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    MODIFIED NUCLEOTIDES
    85.
    发明申请
    MODIFIED NUCLEOTIDES 审中-公开
    改性核酸

    公开(公告)号：US20160362737A1

    公开(公告)日：2016-12-15

    申请号：US15179813

    申请日：2016-06-10

    Applicant: Illumina Cambridge Limited

    Inventor： John MILTON ,  Xiaolin WU ,  Mark SMITH ,  Joseph BRENNAN ,  Colin BARNES ,  Xiaohai LIU ,  Silke RUEDIGER

    IPC: C12Q1/68 ,  C07H19/14 ,  C07H19/10

    CPC classification number: C12Q1/6869 ,  C07H1/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C12Q2525/186 ,  C12Q2535/113 ,  Y02P20/55 ,  C12Q2525/197

    Abstract: 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.

    Abstract translation: 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”为或可移除的保护基团的一部分; 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.

    INHIBITORS OF PROTEIN METHYLTRANSFERASE DOT1L AND METHODS OF USE THEREOF
    90.
    发明申请
    INHIBITORS OF PROTEIN METHYLTRANSFERASE DOT1L AND METHODS OF USE THEREOF 审中-公开
    蛋白质甲基转移酶DOT1L的抑制剂及其使用方法

    公开(公告)号：US20150284422A1

    公开(公告)日：2015-10-08

    申请号：US14420877

    申请日：2013-08-12

    Applicant: Epizyme, Inc.

    Inventor： Edward J. Olhava ,  Richard Chesworth ,  Roy M. Pollock ,  Lei Jin

    IPC: C07H19/16 ,  C40B30/02 ,  G06F19/16 ,  C07H19/14

    CPC classification number: C07H19/16 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07D473/34 ,  C07H19/14 ,  G16B15/00 ,  G16B35/00 ,  G16C20/60

    Abstract: The present invention relates to DOT1L inhibitors and methods of identifying, designing, or optimizing them. The present invention also relates to crystals of DOT1L-inhibitor complexes, the crystal structures thereof, and the use of the crystal structures. Also disclosed are pharmaceutical compositions containing these DOT1L inhibitors and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

    Abstract translation: 本发明涉及DOT1L抑制剂及其鉴别，设计或优化方法。 本发明还涉及DOT1L抑制剂复合物的晶体，其晶体结构以及晶体结构的用途。 还公开了含有这些DOT1L抑制剂的药物组合物和通过将这些化合物和药物组合物给予有需要的受试者来治疗其中DOT1介导的蛋白质甲基化作用的疾病如癌症和神经障碍的方法。

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