- 专利标题: Cationic oligonucleotides, automated methods for preparing same and their uses
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申请号: US14745871申请日: 2015-06-22
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公开(公告)号: US09676798B2公开(公告)日: 2017-06-13
- 发明人: Jean-Paul Behr , Mitsuharu Kotera , Benedicte Pons , Emilie Voirin , Jean-Serge Remy
- 申请人: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE STRASBOURG , POLYPLUS TRANSFECTION
- 申请人地址: FR Paris FR Strasbourg FR Illkirch
- 专利权人: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS),UNIVERSITE DE STRASBOURG,POLYPLUS TRANSFECTION
- 当前专利权人: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS),UNIVERSITE DE STRASBOURG,POLYPLUS TRANSFECTION
- 当前专利权人地址: FR Paris FR Strasbourg FR Illkirch
- 代理机构: Nixon & Vanderhye P.C.
- 主分类号: C07H21/00
- IPC分类号: C07H21/00 ; C07F9/22 ; A61K47/48 ; A61K48/00 ; C12N15/88
摘要:
The invention relates to oligonucleotide-oligocation molecules AiBjH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein .Ai is an i-mer oligonucleotide residue, with i=5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical modifications or substitutions such as phosphorothioate, 2′-fluoro, 2′-O-alkyl, or a marker group such as a fluorescent agent, .Bj is a j-mer organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising .—HPO3—R1—(X—R2n)n1—X—R3—O—, where R1, R2n and R3, identical or different, are lower alkylene, X is NH or NC(NH2)2, n varies from 1 to 5 and n1=2 to 20, .—HPO3—R4—CH(R5X1)—R6—O—, where R4 is lower alkylene, R5 and R6, identical or different, are lower alkylene and X1 is putrescine, spermidine or spermine residue, .—HPO3—R7-(aa)n2-R8—O—, where R7 is lower alkylene and R8 is lower alkylene, serine, a natural aminoalcohol, (aa)n2 is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, -Histidine, Diaminopropionic acid and n2=2 to 20.
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