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    Histone deacetylase inhibitors
    2.
    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。

    SUBSTITUTED THIOPENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS
    3.
    发明申请
    SUBSTITUTED THIOPENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS 审中-公开
    作为IKK-BETA SERINE-，THREONIN-PROTEIN激酶抑制剂的替代噻托溴铵

    公开(公告)号：US20110046210A1

    公开(公告)日：2011-02-24

    申请号：US12989271

    申请日：2009-04-23

    Applicant: David Festus Charles Moffat ,  Stephen John Davies

    Inventor： David Festus Charles Moffat ,  Stephen John Davies

    IPC: A61K31/381 ,  C07D333/38 ,  A61P37/00 ,  A61P29/00 ,  A61P35/00 ,  A61P19/02 ,  A61P17/06 ,  A61P1/00 ,  A61P1/04 ,  A61P3/10 ,  A61P25/28 ,  C12N9/99

    CPC classification number: C07D333/38

    Abstract: Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R1C(R2)(R3)NH—Y-L1-X1-(CH2)z— wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R2 and R3 is hydrogen, or R2 and R3 taken together with the carbon atom to which they are attached form a C3-C7 cycloalkyl ring, and z, Y, L1 and X1 are as defined in the claims.

    Abstract translation: 式（IA）或（IB）化合物是可用于治疗自身免疫性和炎性疾病的IKK抑制剂：其中R 7是氢或任选取代的（C 1 -C 6）烷基; A是任选取代的5-13个环原子的芳基或杂芳基; Z是式R1C（R2）（R3）NH-Y-L1-X1-（CH2）z-的基团，其中R1是羧酸基（-COOH）或可被一个或多个细胞内可水解的酯基 酯酶到羧酸基团; 并且R 2和R 3独立地表示天然或非天然α氨基酸的侧链，但R 2和R 3都不是氢，或者R 2和R 3与它们所连接的碳原子一起形成C 3 -C 7环烷基环 ，z，Y，L1和X1如权利要求中所定义。

    P38 Map Kinase Inhibitors
    5.
    发明申请
    P38 Map Kinase Inhibitors 有权
    P38图激酶抑制剂

    公开(公告)号：US20090099185A1

    公开(公告)日：2009-04-16

    申请号：US12299333

    申请日：2007-05-01

    Applicant: David Charles Festus Moffat ,  Stephane Pintat ,  Stephen Davies

    Inventor： David Charles Festus Moffat ,  Stephane Pintat ,  Stephen Davies

    IPC: A61K31/4412 ,  C07D211/76 ,  C12N9/99 ,  C07D413/12 ,  A61K31/5377 ,  A61P1/00 ,  A61P17/06 ,  A61P11/06 ,  A61P3/10 ,  A61P19/02 ,  A61P37/00 ,  A61P37/06

    CPC classification number: C07D213/73

    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═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 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), —X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.

    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-; D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; R6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），-X1-L1-Y-NH-CHR1R2的基团，其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z，Y，L1和X1如说明书中所定义; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链。

    Inhibitors of P38 map kinase
    8.
    发明授权
    Inhibitors of P38 map kinase 有权
    P38地图激酶抑制剂

    公开(公告)号：US08778953B2

    公开(公告)日：2014-07-15

    申请号：US12867774

    申请日：2009-02-27

    Applicant: David Festus Charles Moffat ,  Stephen John Davies ,  Stephane Pintat

    Inventor： David Festus Charles Moffat ,  Stephen John Davies ,  Stephane Pintat

    IPC: A01N43/54 ,  A61K31/505 ,  A01N43/40 ,  A61K31/44 ,  C07D239/02 ,  C07D213/72

    CPC classification number: C07D213/73

    Abstract: Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.

    Abstract translation: 式（I）化合物是可用于治疗自身免疫性和炎性疾病的p38 MAP激酶抑制剂：其中：G为-N =或-CH =; D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; R6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（IA）的基团; 其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z为0或1; -X1-L1-Y-是连接基或键; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; 并且R 2和R 3如权利要求中所定义。

    ENZYME INHIBITORS
    9.
    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。

    Inhibitors of PLK
    10.
    发明申请
    Inhibitors of PLK 审中-公开
    PLK抑制剂

    公开(公告)号：US20110190306A1

    公开(公告)日：2011-08-04

    申请号：US12989178

    申请日：2009-04-23

    Applicant: David Festus Charles Moffat ,  Sanjay Ratilal Patel ,  Kenneth William John Baker ,  Carl Leslie North

    Inventor： David Festus Charles Moffat ,  Sanjay Ratilal Patel ,  Kenneth William John Baker ,  Carl Leslie North

    IPC: A61K31/519 ,  C07D475/00 ,  A61P35/00

    CPC classification number: C07D475/00

    Abstract: Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R1 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 is hydrogen, —CN, hydroxyl, halogen, optionally substituted (C1C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, —NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1-Y1— wherein L1 and Y1 are as defined in the claims and R is an carbon-linked, alpha alpha disubstituted amino acid or amino acid ester residue.

    Abstract translation: 式（I）化合物是可用于治疗细胞增殖性疾病的PLK抑制剂：其中R 1是氢或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（ C3-C6）环烷基; R 2是氢或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R 3是氢，-CN，羟基，卤素，任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基，-NR 5 R 6或C 1 -C 4烷氧基， R6独立地为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的具有至多12个环原子的单环或双环碳环或杂环或环系; T是式R-L1-Y1-的基团，其中L1和Y1如权利要求中所定义，R是碳连接的α-α取代的氨基酸或氨基酸酯残基。

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