Back to results
US 5,486,603 AGranted
Oligonucleotide having enhanced binding affinity
AssigneeGilead Sciences, Inc.
InventorChris A. Buhr
Life of this patent
Estimating the term…
Loading patent…
Loading patent…
AssigneeGilead Sciences, Inc.
InventorChris A. Buhr
Estimating the term…
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 synthesis. The oligonucleotide conjugates of the invention can have a number of uses. For example, the conjugates may be used for diagnostic purposes by detecting a nucleic acid sequence.
An oligonucleotide conjugate comprising an oligonucleotide containing from about 2 to about 30 nucleotides or analog thereof conjugated to a molecule at a terminal 2', 3' or 5' position of the oligonucleotide, which molecule comprises a rigid structure consisting of:
An oligonucleotide conjugate comprising an oligonucleotide containing from about 2 to about 30 nucleotides or analog thereof, which oligonucleotide or analog (a) consists of at least 8 nucleotides;
An oligonucleotide conjugate comprising an oligonucleotide containing from about 2 to about 30 nucleotides or analog thereof conjugated to a molecule at a terminal 2', 3' or 5' position of the oligonucleotide, wherein said molecule has the structure ##STR1## wherein:
Dependencies are inferred from the claim text.