Patent · US Expired

Oligonucleotide having enhanced binding affinity

US5486603A · kind A · utility

250Cited by
1References
32Claims
0Family size

Assignee

Inventor

Key dates

Filing dateJun 22, 1992
Grant dateJan 23, 1996
Priority date
Expiry dateJun 22, 2012

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07J51/00
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner. The invention also relates to a conjugate comprising a steroid or substituted derivative thereof containing, or attached directly or through a carbon atom to, an amine, which steroid or substituted derivative is conjugated to at least one hydrogen-phosphonate and a cation; such a conjugate may be used as an intermediate in synt…

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