Patent Number: 6,169,170

Title: Oligonucleotide N3'.fwdarw.N5'Phosphoramidate Duplexes

Abstract: Modified oligonucleotides 3'-NHP(O)(O.sup.-)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.

Inventors: Gryaznov; Sergei M. (San Mateo, CA), Schultz; Ronald G. (Urbana, MO), Chen; Jer-kang (Palo Alto, CA)

Assignee: Lynx Therapeutics, Inc.

International Classification: C07H 21/00 (20060101); C07H 19/16 (20060101); C07H 19/00 (20060101); C07H 19/06 (20060101); C07H 021/00 (); C12Q 001/68 ()

Expiration Date: 01/02/2018