Acyclic nucleoside analogs and oligonucleotide sequences containing them
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United States of America Patent
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Nov 19, 1996
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N/A
app pub date -
May 26, 1995
filing date -
Mar 30, 1993
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Abstract
Compounds of formula I; ##STR1## wherein R.sup.1 is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis; R.sup.2 is hydrogen, nitro, lower alkyl amino, diloweralkyl amino or methyl; R.sup.3 is hydrogen or --P(R.sup.4)OR.sup.5 ; R.sup.4 is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-; R.sup.5 is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl; n is from 0 to 2 X is oxygen, sulfur, or --NR.sup.6 ; R.sup.6 is hydrogen or lower alkyl; Q is chosen from the group consisting of ##STR2## R.sup.7 is lower-alkyl or loweralkyloxy methylene; and R.sup.8 is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyl and its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula I are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.
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