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1. 发明授权

EP0778844B1 FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN 失效
标题翻译：功能三联吡啶金属络合物用于生产和寡核苷酸缀合物金属配合物三联吡啶
公开(公告)号：EP0778844B1
公开(公告)日：2002-12-18
申请号：EP95931224.0
申请日：1995-08-30
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： HÄNER, Robert , HALL, Jonathan , HÜSKEN, Dieter , PIELES, Uwe , MOSER, Heinz
IPC分类号： C07H21/00 , C12Q1/68 , C07D213/00
CPC分类号： C07H21/00 , C07D213/00 , C12Q1/6816 , G01N2458/40

2. 发明公开

EP0778845A1 OLIGONUKLEOTIDKONJUGATE, ZUSAMMENSETZUNGEN UND VERFAHREN ZUR SPALTUNG VON RIBONUKLEINSÄUREN 失效
标题翻译：寡核苷酸缀合物，FOR SPLIT核糖核酸组合物和方法
公开(公告)号：EP0778845A1
公开(公告)日：1997-06-18
申请号：EP95931942.0
申请日：1995-08-30
申请人： Novartis AG
发明人： HÜSKEN, Dieter , MOSER, Heinz , HÄNER, Robert , HALL, Jonathan
IPC分类号： C12N15 , A61K31 , A61K41 , A61P31 , A61P35 , C07H21 , C12Q1
CPC分类号： C12Q1/6816 , A61K41/0042
摘要： The invention pertains to an oligonucleotide characterized in that a transesterification or hydrolysis catalyst is bonded to the oligonucleotide, the inner sequence of the oligonucleotide is partially noncomplementary to a naturally occurring target RNA, and the oligonucleotide is composed of deoxyribonucleic acid units, unnatural synthetic nucleotide units or peptide nucleic acids. The oligonucleotides are extremely well suited for splitting a complementary target RNA, the oligonucleotide being released again after the splitting, thus showing a catalytic effect.

3. 发明公开

EP0778844A1 FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN 失效
标题翻译：功能三联吡啶金属络合物用于生产和寡核苷酸缀合物金属配合物三联吡啶
公开(公告)号：EP0778844A1
公开(公告)日：1997-06-18
申请号：EP95931224.0
申请日：1995-08-30
申请人： Novartis AG
发明人： HÄNER, Robert , HALL, Jonathan , HÜSKEN, Dieter , PIELES, Uwe , MOSER, Heinz
IPC分类号： C12N15 , A61K31 , A61P35 , C07D213 , C07D471 , C07F5 , C07F9 , C07H21 , C12Q1
CPC分类号： C07H21/00 , C07D213/00 , C12Q1/6816 , G01N2458/40
摘要： Disclosed are compounds of formula (V), wherein R2 and R7, independently of each other, are H, C1-C4 alkyl, C1-C4 alkoxy, C7-C12 aralkyl, C6-C16 aryl or halogen; R3 and R6, independently of each other, are H, C1-C4 alkyl, C7-C12 aralkyl or C6-C16 aryl; R4 is H, C1-C20 alkyl, C5-C8 cycloalkyl, C6-C12 aryl or C7-C12 aralkyl, the alkyl, cycloalkyl, aralkyl and aryl radicals being unsubstituted or substituted with C1-C4 alkoxy, F, Cl, Br, -CN, C1-C4 alkyl or -NO2; Me is a lanthanide metal or yttrium; Y is an anion of an acid; n stands for 2 or 3 and m is 1, 2 or 3; R9 is a radical of formula (VI) -Xp-A-X'q-A'r-Oligo, and R8 is H, C1-C4 alkyl, C1-C4 alkoxy, C7-C12 aralkyl, C6-C16 aryl, or R9 is H, C1-C4 alkyl, C1-C4 alkoxy, C7-C12 aralkyl, C6-C16 aryl and R8 is a radical of formula (VI); p, q and r, independently of one another, are 0 or 1; X and X', independently of each other, are a radical unsubstituted or substituted by C1-C4 alkoxy, F, Cl, Br, -CN, C1-C4 alkyl or -NO2 substituted radical selected from the group consisting of C1-C20 alkylene, C2-C12 alkenylene, C2-C12 alkinylene, -(CxH2xO)y-, wherein x equals a number from 2 to 6 and y equals a number from 1 to 20, C5-C8 cycloalkylene, C6-C12 arylene and C7-C12 aralkylene; A and A', independently of each other, are -O-, -S-, -S-S-, -NR12-CO-NR12-CO-NR12-, -NR12-CS-NR12-, -NR12-, -NR12-C(O)-O-, -C(O)O-, -C(O)S-, -C(O)NR12-, -C(S)S-, -C(S)O-, -C(S)NR12-, -SO2NR12-, -SO2-, -P(O)(OH)O-, P(S)(SH)S-, -P(S)(SH)O-, -P(S)(OH)O-, -P(O)(SH)S-, -P(O)(OH)S-, -P(O)(SH)O-, -P(O)(OH)-NR12-, -P(S)(SH)-NR12-, -P(S)(OH)-NR12-, -P(O)(SH)-NR12-, -HP(O)O-, -HP(S)S-, -HP(O)NR12- or -HP(S)NR12-, R12 being H or C1-C6 alkyl; and oligo is a natural, modified or synthetic sequence of natural, modified or synthetic deoxynucleosides or peptide nucleic acid units which are bonded via a nucleic base, an internucleotide bridge or a sugar and whose inner region is complementary to a target RNA.

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