Oligonucleotide N3'.fwdarw.P5' phosphoramidates
First Claim
1. An oligodeoxyribonucleotide comprising a non-homopolymeric defined sequence of nucleoside subunits joined by intersubunit linkages wherein at least fifty percent of such intersubunit linkages are N3'"'"'→
- P5'"'"' phosphoramidate linkages, and at least two of said N3'"'"'→
P5'"'"' phosphoramidate linkages are contiguous, wherein said defined sequence has a sequence complementary to mRNA from a gene selected from the group consisting of c-myc, c-myb, c-fos, c-kit, ras and BCR/ABL.
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Accused Products
Abstract
Modified oligonucleotides 3'"'"'-NHP(O)(O-)O-5'"'"' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.
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12 Claims
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1. An oligodeoxyribonucleotide comprising a non-homopolymeric defined sequence of nucleoside subunits joined by intersubunit linkages wherein at least fifty percent of such intersubunit linkages are N3'"'"'→
- P5'"'"' phosphoramidate linkages, and at least two of said N3'"'"'→
P5'"'"' phosphoramidate linkages are contiguous, wherein said defined sequence has a sequence complementary to mRNA from a gene selected from the group consisting of c-myc, c-myb, c-fos, c-kit, ras and BCR/ABL. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- P5'"'"' phosphoramidate linkages, and at least two of said N3'"'"'→
Specification