Invention Grant
US07674778B2 Oligonucleotides comprising a conjugate group linked through a C5-modified pyrimidine
有权
包含通过C5-修饰的嘧啶连接的共轭基团的寡核苷酸
- Patent Title: Oligonucleotides comprising a conjugate group linked through a C5-modified pyrimidine
- Patent Title (中): 包含通过C5-修饰的嘧啶连接的共轭基团的寡核苷酸
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Application No.: US11119533Application Date: 2005-04-29
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Publication No.: US07674778B2Publication Date: 2010-03-09
- Inventor: Muthiah Manoharan , Kallanthottathil G. Rajeev
- Applicant: Muthiah Manoharan , Kallanthottathil G. Rajeev
- Applicant Address: US MA Cambridge
- Assignee: Alnylam Pharmaceuticals
- Current Assignee: Alnylam Pharmaceuticals
- Current Assignee Address: US MA Cambridge
- Agency: Nixon Peabody LLP
- Agent Jeffrey N. Townes
- Main IPC: A61K31/70
- IPC: A61K31/70 ; C07H21/04

Abstract:
One aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one ligand. In certain embodiments, a ligand is bound to only one of the two oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, both of the oligonucleotide strands of the double-stranded oligonucleotide independently comprise a bound ligand. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. In certain embodiments, a phosphate linkage in one or both of the strands of the oligonucleotide has been replaced with a phosphorothioate or phosphorodithioate linkage. In a preferred embodiment, the ligand is cholesterol or 5β-cholanic acid. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one ligand. In certain embodiments, the oligonucleotide comprises at least one modified sugar moiety. In certain embodiments, a phosphate linkage of the oligonucleotide has been replaced with a phosphorothioate or phosphorodithioate linkage. In a preferred embodiment, the ligand is cholesterol or 5β-cholanic acid. The ligand improves the pharmacokinetic properties of the oligonucleotide.
Public/Granted literature
- US20050288244A1 Oligonucleotides comprising a C5-modified pyrimidine Public/Granted day:2005-12-29
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