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N-Acylphosphoramidites and Their Use in Oligonucleotide Synthesis

This technology relates to the synthesis of oligonucleotides, and intermediates useful in its synthesis. The therapeutic application of oligonucleotides is based on the selective formation of hybrids between antisense oligonucleotides and complimentary nucleic acids, such as messenger RNAs. Such hybrids inhibit gene expression by blocking protein translation. Successful inhibition of gene expression requires the antisense oligonucleotide to be nuclease resistant so that it can be successfully transported through biological membranes and can hybridize selectively to a target complementary nucleic acid, thereby actively blocking protein translation.

Serge Beaucage
Andrzej Wilk
Andrzej Grajkowski

Intellectual Property:
U.S. Patent No. 6,965,041 issued 2005-11-15
U.S. Patent No. 6,762,298 issued 2004-07-13
PCT Application No. PCT/US00/04032

Licensing Contact:
Bill Ronnenberg, JD-MIP, MS
FDA Technology Transfer Program
10903 New Hampshire Ave.
Building WO1, Rm 4214
Silver Spring, MD 20993
Email: FDAInventionlicensing@fda.hhs.gov
Phone: 240-402-4561

OTT Reference No: E-1998-003
Updated: August 11, 2015

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