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N-2 substituted purines in oligonucleotides

  • US 5,808,027 A
  • Filed: 12/10/1996
  • Issued: 09/15/1998
  • Est. Priority Date: 01/11/1990
  • Status: Expired due to Fees
First Claim
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1. An oligonucleotide for affecting RNase H cleavage of RNA comprising:

  • a first oligonucleotide region and a second nucleotide region;

    said second region including a plurality of consecutive phosphorothiate linked nucleotides having a 2'"'"'-deoxy-erythro-pentofuranosyl sugar moiety;

    said first region including at least one nucleotide of formula;

    ##STR7## wherein G is CH or N;

    X is NH2 or OH;

    Y is RQ or NHRQ, wherein R is a hydrocarbyl group having from 2 to about 20 carbon atoms; and

    Q is H, NH2, a polyalkylamine, a hydrazine, a hydroxylamine, a semicarbazide, a thiosemicarbazide, a hydrazone, a hydrazide, an imidazole, an imidazole amide, an alkyl imidazole, an alkylimidazole, a tetrazole, a triazole, a pyrrolidine, a piperidine, a piperazine, a morpholine, a thiol, an aldehyde, a ketone, an alcohol, an alkoxy group, or a halogen; and

    Z is ribose, 2'"'"'-O-alkyl ribose or deoxyribose.

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