Ceskoslovenska Akademie Ved

Institute of Organic Chemistry and Biochemistry of the Academy of

Rega Stichting, V.z.w.

Stichting Rega Vzw

Rega Institut

Ivan Rosenberg

Antonin Holy

Erik D De Clercq

Karel Slama

This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyolic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

9-(2-phosphonylmethoxyethyl) guanine

This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases and their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

N-phosphonylmethoxyalkyl derivatives of pyrimdine and purine bases and a

This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases andd their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

N-phosphonylmethoxyalkyl derivatives of pyrimidine and purine bases and

The invention relates to 9-(phosphonylmethoxyalkyl)adenines of the general formula I ##STR1## wherein R.sup.1 is a hydrogen atom, and alkyl group containing one to three carbon atoms, or a hydroxymethyl group, R.sup.2 is a methylene, ethylene, propylene, ethylidene, methoxyethylene, benzyloxyethylene, tetrahydropyran-2-yloxyethylene, (1-ethoxyethoxy)ethylene or 1,2-O-isopropylidene-1,2-dihydroxypropylene group the method of their preparation and utilization. Compounds of the general formula I exhibit biological effects (e.g. antiviral) or can be converted into compounds with such effects.

9-(phosponylmethoxyalkyl) adenines, the method of preparation and

The (S) and (RS) forms of certain phosphonylmethoxyalkyl adenines and their salts have an antiviral effect against several DNA viruses and can be used for the treatment of virus diseases in human and veterinary medicine.

Therapeutical application of phosphonylmethoxyalkyl adenines

This invention relates to isomeric O-phosphonylmethyl derivatives of the formula I ##STR1## wherein R.sup.5 designates an adenin-9-yl moiety, R.sup.4 are alternately a hydrogen atom and a --CH.sub.2 P(O)(OH).sub.2 group, and the configuration at the carbon atom in the position 2 is S, R or RS. The compounds according to the invention are biologically active as inhibitors of metabolic processes and in organism they are stable towards enzymes, cleaving phosphomonoester bonds. The said compounds exhibit also chemosterilizing action on insects.

Growing community of inventors

Prague, Czechia

Ivan Rosenberg