Patent · US Expired

Sugar modified nucleosides and their use for synthesis of oligonucleotides

US5712378A · kind A · utility

61Cited by
1References
6Claims
0Family size

Assignee

Inventor

Key dates

Filing dateNov 2, 1995
Grant dateJan 27, 1998
Priority date—
Expiry dateNov 2, 2015

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07H21/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one of the forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.