting protein and their use as an antiviral.

An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, Ris selected from hydrogen, methyl or ethyl, Ris selected from hydrogen, SH or &#x2014;SRwherein Ris methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl. This invention further relates to the use of compounds of formula (I) as agents having biological activity, especially against viral infections.

HIV inhibiting N-aminoimidazole derivatives

Compounds of the general formula (I)are described wherein R, R', R&#x2033;, Q, T, T&#x2032;, T&#x2033;, T&#x2033;&#x2032;, W, X, and Z are as defined in the specification. Compounds according to the invention preferably display potent anti-viral activity against, for example, cytomegalo virus.

Anti-viral pyrimidine nucleoside analogues

A compound having formula (I), wherein R is selected from the group comprising C to C alkyl, C to C cycloalkyl, halogens, aryl and alkylaryl; R&prime; is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, alkyl; R&Prime; is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, alkyloxy, aryloxy and aryl; Q is selected from the group comprising O, S and CY , where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH ) where n is 1 to 10, and CY where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N alkyl; U&Prime; is H and U&prime; is selected from H and CH T, or U&prime; and U&Prime; are joined so as to form a ring moiety including Q wherein U&prime;-U&Prime; together is respectively selected from the group comprising &mdash;CTH&mdash;CT&prime;T&Prime;&mdash; and &mdash;CT&boxH;CT&mdash; and &mdash;CT&prime;&boxH;CT&prime;&mdash;, so as to provide ring moieties selected from the group comprising formula (II) and (III) wherein T is selected from the group comprising OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH and N ; T&prime; is selected from the group comprising H and halogens and where more than one T&prime; is present they may be the same or different; T&Prime; is selected from the group comprising H and halogens, and W is selected from the group comprising H, a phosphate group and a pharmacologically acceptable salt, derivative or prodrug thereof shows potent anti-viral activity against, for example, varicella zoster virus and cytomegalovirus.

An antiviral agent against viruses causative of AIDS, containing fuchsinic acid as an active ingredient. The antiviral agents provided by the present invention inhibit cellular infection by AIDS-causing virus and progress of the infection into ARC and are effective in the treatment of AIDS.

Growing community of inventors

Lovenjoel, Belgium

Erik De Clercq