Modified nucleotides
    14.
    发明授权
    Modified nucleotides 有权
    修饰的核苷酸

    公开(公告)号:US07771973B2

    公开(公告)日:2010-08-10

    申请号:US12455397

    申请日:2009-06-01

    摘要: The invention provides modified nucleotide or nucleoside molecule comprising a purine or pyrimidine base and a ribose or deoxyribose sugar moiety having a removable 3′-OH blocking group covalently attached thereto, such that the 3′ carbon atom has attached a group of the structure —O—Z wherein Z is any of —C(R′)2-O—R″, —C(R′)2-N(R″)2, —C(R′)2-N(H)R″, —C(R′)2-S—R″ and —C(R″)2-F, wherein each R″ is or is part of a removable protecting group; each R′ is independently a hydrogen atom, an alkyl, substituted alkyl, arylalkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclic, acyl, cyano, alkoxy, aryloxy, heteroaryloxy or amido group, or a detectable label attached through a linking group; or (R′)2 represents an alkylidene group of formula ═C(R′″)2 wherein each R′″ may be the same or different and is selected from the group comprising hydrogen and halogen atoms and alkyl groups; and wherein said molecule may be reacted to yield an intermediate in which each R″ is exchanged for H or, where Z is —C(R′)2-F, the F is exchanged for OH, SH or NH2, preferably OH, which intermediate dissociates under aqueous conditions to afford a molecule with a free 3′OH; with the proviso that where Z is —C(R′)2-S—R″, both R′ groups are not H.

    摘要翻译: 本发明提供了修饰的核苷酸或核苷分子,其包含嘌呤或嘧啶碱基和核糖或脱氧核糖糖部分,其具有共价连接到其上的可移除的3'-OH封闭基团,使得3'碳原子连接一组结构-O -Z其中Z是-C(R')2 -O-R“,-C(R')2 -N(R”)2,-C(R')2 -N(H)R“ -C(R')2 -S-R“和-C(R”)2 -F,其中每个R“为或可除去保护基团的一部分; 每个R'独立地是氢原子,烷基,取代的烷基,芳基烷基,烯基,炔基,芳基,杂芳基,杂环,酰基,氰基,烷氧基,芳氧基,杂芳氧基或酰氨基,或通过连接基团连接的可检测标记; 或(R')2表示式≡C(R'“)2的亚烷基,其中每个R”可以相同或不同,并且选自氢和卤素原子和烷基; 并且其中所述分子可以反应以产生其中每个R“被交换为H的中间体,或其中Z是-C(R')2 -F,F被交换成OH,SH或NH 2,优选OH,其中 中间体在水性条件下解离得到具有游离3'OH的分子; 条件是其中Z是-C(R')2 -S-R“,两个R'基团不是H.

    Labelled nucleotides
    15.
    发明授权
    Labelled nucleotides 有权
    标记核苷酸

    公开(公告)号:US07414116B2

    公开(公告)日:2008-08-19

    申请号:US10525399

    申请日:2003-08-22

    摘要: The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl), T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

    摘要翻译: 本发明提供了具有通过可切割接头连接到可检测标记的碱基的核苷酸或核苷,其特征在于可切割连接体含有选自以下的部分:式(I)其中X选自O,S ,NH和NQ,其中Q是C 1-10取代或未取代的烷基,Y选自O,S,NH和N(烯丙基),T是氢或C < 取代或未取代的烷基,*表示部分与核苷酸或核苷的剩余部分连接的位置)。

    Pharmaceutical compounds
    16.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号:US06552021B2

    公开(公告)日:2003-04-22

    申请号:US09797902

    申请日:2001-03-05

    IPC分类号: C07D47104

    CPC分类号: C07D471/04 C07D487/04

    摘要: A compound which is a heteroaromatic[a]phenazine carboxamide derivative of formula (I) wherein X is a five- or six-membered heteroaromatic ring which contains one or two nitrogen atoms and which is unsubstituted or substituted by C1-C6 alkyl, hydroxyl or C1-C6 alkoxy; Q is C1-C6 alkylene which is unsubstituted or substituted by C1-C6 alkyl which is unsubstituted or substituted by a hydroxy group; and R1 and R2 which are the same or different are each C1-C6 alkyl; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of topoisomerase I and II and can be used to treat tumours, including tumours which express MDR.

    摘要翻译: 一种化合物,其是式(I)的杂芳族[a]吩嗪甲酰胺衍生物,其中X是含有一个或两个氮原子且未被取代或被C 1 -C 6烷基取代的五元或六元杂芳环,羟基或 C 1 -C 6烷氧基; Q是未被取代或被未取代或被羟基取代的C1-C6烷基取代的C1-C6亚烷基; 和相同或不同的R 1和R 2各自为C 1 -C 6烷基;或其药学上可接受的盐。 这些化合物是拓扑异构酶I和II的抑制剂,可用于治疗肿瘤,包括表达MDR的肿瘤。

    Labelled nucleotides
    19.
    发明授权
    Labelled nucleotides 有权
    标记核苷酸

    公开(公告)号:US07795424B2

    公开(公告)日:2010-09-14

    申请号:US12220682

    申请日:2008-07-24

    IPC分类号: C07H19/04 C07H21/04 C12Q1/68

    摘要: The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterized in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl). T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

    摘要翻译: 本发明提供了具有通过可切割接头连接到可检测标记的碱基的核苷酸或核苷,其特征在于所述可切割连接体含有选自以下的部分:式(I)(其中X选自O, S,NH和NQ,其中Q是C1-10取代或未取代的烷基,Y选自O,S,NH和N(烯丙基),T是氢或C1-10取代或未取代的烷基, *表示部分连接到核苷酸或核苷的剩余部分)。

    Modified nucleosides and nucleotides and uses thereof
    20.
    发明授权
    Modified nucleosides and nucleotides and uses thereof 有权
    修饰的核苷和核苷酸及其用途

    公开(公告)号:US07592435B2

    公开(公告)日:2009-09-22

    申请号:US11494279

    申请日:2006-07-27

    CPC分类号: C12Q1/686 C12Q2525/113

    摘要: The invention is directed to modified guanine-containing nucleosides and nucleotides and uses thereof. More specifically, the invention relates to modified fluorescently labelled guanine-containing nucleosides and nucleotides which exhibit enhanced fluorophore intensity by virtue of reduced quenching effects.

    摘要翻译: 本发明涉及修饰的含鸟嘌呤核苷及其用途。 更具体地,本发明涉及经修饰的荧光标记的含有鸟嘌呤的核苷和核苷酸,其通过降低猝灭效应表现出增强的荧光团强度。