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US Patent 6846921 Chimeric antisense oligonucleotides and cell transfecting formulations thereof

Patent 6846921 was granted and assigned to Chiron Corporation on January, 2005 by the United States Patent and Trademark Office.

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Patent
Patent
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Patent attributes

Patent Applicant
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Current Assignee
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Chiron Corporation
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Patent Jurisdiction
United States Patent and Trademark Office
United States Patent and Trademark Office
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Patent Number
68469211
Patent Inventor Names
Christoph J. Reinhard1
Michael A. Innis1
Ronald N. Zuckermann1
Date of Patent
January 25, 2005
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Patent Application Number
098265191
Date Filed
April 3, 2001
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Patent Citations Received
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US Patent 11873490 Antisense oligomers for treatment of conditions and diseases
2
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US Patent 11891605 Reducing intron retention
3
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US Patent 12060558 Methods and compositions for treatment of cholesteryl ester storage disease
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Patent Primary Examiner
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Janet L. Epps-Ford
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Patent abstract

Chimeric oligonucleotide of the formula 5′-W—X1—Y—X2—Z-3′, where W represents a 5′-O-alkyl nucleotide, each of X1 and X2 represents a block of seven to twelve phosphodiester-linked 2′-O-alkyl ribonucleotides, Y represents a block of five to twelve phosphorothioate-linked deoxyribonucleotides, and Z represents a blocking group effective to block nuclease activity at the 3′ end of the oligonucleotide, are described. These compounds exhibit high resistance to endo- and exonucleases, high sequence specificity, and the ability to activate RNAse H, as evidenced by efficient and long-lasting suppression of target mRNA. The oligonucleotides are preferably transfected into cells in formulations containing a lipid-peptoid conjugate carrier molecule of the formulaL-linker-[N(CH2CH2NH2)CH2(C═O)—N(CH2CH2R)CH2(C═O)—N(CH2CH2R)CH2(C═O)]3—NH2,where L is a lipid moiety, including a steroid, and each group R is independently selected from alkyl, aminoalkyl, and aralkyl.

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