发明公开
EP0778844A1 FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN 失效
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

  • 专利标题: FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN
  • 专利标题(英): Functional terpyridine metal complexes, methods for their preparation and oligonucleotide conjugates with terpyridine metal complexes
  • 专利标题(中): 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
  • 申请号: EP95931224.0
    申请日: 1995-08-30
  • 公开(公告)号: EP0778844A1
    公开(公告)日: 1997-06-18
  • 发明人: HÄNER, RobertHALL, JonathanHÜSKEN, DieterPIELES, UweMOSER, Heinz
  • 申请人: Novartis AG
  • 申请人地址: Schwarzwaldallee 215 4058 Basel CH
  • 专利权人: Novartis AG
  • 当前专利权人: Novartis AG
  • 当前专利权人地址: Schwarzwaldallee 215 4058 Basel CH
  • 优先权: CH19940002693 19940902
  • 国际公布: WO1996007668 19960314
  • 主分类号: C12N15
  • IPC分类号: C12N15 A61K31 A61P35 C07D213 C07D471 C07F5 C07F9 C07H21 C12Q1
FUNKTIONELLE TERPYRIDIN-METALLKOMPLEXE, VERFAHREN ZU DEREN HERSTELLUNG UND OLIGONUKLEOTID-KONJUGATE MIT TERPYRIDIN-METALLKOMPLEXEN
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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