US Patent No: 5,212,295

Number of patents in Portfolio can not be more than 2000

Monomers for preparation of oligonucleotides having chiral phosphorus linkages

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Abstract

Sequence-specific oligonucleotides are provided having substantially pure chiral Sp phosphorothioate, chiral Rp phosphorothioate, chiral Sp alkylphosphonate, chiral Rp alkylphosphonate, chiral Sp phosphoamidate, chiral Rp phosphoamidate, chiral Sp phosphotriester, and chiral Rp phosphotriester linkages. The novel oligonucleotides are prepared via a stereospecific SN.sub.2 nucleophilic attack of a phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate anion on the 3' position of a xylonucleotide. The reaction proceeds via inversion at the 3' position of the xylo reactant species, resulting in the incorporation of phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate linked ribofuranosyl sugar moieties into the oligonucleotide.

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First Claim

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Patent Owner(s)

Patent OwnerAddressTotal Patents
ISIS PHARMACEUTICALS, INC.CARLSBAD, CA963

International Classification(s)

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  • [Patents Count]

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cook, Phillip D Fallbrook, CA 46 2840

Cited Art

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UNIVERSITY PATENTS, INC. (1)
4,500,707 Nucleosides useful in the preparation of polynucleotides 302 1982

Patent Citation Ranking

Forward Cites

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5,859,221 2'-modified oligonucleotides 70 1995
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6,762,169 Ligand-conjugated oligomeric compounds 6 2000
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6,525,031 Targeted Oligonucleotide conjugates 12 2001
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7,056,896 Carbohydrate or 2'-modified oligonucleotides having alternating internucleoside linkages 1 2001
7,119,184 Oligonucleotides having A-DNA form and B-DNA form conformational geometry 0 2001
6,861,514 Nucleosidic and non-nucleosidic folate conjugates 2 2001
6,610,663 Compositions and methods for modulating RNA 1 2001
7,138,517 Sugar modified oligonucleotides 8 2001
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6,537,973 Oligonucleotide inhibition of protein kinase C 4 2001
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6,699,979 Oligonucleotides having chiral phosphorus linkages 1 2002
6,849,723 Oligonucleotide analogs having modified dimers 0 2002
6,858,715 Process for the synthesis of oligomeric compounds 4 2002
6,660,720 Targeted oligonucleotide conjugates 0 2002
6,677,471 Intermediates for the synthesis of oligonucleotide analogues 0 2002
6,974,865 C3′ -methylene hydrogen phosphonate oligomers and related compounds 0 2002
6,780,989 Diribonucleoside Phosphoramidites 0 2003
7,002,006 Protection of nucleosides 0 2003
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