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Generated: December 14, 2017

DrugPatentWatch Database Preview

Claims for Patent: 6,166,197

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Claims for Patent: 6,166,197

Title: Oligomeric compounds having pyrimidine nucleotide (S) with 2'and 5 substitutions
Abstract:Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2' and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position.
Inventor(s): Cook; Phillip Dan (San Marcos, CA), Sanghvi; Yogesh S. (San Marcos, CA), Sprankle; Kelly G. (Vista, CA), Ross; Bruce S. (Carlsbad, CA), Griffey; Rich H. (Vista, CA)
Assignee: ISIS Pharmaceuticals, Inc. (Carlsbad, CA)
Application Number:08/398,901
Patent Claims: 1. An oligomeric compound comprising at least one monomeric sub-unit of structure I: ##STR4## wherein: X is amino;

R is methyl;

L is oxygen;

Z is --O--CH.sub.3 ; and

one of Q.sub.1 and Q.sub.2 is attached via a phosphorothioate linking moiety to a nucleotide, oligonucleotide, nucleoside, or oligonucleoside and the other of said Q.sub.1 and Q.sub.2, is a hydroxyl, a protected hydroxyl, an activated solid support, a nucleotide, an oligonucleotide, a nucleoside, an oligonucleoside, an oligo-nucleotide/nucleoside, an activated phosphate, a phosphate, an activated phosphite, or a phosphite;

provided that said linking moiety is not a sulfamate group.

2. An oligomeric compound comprising at least one monomeric sub-unit of structure I: ##STR5## wherein: X is amino;

R is methyl;

L is oxygen;

Z is O--R.sub.1 X.sub.1, where R.sub.1 is C.sub.1 -C.sub.6 alkyl, and X.sub.1 is H; and

one of Q.sub.1 and Q.sub.2 is attached via a phosphorothioate linking moiety to a nucleotide, oligonucleotide, nucleoside, or oligonucleoside and the other of said Q.sub.1 and Q.sub.2, is a hydroxyl, a protected hydroxyl, an activated solid support, a nucleotide, an oligonucleotide, a nucleoside, an oligonucleoside, an oligo-nucleotide/nucleoside, an activated phosphate, a phosphate, an activated phosphite, or a phosphite;

provided that said linking moiety is not a sulfamate group.

3. An oligomeric compound comprising at least one monomeric sub-unit of structure I: ##STR6## wherein: X is amino;

R is methyl;

L is oxygen;

Z is O--R.sub.1 X.sub.1, where R.sub.1 is substituted C.sub.1 -C.sub.6 alkyl, and X.sub.1 is H; and

one of Q.sub.1 and Q.sub.2 is attached via a phosphorothioate linking moiety to a nucleotide, oligonucleotide, nucleoside, or oligonucleoside and the other of said Q.sub.1 and Q.sub.2, is a hydroxyl, a protected hydroxyl, an activated solid support, a nucleotide, an oligonucleotide, a nucleoside, an oligonucleoside, an oligonucleotide/nucleoside, an activated phosphate, a phosphate, an activated phosphite, or a phosphite;

provided that said linking moiety is not a sulfamate group.
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