K.u. Leuven Research & Development

Ustav Organicke Chemie a Biochemie Akademie Ved Cr, V.v.i.

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

Ustav Experimentalni Mediciny Akademie Ved Cr, V.v.i.

Antonin Holy

Johan Neyts

Erik De Clercq

Marcela Krecmerova

Zdenek Zidek

Zlatko Janeba

Alois Piskala

Graciela Andrei

Robert Snoeck

Petr Jansa

Lieve Naesens

Eva Kmonickova

Dana Hockova

Erik Desire De Clercq

Jan Marie Balzarini

The invention provides pyrimidine compounds of general formula (I), which reduce simultaneously the production of nitric oxide (NO) and prostaglandin E2 (PGE2). They have no negative effect on the viability of cells in concentrations decreasing the production of these factors by up to 50%; they are not cytotoxic. Furthermore, a method of preparation of the pyrimidine compounds of general formula (I), carrying 2-formamido group, a pharmaceutical composition comprising the substituted pyrimidine compounds according to the invention, and the use of these compounds for the treatment of inflammatory and cancer diseases are provided. 

Pyrimidine compounds inhibiting the formation of nitric oxide and prostaglandin E2, method of production thereof and use thereof

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

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Prague, Czechia

Antonin Holy