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    Pyrimidine nucleoside compounds and oligonucleoside compounds containing same
    4.
    发明授权
    Pyrimidine nucleoside compounds and oligonucleoside compounds containing same 失效
    嘧啶核苷化合物和含有其的寡核苷酸化合物

    公开(公告)号：US6060592A

    公开(公告)日：2000-05-09

    申请号：US212006

    申请日：1994-03-11

    申请人： Oscar L. Acevedo ,  Martin G. Dunkel ,  Phillip Dan Cook

    发明人： Oscar L. Acevedo ,  Martin G. Dunkel ,  Phillip Dan Cook

    IPC分类号： A61K31/70 ,  C07H19/06 ,  C07H21/00

    CPC分类号： C12N15/1137 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H23/00 ,  C07J43/003 ,  C07K14/005 ,  C12N15/113 ,  C12N9/0069 ,  C12Q1/68 ,  C12Q1/6813 ,  C12Y113/11012 ,  A61K48/00 ,  C12N2310/3125 ,  C12N2310/315 ,  C12N2310/32 ,  C12N2310/321 ,  C12N2310/322 ,  C12N2310/33 ,  C12N2310/333 ,  C12N2310/336 ,  C12N2310/3511 ,  C12N2310/3521 ,  C12N2310/3523 ,  C12N2310/3527 ,  C12N2310/3531 ,  C12N2310/3533 ,  C12N2740/16322 ,  Y02P20/55

    摘要： Novel 2- and 4-substituted pyrimidine nucleosides and oligonucleosides are provided, as are methods and intermediates useful in preparing same. In preferred embodiments, one of the 2- and 4-substituents is .dbd.O, .dbd.NH, or .dbd.NH.sub.2.sup.+ and the other is Q, .dbd.C (R.sub.A)--Q, C(R.sub.A)(R.sub.B)--C(R.sub.C)(R.sub.D)--Q, C (R.sub.A).dbd.C(R.sub.C)--Q or C.tbd.C--Q, where R.sub.A, R.sub.B, R.sub.C and R.sub.D independently are H, SH, OH, NH.sub.2, or C.sub.1 -C.sub.20 alkyl, or one of (R.sub.A)(R.sub.B) or (R.sub.C)(R.sub.D) is .dbd.O, and Q is halogen, hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkylamine, C.sub.1 -C.sub.20 alkyl-N-phthalimide, C.sub.1 -C.sub.20 alkylimidazole, C.sub.1 -C.sub.20 alkylbis-imidazole, imidazole, bis-imidazole, amine, N-phthalimide, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, hydroxyl, thiol, keto, carboxyl, nitrates, nitro, nitroso, nitrile, trifluoromethyl, trifluoromethoxy, O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aralkyl, S-aralkyl, NH-aralkyl, azido, hydrazino, hydroxylamino, isocyanato, sulfoxide, sulfone, sulfide, disulfide, silyl, O-(hydroxyl protecting group), a leaving group, a heterocycle, an intercalator, a reporter molecule, a conjugate, a polyamine, a polyamide, a polyethylene glycol, a polyether, or a depurination enhancing group.

    摘要翻译： 提供新的2-和4-取代的嘧啶核苷和寡核苷，以及可用于制备它们的方法和中间体。 在优选的实施方案中，2-和4-取代基之一是= O，= NH或= NH 2 +，另一个是Q，= C（RA）-Q，C（RA）（RB）-C（RC） RD）-Q，C（RA）= C（RC）-Q或C 3BOND CQ，其中RA，RB，RC和RD独立地为H，SH，OH，NH2或C1-C20烷基，或（RA ）（RB）或（RC）（RD）为= O，Q为卤素，氢，C1-C20烷基，C1-C20烷基胺，C1-C20烷基-N-邻苯二甲酰亚胺，C1-C20烷基咪唑，C1-C20烷基双 咪唑，双咪唑，胺，N-邻苯二甲酰亚胺，C2-C20烯基，C2-C20炔基，羟基，硫醇，酮基，羧基，硝酸酯，硝基，亚硝基，腈，三氟甲基，三氟甲氧基，O-烷基， - 烷基，N-烷基，N-二烷基，O-芳烷基，S-芳烷基，NH-芳烷基，叠氮基，肼基，羟基氨基，异氰酸根合，亚砜，砜，硫醚，二硫化物，甲硅烷基，O-（羟基保护基） 离去基团，杂环，嵌入剂，报道分子，缀合物，多胺，聚酰胺，聚乙二醇，聚醚或脱毒增强基团。

    Sugar-modified 7-deaza-7-substituted oligonucleotides
    6.
    发明授权
    Sugar-modified 7-deaza-7-substituted oligonucleotides 失效
    糖修饰的7-脱氮-7-取代的寡核苷酸

    公开(公告)号：US6093807A

    公开(公告)日：2000-07-25

    申请号：US272977

    申请日：1999-03-19

    申请人： Guity P. Balow ,  Oscar L. Acevedo ,  Phillip Dan Cook

    发明人： Guity P. Balow ,  Oscar L. Acevedo ,  Phillip Dan Cook

    IPC分类号： C07H19/14 ,  C07H19/16 ,  C07H21/02

    CPC分类号： C07H19/16 ,  C07H19/14

    摘要： Functionalized nucleomonomers and oligonucleotides are provided which have increased nuclease resistance and enhanced binding affinity to target DNA or RNA molecules. The oligonucleotides of the present invention comprise at least one 7-deaza-7-iodo-2'-substituted purine, herein referred to as a functionalized nucleomonomer. A preferred 2' substituent on the sugar moiety is a 2'-O-alkoxy alkyl group. More preferably, the 2'-substituent is 2'--O--CH.sub.2 --CH.sub.2 --O--CH.sub.3 (or 2'-methoxyethoxy). Such oligonucleotides are useful as therapeutics for modulating protein expression in organisms and treating disease states susceptible to oligonucleotide therapeutics. Such oligonucleotides are also useful as diagnostics for the diagnosis and detection of disease states, and as research reagents.

    摘要翻译： 提供功能化的核小体单体和寡核苷酸，其具有增加的核酸酶抗性并增强与靶DNA或RNA分子的结合亲和力。 本发明的寡核苷酸包含至少一种7-脱氮-7-碘-2'-取代嘌呤，在本文中称为官能化核小体单体。 糖部分上优选的2'取代基是2'-O-烷氧基烷基。 更优选地，2'-取代基是2'-O-CH 2 -CH 2 -O-CH 3（或2'-甲氧基乙氧基）。 这样的寡核苷酸可用作调节生物体中的蛋白质表达并治疗对寡核苷酸治疗敏感的疾病状态的治疗剂。 这样的寡核苷酸也可用作诊断和检测疾病状态以及作为研究试剂。