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    • 7. 发明公开
    • FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN
    • 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
    • EP0778844A1
    • 1997-06-18
    • EP95931224.0
    • 1995-08-30
    • Novartis AG
    • HÄNER, RobertHALL, JonathanHÜSKEN, DieterPIELES, UweMOSER, Heinz
    • C12N15A61K31A61P35C07D213C07D471C07F5C07F9C07H21C12Q1
    • C07H21/00C07D213/00C12Q1/6816G01N2458/40
    • 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.