主权项 |
1. A compound of formula I: wherein
Nucleoside is a natural nucleoside or a nucleoside analogue;R1 has the general formula II: wherein
R3 is selected from the group consisting of aryl, heteroaryl, C1-C10 alkyl, C3-C8-cycloalkyl, C3-C8cycloalkyl-alkyl, aryl(C1-C6)alkyl, C2-C10 alkenyl, C2-C10 alkynyl, hydroxyl C1-C10 alkyl, halo C1-C10 alkyl, and alkoxyalkyl;R4 is selected from the group consisting of X—COR5, and X—O—R6, wherein X is aryl, heteroaryl, C1-C10 alkyl, or C3-C8-cycloalkyl, and wherein said aryl, heteroaryl, C1-C10 alkyl, and C3-C8-cycloalkyl optionally contains one or more functions, atoms or radicals independently selected from the group consisting of halogen, carbonyl, thiocarbonyl, hydroxyl, thiol, ether, thio-ether, acetal, thio-acetal, amino, imino, oximino, alkyloximino, aminoacid, cyano, acylamino, thioacylamino, carbamoyl, thiocarbamoyl, ureido, thio-ureido, carboxylic acid ester or halide or anhydride or amide, thiocarboxylic acid or ester or thioester or halide or anhydride or amide, nitro, thio C1-7 alkyl, thio C3-10 cycloalkyl, hydroxylamino, mercaptoamino, alkyl-amino, cycloalkylamino, alkenylamino, cycloalkenylamino, alkynylamino, arylamino, arylalkylamino, hydroxyalkylamino, mercaptoalkylamino, heterocyclic-substituted alkylamino, hetero-cyclic amino, heterocyclic-substituted arylamino, hydrazine, alkylhydrazino, phenylhydrazino, sulfonyl, sulfinyl and sulfonamido; R5 is selected from the group consisting of C1-C7 alkoxy, aryloxy, C3-C10 cycloalkoxy, and arylalkyloxy; R6 is selected from the group consisting of acyl, alkoxyalkyl, C3-C10 cycloalkyl-alkyl, C3-10 cycloalkyl, heterocyclic-substituted alkyl, acyl-substituted alkyl, carboxylato-substituted alkyl, heterocyclic, halo C1-C7 alkyl, C2-C7 alkenyl, C2-C7 alkynyl, arylalkenyl, aryloxyalkyl, arylalkyl, and aryl; wherein the aryl moiety of each of said arylalkenyl, aryloxyalkyl, arylalkyl and aryl radicals is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C7 alkyl, C2-C7 alkenyl, C2-C7 alkynyl, halo C1-C7 alkyl, nitro, hydroxyl, sulfhydryl, amino, C1-C7 alkoxy, C3-C10 cycloalkoxy, thio C1-C7 alkyl, thio C3-C10 cycloalkyl, thioaryl, cyano, carboxylic acid or esters or amides thereof, alkylamino, cycloalkylamino, alkenylamino, cyclo-alkenylamino, alkynylamino, arylamino, and arylalkylamino;
R2 is Y—Ar wherein Y is O; and Ar is a monocyclic aryl moiety or a fused bicyclic aryl moiety, either of which aryl moieties is carbocyclic or heterocyclic and is optionally substituted with a halogen, C1-C6 alkyl, C1-C6 alkoxy; wherein when R3 is C1-C10 alkyl and R5 comprises an alkoxy moiety, R5 comprises at least 3 carbon atoms; and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and/or prodrugs thereof. |