Medivir Ab

Astra Lakemedel Aktiebolag

Karl N Johansson

Goran B Stening

Bjorn G Lindborg

Roelf Datema

Bo F Oberg

Alfons Misiorny

Jan O Noren

Zsuzsanna M Kovacs

Ake J Helgstrand

Zsuzanna M Kovacs

Bo F Berg

Bertil F Eriksson

Rolf Noreen

Daniel Dungan Sohn

Kristina B Gotthammar

ANGke J Helgstrand

Curt-Erik Hagberg

S Christer Sahlberg

Jan-Olof Noren

Sal O Gronowitz

Hans C Malmberg

Bj Orn Lindborg

Ulf Norinder

BjoG Lindborg

Antivirally active compounds of formula (I), wherein R.sup.1 is hydrogen, hydroxy, mercapto or amino; R.sup.2 is hydrogen, hydroxy, fluoro, chloro or amino; R.sup.3 and R.sup.4 are independently selected from (II), (III), amino, hydroxy or an ether or ester residue thereof, or R.sup.3 together with R.sup.4 is (IV), wherein M is hydrogen or a pharmaceutically acceptable counterion; and n is 1 or 2; with the proviso that, when R.sup.2 is amino and R.sup.3 and R.sup.4 are hydroxy, R.sup.1 is not hydroxy and in addition, when n=1, R.sup.1 is not hydrogen, and pharmaceutically acceptable salts thereof; processes for preparation of said compounds, a pharmaceutical composition comprising said compounds, methods for treatments of virus infections as well as use of compounds of formula (I) without the proviso for the manufacture of a medicament for treatment of AIDS. ##STR1##

Derivatives of purine, process for their preparation and a

The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections.

5-substituted pyrimidine nucleosides and nucleotides

The present invention is directed to a method of treating an HIV infection in a host in need of such treatment which comprises administering an effective anti-HIV amount of a compound having the formula ##STR1## wherein: R.sup.1 is hydrogen, hydroxyl;

A 2',3'-deoxy-3'-fluoro-pyrimidine nucleoside having the formula: ##STR1## wherein R.sup.1 is OH or NH.sub.2 ;

1-(3'-fluoro-2',3'-dideoxy-.beta.-D-ribofuranosyl)-5-substituted

Use of a compound of the formula ##STR1## wherein Base is thymine, Cytosine, adenine or guanine, or a physiologically acceptable salt thereof, for therapeutic treatment of hepatitis B virus infections and to a method for such treatment.

Anti-retroviral activity of 2',3'-dideoxy-3'-fluoronucleosides

A compound of the formula ##STR1## wherein the radicals A, X, R.sup.1, R.sup.2 and R.sup.3 are defined as follows:

.alpha. nucleoside compounds and a method for treating HBV using said

Use of a compound of the formula ##STR1## wherein A is .beta.-2'-deoxy-D-ribofuranosyl or .beta.-D-arabinofuranosyl;

Antiviral pharmaceutical composition comprising 5-substituted pyrimidine

A compound of the formula ##STR1## wherein the radicals A, X, R.sup.1, R.sup.2 and R.sup.3 are defined as follows: ##STR2## R.sup.2 : H; or R.sup.2 constitutes together with R.sup.3 with a carbon - carbon bond

Nucleosides and nucleotide analogues, pharmaceutical composition and

Antivirally active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxymethyl;

Derivatives of purine

Antivirally active compounds of the formula ##STR1## wherein A is ##STR2## wherein m is 1 or 2,

