Nucleoside derivatives and their use as medicaments

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) C07H 19/04 (2006.01) C12Q 1/68 (2006.01) A61K 31/71 (1990.01)

Patent

CA 2064024

2064024 9101325 PCTABS00003 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 R1, R2 and R3, and R1, R2 and R3, 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 -NHR4, or -N(R4)2, or an imino group -N=CH-R4, and R4 has the meaning given in the description; R5, R6, R7 and R8 are each hydrogen or one or two of the residues R5, R6, R7 and R8 are a hydroxy, halogen, cyano, azido or a substituted amino-NHR4 or N(R4)2 group, or R5 and R7 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, N7-or N9-regioisomers (purine nomenclature), tautomers and salts, as well as nucleic acids, which contain compounds of formula (I) as the constituents.

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