发明授权
- 专利标题: Carbohydrate conjugates as delivery agents for oligonucleotides
- 专利标题(中): 碳水化合物缀合物作为寡核苷酸的递送剂
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申请号: US12328528申请日: 2008-12-04
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公开(公告)号: US08106022B2公开(公告)日: 2012-01-31
- 发明人: Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
- 申请人: Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Martin Maier
- 申请人地址: US MA Cambridge
- 专利权人: Alnylam Pharmaceuticals, Inc.
- 当前专利权人: Alnylam Pharmaceuticals, Inc.
- 当前专利权人地址: US MA Cambridge
- 代理机构: LeClairRyan
- 代理商 Jeffrey N. Townes
- 主分类号: A01N43/04
- IPC分类号: A01N43/04 ; A61K31/70
摘要:
The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z′)(Z″)O-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.
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