Boronic acid conjugates of oligonucleotide analogues
US-2015080340-A1 · Mar 19, 2015 · US
US9249243B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9249243-B2 |
| Application number | US-201313963919-A |
| Country | US |
| Kind code | B2 |
| Filing date | Aug 9, 2013 |
| Priority date | Jul 13, 2005 |
| Publication date | Feb 2, 2016 |
| Grant date | Feb 2, 2016 |
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A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3′ or 5′ end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.
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It is claimed: 1. A compound having the following formula (I): or a salt thereof, wherein: R 1 is H or trityl; R 2 is H or and R 3 is H or a linkage to a solid support. 2. The compound of claim 1 , wherein the compound has the fo…
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