2-aminopurine derivatives

Details 2-aminopurine derivatives 2-aminopurine derivatives

C - Chemistry, Metallurgy

07

H

C07H 19/173 (2006.01) A61K 31/7076 (2006.01) A61K 31/7088 (2006.01) A61P 43/00 (2006.01) C07H 19/16 (2006.01) C07H 19/20 (2006.01) C07H 21/00 (2006.01) C07H 21/04 (2006.01)

Patent

CA 2390233

2-Aminopurine derivatives represented by general formula (1); and compositions for controlling gene expression, characterized by containing said derivatives; wherein R is hydrogen or acyl; X is a phosphoramidite group or an oligonucleotide; Y is dimethyltrityl or an oligonucleotide; and Z1, Z2, Z3, Z4 and Z5 are each independently hydrogen, hydroxyl, amino, lower alkyl, alkoxy, carboxyl, or sulfo, with the proviso that cases wherein all of Z1, Z2, Z3, Z4 and Z5 are hydrogen are excepted]. Oligonucleotides obtained by the introduction of the 2-aminopurine derivatives exhibit a high reactivity for a target nucleic acid and permit crosslinking of remarkably high base-sequence specificity.

L'invention concerne des dérivés de 2-aminopurine représentées par la formule générale (1), et des compositions contenant lesdits dérivés et pouvant réguler l'expression génique. Dans ladite formule, R est hydrogène ou acyle; X est un groupe phosphoramidite ou un oligonucléotide; et Z?1¿, Z?2¿, Z?3¿, Z?4¿ et Z?5¿ sont individuellement et indépendamment hydrogène, hydroxyle, amino, alkyle inférieur, alcoxy, carboxyle ou sulfo, à l'exception des cas où Z?1¿, Z?2¿, Z?3¿, Z?4¿ et Z?5¿ sont hydrogène. Des oligonucléotides obtenus par introduction des dérivés de 2-aminopurine démontrent une grande réactivité pour un acide nucléique cible et permettent de réaliser une réticulation dont la spécificité de séquence des bases est remarquablement élevée.

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