Guanine derivative

A pharmaceutical preparation containing as active ingredient a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and each is selected from the group consisting of hydrogen, alkyl groups containing 1-6 carbon atoms; cycloalkyl groups containing 3-6 carbon atoms; cycloalkyl-alkyl groups containing 4-6 carbon atoms; 1-adamantyl; 2-adamantyl, benzyl; and phenyl groups of the formula ##STR2## wherein R.sub.4 and R.sub.5 are the same or different and each is selected from the group consisting of hydrogen, halogen, alkyl having 1, 2, or 3 carbon atoms, alkoxy having 1, 2, or 3 carbon atoms, alkoxycarbonyl having 2-7 carbon atoms and alkylcarbonyl groups having 2-7 carbon atoms; or R.sub.4 and R.sub.5 together form a straight saturated alkylene chain having 3 or 4 carbon atoms and being bound to adjacent positions, i.e. 2,3- or 3,4- in the phenyl ring; and R.sub.3 is selected from the group consisting of hydrogen, alkyl groups containing 1-8 carbon atoms; cycloalkyl groups containing 3-8 carbon atoms; cycloalkyl-alkyl groups containing 4-8 carbon atoms; 1-adamantyl; 2-adamantyl; benzyl; and phenyl groups of the formula ##STR3## wherein R.sub.4 and R.sub.5 have the meaning given above; provided that at least one of the groups R.sub.1, R.sub.2 and R.sub.3 is alkyl, cycloalkyl, or cycloalkyl-alkyl as defined above, or 1-adamantyl, 2-adamantyl, or benzyl; and provided that when R.sub.3 is H, then one of R.sub.1 and R.sub.2 is alkyl, cycloalkyl, or cycloalkyl-alkyl as defined above, or 1-adamantyl, 2-adamantyl, or benzyl and the other of R.sub.1 and R.sub.2 is H; or a physiologically acceptable salt or an optical isomer thereof; novel compounds within formula I, methods for their preparation and their medicinal use.

Phosphonoformic acid esters and pharmaceutical compositions containing

A compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different, and each is selected from the group consisting of hydrogen and phenyl groups of the formula ##STR2## wherein R.sub.4 and R.sub.5 are the same or different and each is selected from the group consisting of hydrogen, halogen, alkyl having 1, 2, or 3 carbon atoms, alkoxy having 1, 2, or 3 carbon atoms, alkoxycarbonyl having 2-7 carbon atoms; and alkylcarbonyl groups having 2-7 carbon atoms; or R.sub.4 and R.sub.5 together form a straight saturated alkylene chain having 3 or 4 carbon atoms and being bound to adjacent positions, i.e. 2,3- or 3,4- in the phenyl ring; provided that one of R.sub.1 and R.sub.2 is a phenyl group of the formula II when R.sub.3 is H; and physiologically acceptable salts and optical isomers thereof; methods for preparation of the compounds, pharmaceutical compositions containing them, and their medicinal use.

Phosphonoformic acid esters

Novel antiviral compounds of the formula ##STR1## wherein each of R.sub.1 and R.sub.2, which are the same or different is hydrogen, hydroxy or fluoro; provided that R.sub.1 or R.sub.2 is hydrogen when R.sub.1 and R.sub.2 are different, and provided that R.sub.1 and R.sub.2 are hydroxy or fluoro when R.sub.1 and R.sub.2 are the same; or a physiologically acceptable salt or an optical isomer thereof, methods for their preparation, pharmaceutical preparations containing the compounds, and methods for the treatment of virus infections and other diseases caused by viruses.

Derivatives of guanine for combating herpes virus infections

A pharmaceutical preparation containing as active ingredient a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and each is selected from the group consisting of hydrogen, alkyl groups containing 1-6 carbon atoms; cycloalkyl groups containing 3-6 carbon atoms; cycloalkyl-alkyl groups containing 4-6 carbon atoms; 1-adamantyl; 2-adamantyl, benzyl; and phenyl groups of the formula ##STR2## wherein R.sub.4 and R.sub.5 are the same or different and each is selected from the group consisting of hydrogen, halogen, alkyl having 1, 2, or 3 carbon atoms, alkoxy having 1, 2, or 3 carbon atoms, alkoxycarbonyl having 2-7 carbon atoms and alkylcarbonyl groups having 2-7 carbon atoms; or R.sub.4 and R.sub.5 together form a straight saturated alkylene chain having 3 or 4 carbon atoms and being bound to adjacent positions, i.e. 2,3- or 3,4- in the phenyl ring;

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Enhorna, Sweden

Karl N Johansson