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    ENZYME INHIBITORS
    1.
    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。

    Hydroxamates as inhibitors of histone deacetylase
    3.
    发明授权
    Hydroxamates as inhibitors of histone deacetylase 有权
    羟肟酸盐作为组蛋白脱乙酰酶的抑制剂

    公开(公告)号：US08962825B2

    公开(公告)日：2015-02-24

    申请号：US12446267

    申请日：2006-10-30

    Applicant: David Charles Festus Moffat ,  Sanjay Ratilal Patel ,  Francesca Ann Day ,  Andrew James Belfield ,  Alistair David Graham Donald ,  Alan Hornsby Davidson ,  Alan Hastings Drummond

    Inventor： David Charles Festus Moffat ,  Sanjay Ratilal Patel ,  Francesca Ann Day ,  Andrew James Belfield ,  Alistair David Graham Donald ,  Alan Hornsby Davidson ,  Alan Hastings Drummond

    IPC: C07D345/00 ,  C07D239/42

    CPC classification number: C07D239/42

    Abstract: Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6). wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical; and R is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— or (b) a radical of formula R-L1-Y1—(CH2)z—.

    Abstract translation: 式（I）化合物及其盐，N-氧化物，水合物和溶剂化物是组蛋白脱乙酰酶抑制剂，可用于治疗细胞增殖性疾病，包括癌症：其中Q，V和W独立地表示-N =或-C ═; B是选自（B1），（B2），（B3），（B4），（B5）和（B6）的二价基团。 其中标记为*的键与包含Q，V和W通过 - [Linker1] - 的环连接，并且标记为**的键与A至 - [Linker2] - 连接。 A是任选取代的单环，二环或三环碳环或杂环系; - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团; 并且R是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-或（b）式R-L1-Y1-（CH2）z-的基团的基团。

    ENZYME INHIBITORS
    4.
    发明申请
    ENZYME INHIBITORS 审中-公开
    酶抑制剂

    公开(公告)号：US20130303576A1

    公开(公告)日：2013-11-14

    申请号：US13946488

    申请日：2013-07-19

    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: C07D213/58

    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(═O)—, —S(═O)2—, —C(═O)O—, —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)n(Alk2)p- wherein m, n, p, Q. Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —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-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR' - ， - ，-C（= NH）NR'或-S（= O）2 NH-，其中R'是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）n（Alk2）p-的二价基团，其中m，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 - ; -NR4C（= O） - ， - C（= O）NR4-，-NR4C（= O）NR5-，-NR4S（= O）2-或-S（= O）2NR4-，其中R4和R5独立地 氢或任选取代的C 1 -C 6烷基; z为0或1。

    Histone deacetylase inhibitors
    5.
    发明授权
    Histone deacetylase inhibitors 有权
    组蛋白脱乙酰酶抑制剂

    公开(公告)号：US07932246B2

    公开(公告)日：2011-04-26

    申请号：US11918237

    申请日：2006-05-15

    Applicant: David Festus Charles Moffat ,  Sanjay Ratilal Patel ,  Francesca Ann Mazzei ,  Andrew James Belfield ,  Sandra Van Meurs

    Inventor： David Festus Charles Moffat ,  Sanjay Ratilal Patel ,  Francesca Ann Mazzei ,  Andrew James Belfield ,  Sandra Van Meurs

    IPC: A01N43/00 ,  A61K31/33

    CPC classification number: C07D209/52 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04

    Abstract: Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.

    Abstract translation: 式（I）化合物及其盐，N-氧化物，水合物和溶剂合物是组蛋白脱乙酰酶抑制剂，可用于治疗包括癌症的细胞增殖性疾病：（I）其中Q，V和W独立地表示-N ═或-C =; B是选自：（IIA），（IIB），（IIC），（IID）和（IIE）的二价基团。 其中标有*的债券与含有Q，V和W的环通过 - [Linker1]相连，并且标记为**的债券与A至 - [Linker2] - 链接。 A是任选取代的单环，二环或三环碳环或杂环系; 和 - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团。

    ENZYME INHIBITORS
    6.
    发明申请
    ENZYME INHIBITORS 审中-公开
    酶抑制剂

    公开(公告)号：US20120149736A1

    公开(公告)日：2012-06-14

    申请号：US13202105

    申请日：2010-02-25

    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: A61K31/44 ,  C07C259/06 ,  A61K31/216 ,  A61K31/196 ,  A61P35/00 ,  A61P25/00 ,  A61P29/00 ,  A61P3/10 ,  A61P7/00 ,  A61P19/02 ,  A61P11/06 ,  A61P11/00 ,  A61P17/06 ,  A61P1/00 ,  C07D213/56

    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 intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural 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(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═5)—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)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —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），或可通过一个或多个细胞内羧酸酯酶可羧酸酯基的酯基; 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元饱和环烷基或杂环基环; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）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）n（Alk2）p-的二价基团，其中m，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（= O）NR 4 - ， - NR 4 C（= O）NR 5 - ，-NR 4 S（= O）2 - 或-S（= O）2 NR 4 - 氢或任选取代的C 1 -C 6烷基; z为0或1。

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