Oligonucleotide N3'.fwdarw.P5' phosphoramidates
US5965720A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jan 10, 1997 |
| Grant date | Oct 12, 1999 |
| Priority date | — |
| Expiry date | Jan 10, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H21/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.