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    Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity
    11.
    发明授权
    Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity 有权

    公开(公告)号：US07973181B2

    公开(公告)日：2011-07-05

    申请号：US11919048

    申请日：2006-05-04

    Applicant: Alan Hornsby Davidson ,  Sanjay Ratilal Patel ,  David Festus Charles Moffat

    Inventor： Alan Hornsby Davidson ,  Sanjay Ratilal Patel ,  David Festus Charles Moffat

    IPC: C07D333/70 ,  C07C229/36

    CPC classification number: C07C259/06 ,  C07D333/70

    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi— or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein 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; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.

    Inhibitors of P38 Map Kinase
    14.
    发明申请
    Inhibitors of P38 Map Kinase 审中-公开
    P38地图激酶抑制剂

    公开(公告)号：US20090203711A1

    公开(公告)日：2009-08-13

    申请号：US12299498

    申请日：2007-05-01

    Applicant: David Charles Festus Moffat

    Inventor： David Charles Festus Moffat

    IPC: A61K31/4418 ,  C07D213/72 ,  C07D401/12 ,  A61K31/496 ,  A61P37/00 ,  A61P29/00

    CPC classification number: C07D213/73 ,  C07D401/12

    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N═ or —CH═; B is an optionally substituted divalent mono- or bicyclic aryl or heteroaryl radical having 5-13 ring members; R2 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z-L1-Y1—R wherein A, z, Y1, and L1 are as defined in the specification; R is a radical of formula (X) or (Y) wherein 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; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; and D is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring D is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.

    Abstract translation: 式（I）化合物是p38MAP激酶的抑制剂，因此可用于治疗特别是炎性病症，包括类风湿性关节炎和COPD：其中：G是-N-或-CH-; B是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R2是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式-A-（CH2）z-L1-Y1-R的基团，其中A，z，Y1和L1如说明书中所定义; R是式（X）或（Y）的基团，其中R 1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; R4是氢; 或任选取代的C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂芳基或 - （C-O）R 3， - （C 0）OR 3或 - （C-O）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基; 并且D是5或6个环原子的单环杂环，其中R 1与所示的环氮相邻的环碳连接，并且环D任选地与5或6个环原子的第二碳环或杂环稠合，在这种情况下 显示与波浪线相交的键可以来自所述第二环中的环原子。

    Methods and means of histone methylation
    15.
    发明授权
    Methods and means of histone methylation 失效
    组蛋白甲基化的方法和手段

    公开(公告)号：US07074578B2

    公开(公告)日：2006-07-11

    申请号：US10477225

    申请日：2002-05-02

    Applicant: Tony Kouzarides ,  Helena Santos-Rosa

    Inventor： Tony Kouzarides ,  Helena Santos-Rosa

    IPC: G01N33/53

    CPC classification number: C12N9/1007 ,  A61K38/00 ,  C12Q1/48 ,  G01N33/573

    Abstract: This invention relates to the methylation of histones, in particular to a previously uncharacterised group of histone H3 methylases which comprise a SET domain and which methylate either lysine 4 within the amino tail of histone H3 or within the histone H3 core. Methylation by these methylases, in particular trimethylation, is shown to be important for transcriptional activity.

    Abstract translation: 本发明涉及组蛋白的甲基化，特别是组合蛋白H3甲基化酶的先前未表征的组，其包含SET结构域，甲基化组氨酸H3氨基末端内的赖氨酸4或组蛋白H3核心内的甲基化。 这些甲基化酶特别是三甲基化的甲基化被证明对于转录活性是重要的。

    ENZYME INHIBITORS
    18.
    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

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

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

    IPC: C07D213/56 ,  C07C237/20

    CPC classification number: C07C237/20 ,  C07C259/06 ,  C07C2601/08 ,  C07D213/56 ,  C07D213/58

    Abstract: 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.

    Abstract translation: 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。

    IMAGING AGENTS
    20.
    发明申请
    IMAGING AGENTS 审中-公开
    成像代理

    公开(公告)号：US20140010762A1

    公开(公告)日：2014-01-09

    申请号：US13994835

    申请日：2011-12-16

    Applicant: Margaret Struthers Drummond

    Inventor： Michael Hugh Charlton ,  David Festus Charles Moffat ,  Stephen John Davies ,  Alan Hastings Drummond

    IPC: A61K49/00 ,  C07F5/02 ,  G01N33/58 ,  C07D271/12

    CPC classification number: A61K49/0021 ,  C07D271/12 ,  C07F5/003 ,  C07F5/02 ,  G01N33/582

    Abstract: An imaging agent for cells which produces an intracellular imaging signal proportional to the amount of hCE-1 in the cells independently of the amount of hCE-2 and/or hCE-3 in the cells, said imaging agent being a covalent conjugate of (a) an imaging agent and (b) an alpha mono- or di-substituted amino acid ester, wherein (a) is directly linked to (b), or (a) is indirectly linked to (b) by a linker radical, and wherein said direct or indirect linkage is via the amino group of (b), and wherein the amino group is not directly linked to a carbonyl group, and wherein the said alpha mono- or di-substituted amino acid ester part is selectively hydrolysable to the corresponding carboxylic acid part by the intracellular carboxylesterase enzyme hCE-1 relative to the intracellular enzymes hCE-2 or hCE-3.

    Abstract translation: 一种用于细胞的成像剂，其与细胞中hCE-2和/或hCE-3的量独立地产生与细胞中hCE-1的量成比例的细胞内成像信号，所述显像剂是（a ）成像剂和（b）α单取代或二取代的氨基酸酯，其中（a）直接与（b）连接，或（a）通过连接基团间接连接到（b），并且其中 所述直接或间接连接通过（b）的氨基，并且其中氨基不直接连接到羰基上，并且其中所述α单取代或二取代的氨基酸酯部分可选择性地水解成相应的 羧酸部分通过细胞内羧酸酯酶hCE-1相对于细胞内酶hCE-2或hCE-3。

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