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    • 3. 发明授权
    • 2'-O-alkylnucleotides as well as polymers which contain such nucleotides
    • 2'-O-烷基核苷酸以及含有这些核苷酸的聚合物
    • US5658731A
    • 1997-08-19
    • US376697
    • 1995-01-23
    • Brian SproatAngus Lamond
    • Brian SproatAngus Lamond
    • C07H19/06C07H19/10C07H19/16C07H19/20C07H21/00C12Q1/68
    • C07H19/06C07H19/10C07H19/16C07H19/20C07H21/00
    • Oligonucleotides having the general formula, ##STR1## in which B denotes an arbitrary nucleobase,A equals 0 or CH.sub.2 ;X or Z equals O, S, NH or denotes CH.sub.2 whereby X and Z can be the same or different,V and W denote O, S, Se, NH.sub.2 or an alkyloxy residue, or OH or SH whereby V and W can be the same or different in a monomer unit andL is a H atom or a partner of a binding pair andC equals --O--R and R is an alkyl group with at least 1 C atom which may be modified if desired, or it denotes an alkenyl or alkynyl group with at least 2 C atoms which may be modified if desired, whereby the modification consists of a substitution by one or several halogen, cyano, carboxy, hydroxy, nitro or/and mercapto residues, andn is an arbitrary whole number, are stable antisense probes which bind specifically. Such oligonucleotides and polynucleotides may be used for the regulation of gene expression and as pharmaceutical agents. They are synthesized from the corresponding 2'-substituted monomers according to well-known methods, preferably on a solid phase.
    • 具有通式“IMAGE”的寡核苷酸,其中B表示任意的核碱基,A等于0或CH2; X或Z等于O,S,NH或CH2,由此X和Z可以相同或不同,V和W表示O,S,Se,NH2或烷氧基残基,或OH或SH,由此V和W可以是 相同或不同的单体单元,L是H原子或结合对的配偶体,C等于-OR,R是具有至少1个C原子的烷基,如果需要可以进行修饰,或者表示烯基或 具有至少2个C原子的炔基,如果需要,可以进行修饰,由此修饰由一个或多个卤素,氰基,羧基,羟基,硝基或/和巯基残基取代,n是任意整数, 稳定的反义探针。 这样的寡核苷酸和多核苷酸可用于调节基因表达和作为药剂。 根据众所周知的方法,它们由相应的2'-取代单体合成,优选在固相上。