abstract |
Derivatives of nucleosides and nucleotides, process for their manufacture, and use of said nucleoside derivatives as medicaments and their use in the sequencing of nucleic acids. The invention concerns new derivatives of nucleosides having the general formula (I) in which Ba is an indolyl (A), benzimidazolyl (B), pyrrolopyridinyl (C), imidazopyridinyl (D), triazolopyrimidinyl (E), imidazotriazinyl (F) or imidazopyrimidinyl (G) group substituted by R<1>, R<2> and R<3>, and R<1>, R<2> and R<3>, which may be identical or different are hydrogen, halogen, C1-C7-alkyl, C2-C7-alkenyl, hydroxy, mercapto, C1-C7-alkylthio, C1-C7-alkyloxy, C2-C7 alkenyloxy, Ar-C1-C5-alkyl, Ar-C2-C5-alkenyl, Ar-C1-C5 alkyloxy, Ar-C2-C5 alkenyloxy, aryloxy, nitro, amino-C1-C7-alkyl, C1-C7-alkylamino-C1-C7-alkyl, Di-C1-C7-alkylamino-C1-C7-alkyl, amino groups, a substituted amino group -NHR<4>, or -N(R<4>)2, or an imino group -N=CH-R<4>, and R<4> has the meaning given in the description; R<5>, R<6>, R<7> and R<8> are each hydrogen or one or two of the residues R<5>, R<6>, R<7> and R<8> are a hydroxy, halogen, cyano, azido or a substituted amino-NHR<4> or N(R<4>)2 group, or R<5> and R<7> together can be a further bond between C-2' and C-3'; and Y is hydrogen or a C1-C7 alkyl carbonyl, monophosphate, diphosphate or triphosphate group, where ''aryl'' represents a phenyl or naphthyl group and ''hetaryl'' represents a furanyl, thienyl or pyridyl group, as well as their possible anomers, N<7>-or N<9>-regioisomers (purine nomenclature), tautomers and salts, as well as nucleic acids, which contain compounds of formula (I) as the constituents. |