Patent ID: 6025343
Filing Date: 2000-02-15
Classification: A61P,C07H,Y10S

Abstract:
A nucleoside monophosphate derivative of formula (I) ##STR7## wherein R.sup.1 is selected from the group consisting of a straight-chain or branched, saturated or unsaturated alkyl chain having 1-20 carbon atoms, which is unsubstituted or substituted at least once by halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylmercapto, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkysulfinyl, or C.sub.1 -C.sub.6 alkylsulfonyl groups;R.sup.2 is selected from the group consisting of hydrogen, a straight-chain or branched, saturated or unsaturated alkyl chain having 1-20 carbon atoms, which is unsubstituted or substituted at least once by halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylmercapto, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.1 -C.sub.6 alkylsulfonyl group;R.sup.3 is selected from the group consisting of hydrogen, hydroxy, azido, amino, cyano, and halogen;R.sup.4 is selected from the group consisting of hydroxy, azido, amino, cyano, and halogen;R.sup.5 is selected from the group consisting of hydrogen, hydroxy, azido, amino, cyano, and halogen;X is selected from the group consisting of a valence bond, sulfur, a sulfinyl group and a sulfonyl group;Y is selected from the group consisting of a valence bond, and an oxygen atom;B is a purine or pyrimidine base selected from formulas III (a-d) ##STR8## wherein R.sup.6 is selected from the group consisting of hydrogen; an alkyl chain having 1-6 carbon atoms, which is unsubstituted or substituted by halogen; an alkenyl or alkinyl residue having 2-6 carbon atoms, which is unsubstituted or substituted by halogen, and halogen;R.sup.6' is selected from the group consisting of a hydrogen atom, a benzyl residue and a phenylthio residue;R.sup.7 is selected from the group consisting of hydrogen; an alkyl chain having 1-6 carbon atoms, which is unsubstituted or substituted by halogen; and halogen;R.sup.8 is selected from the group consisting of hydrogen, an alkyl chain having 1-6 carbon atoms, halogen, a hydroxy group and an amino group;R.sup.9 is selected from the group consisting of hydrogen, an amino group and a halogen atom; andR.sup.10 is selected from the group consisting of hydrogen; halogen; mercapto; hydroxy; C.sub.1 -C.sub.6 alkoxy; C.sub.1 -C.sub.6 alkylmercapto; and an amino group which is unsubstituted or substituted at least once by C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; hydroxy-C.sub.2 -C.sub.6 alkyl; C.sub.3 -C.sub.6 cycloalkyl; aryl, hetaryl, aralkyl, or hetarylalkyl groups or a C.sub.2 -C.sub.6 alkenyl which is unsubstituted or substituted by mono- or dialkyl or alkoxy groups; wherein said aryl, hetaryl, aralkyl, or hetarylalkyl groups are unsubstituted or substituted at the aryl or hetaryl residue by at least one mercapto, hydroxy, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.6 alkyl group or halogen;with the proviso that at least one of the residues R.sup.3 or R.sup.5 is hydrogen; their tautomers, their optically active forms and racemic mixtures, and their physiologically acceptable salts of inorganic and organic acids or bases.