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    ENZYME INHIBITORS
    5.
    发明申请
    ENZYME INHIBITORS 审中-公开
    酶抑制剂

    公开(公告)号：US20140155439A1

    公开(公告)日：2014-06-05

    申请号：US14175072

    申请日：2014-02-07

    申请人： Alastair David Graham Donald ,  David Festus Charles Moffat ,  Andrew James Belfield ,  Carl Leslie North ,  Stewart Andrew Wayne Jones

    发明人： Alastair David Graham Donald ,  David Festus Charles Moffat ,  Andrew James Belfield ,  Carl Leslie North ,  Stewart Andrew Wayne Jones

    IPC分类号： C07D213/56 ,  C07C237/20

    CPC分类号： C07C237/20 ,  C07C259/06 ,  C07C2601/08 ,  C07D213/56 ,  C07D213/58

    摘要： Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C═O)—, —S(═O)2—, —C(C═O)O—, —C(C═O)NR′—, —C(═S)—NR′, —C(═NH)NR′ or —S(═O)2NR— wherein R′ is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(C═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.

    摘要翻译： 式（I）化合物抑制HDAC活性：其中A，B和D独立地表示= CH-或= N-; W是-CH = CH-或-CH 2 CH 2 - ; R1是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R2和R3选自天然或非天然α氨基酸的侧链，条件是R2和R3都不是氢，或者R2和R3与它们所连接的碳一起形成3-6 元环饱和环烷基或杂环基环; Y是键，-C（= O） - ， - S（= O）2 - ， - C（C = O）O-，-C（C = O）NR' - ， - -NR'，-C（= NH）NR'或-S（= O）2 NR-，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价基团，其中n，n，p，Q，Alk1和Alk2如权利要求中所定义; X1表示键; -C（= O）; 或-S（= O）2 - ; -NR 4 C（= O） - ， - C（C = O）NR 4 - ，-NR 4 C（= O）NR 5 - ，-NR 4 S（= O）2 - 或-S（= O）2 NR 4 - 独立地是氢或任选取代的C 1 -C 6烷基; z为0或1。