EP0081099A2
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EP
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Capped oligonucleotide anti-viral agents
Assignee: Memorial Sloan Kettering Cancer Center
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Filing: 1982-11-13
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Granted: —
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Expires: 2002-11-13
Abstract
Abstract Capped oligonucleotide anti-viral agent comprising: a cap having the formula m 7 G (5')-ppp (5') Nm, where N=A or G and m=2' O-methyl ribose, a linkage group X, attached to said cap, where X=A, G, C or U, a polymeric chain attached to said linkage group comprised of nucleotides that inhibit influenza virus RNA transcription when in polymer form, said polymeric chain being modified to prevent it from acting as a primer to stimulate transcription.
Inventors
- 👤 Robert M. Krug
- 👤 Stephen J. Plotch
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 14:49
CPC Classifications
C; C07; C07H; C07H21/00; A; A61; A61P; A61P31/00; A61P31/12; A61P31/14; A61P31/16
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
85 words
Capped oligonucleotide comprising: a cap having the formula m 7 G (5') ppp (5') Nm, where N = A or G and m = 2' 0 -methyl ribose a linkage group X, where X = A, G, C or U attached to said cap a polymeric chain attached to said linkage group comprised of nucleotides that inhibit influenza virus RNA transcription when in polymer form, said polymeric chain being modified to prevent it, when attached to the cap from acting as a primerto stimulate transcription.
Claim 2
Dependent Claim
85 words
Capped oligonucleotide comprising: a cap having the formula m 7 G (5') ppp (5') Nm, where N = A or G and m = 2' 0 -methyl ribose a linkage group X, where X = A, G, C or U attached to said cap a polymeric chain attached to said linkage group comprised of nucleotides that inhibit influenza virus RNA transcription when in polymer form, said polymeric chain being modified to prevent it, when attached to the cap from acting as a primerto stimulate transcription.
Claim 3
Dependent Claim
25 words
Oligonucleotide of claim 1 wherein said polymeric chain is modified to prevent cleavage at the 10 th to 13 th nucleotide by the virion-associated endonuclease.
Claim 4
Dependent Claim
21 words
Oligonucleotide of claim 1 wherein said polymeric chain is modified so that, if cleaved, the cleavage fragments cannot act as primers.
Claim 5
Dependent Claim
59 words
Oligonucleotide of claim 1 having a formula m 7 G (5') ppp (5') NmpX (B) n where n > 11 and B = S 4 U; S 4 cyanoethyl-U; S 4 -ethylenimine-U; S 4 - (N- ethyl-maleimide) -U; AG 1:1 (Kethox y lated); AG 1:1 (glyoxylated); AG 1:1 (n-7 methyl G) ; and AG 1:1 (n-1 methyl A) and
Claim 6
Dependent Claim
13 words
Oligonucleotide of claim 1 wherein said nucleotide is modified at the sugar moiety.
Claim 7
Dependent Claim
20 words
Oligonucleotide of claim 5 wherein said sugar modification consists of 2'-O-methyl; 2'H; or the sugar is arabinose instead of ribose.
Claim 8
Dependent Claim
23 words
Oligonucleotide of claim 1 further comprising an internucleotide linkage of 2' - 5' phosphate in place of 3' - 5' phosphate normally present.
Claim 9
Dependent Claim
74 words
Oligonucleotide of claim 1 wherein said polymeric chain attached to said linkage group is comprised of 5 - 7 nucleotides to which is attached at its 3' terminus either a deoxymononucleotide or a 3'-O-methylmononucleotide, said capped oligonucleotide acting as a specific inhibitor for the influenza virion transcriptase while at the same time being unable to act as primer by virtue of its 3 terminal nucleotide and its short length of less than 10 oligoribonucleotides.
Claim 10
Dependent Claim
75 words
Oligonucleotide of claim 8 having the formula m 7 G (5') ppp ( 5 ') NmpX (B) n M where B = S 4 U; S 4- ethylenimine-U; S 4- (N-ethylmaleimide)- U: AG 1:1 (kethoxylated); AG 1:1 (glyoxylated ) ; AG (n-7 methyl G) AG 1:1 (n-1 methyl A) ; and AG 1:1 . n = 5, 6 or 7 M = p dA p , pdGp, pdCp pdUp or pA(3'O-methyl), pG(3'O-methyl), pC(3'O-methyl), pU(3'0-methyl). -
Claim 11
Dependent Claim
13 words
Oligonucleotide of claim 8 wherein said nucleotide is modified at the sugar moiety.
Claim 12
Dependent Claim
20 words
Oligonucleotide of claim 10 wherein said sugar modification consists of 2'-O-methyl; 2'H; or the sugar is arabinose instead of ribose.
Claim 13
Dependent Claim
19 words
Oligonucleotide of claim 8 further comprising an internucleotide linkage of 2'-5' phosphate in place of 3'-5' phosphate normally present.
Claim 14
Dependent Claim
17 words
Antiviral agent comprising an effective amount of the oligonucleotide of claim 1 in a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
21 words
Method of inhibiting influenza virion transcriptase comprising applying an effective amount of the oligonucleotide of claim 1 to influenza virus-infected cells.
References Cited (Backward Citations)
No citation records indexed.
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