Isis Pharmaceuticals, Inc.

Glen Research Corporation

Harri Lonnberg

Muthiah Manoharan

Harri Salo

Pasi Virta

Andrei P Guzaev

Alex Azhayev

The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include an aminooxy linkage. These oligomers are useful for diagnostic, therapeutic and investigative purposes.

Aminooxy functionalized oligomers, oligomer arrays and methods of using them

Aminooxy functionalized oligomers

Phosphoramidite building blocks according to the following formula 1 are used for phosphorylating oligonucleotides, preferably at the 5'- or 3'-terminus. The building blocks include phosphoramidite compounds according to formula 1: ##STR1## wherein DMTr is a 4,4'-dimethoxytrityl group; R.sub.1 is an electron withdrawing group; R.sub.2 is an electron withdrawing group which may be the same or different from the R.sub.1 group; R.sub.3 is an alkyl group; and R.sub.4 is an alkyl group which may be the same or different from the R.sub.3 group. Preferred electron withdrawing groups include --CO.sub.2 Et groups, --CO.sub.2 Me groups, --CN groups, --CON(Me).sub.2 groups, and --CONHMe groups, wherein Et represents an ethyl group and Me represents a methyl group. One preferred alkyl group is an isopropyl group.

Chemical phosphorylation of oligonucleotides and reactants used therefor

Growing community of inventors

Turku, Finland

Harri Lonnberg