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    Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity
    1.
    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

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

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

    IPC分类号： C07D333/70 ,  C07C229/36

    CPC分类号： C07C259/06 ,  C07D333/70

    摘要： 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.

    DHFR enzyme inhibitors
    5.
    发明授权
    DHFR enzyme inhibitors 失效
    DHFR酶抑制剂

    公开(公告)号：US08211900B2

    公开(公告)日：2012-07-03

    申请号：US12299356

    申请日：2007-04-24

    申请人： Alan Hornsby Davidson

    发明人： Alan Hornsby Davidson

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D471/00

    CPC分类号： C07D239/95 ,  C07D471/04

    摘要： Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: wherein A and D are independently —CHR7— or —NR7—; E and G are independently ═CR7— or ═N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; 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 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)NR3—, —C(═S)—NR3, —C(═NH)NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and 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.

    摘要翻译： 式（I）或（II）的化合物是二氢叶酸还原酶抑制剂，可用于治疗例如细胞增殖性疾病：其中A和D独立地是-CHR7-或-NR7-; E和G独立地为= CR7-或= N-; 每个R6独立地表示氢或-OR7; R7是氢或C1-C6烷基; 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是不含羧基或羧基酯基团的天然或非天然α氨基酸的侧链; Y是一个键，-C（= O） - ， - S（= O）2 - ， - C（= O）NR 3 - ， - （C 1 -C 6）-NR 3，-C（= NH）NR 3或-S （= O）2 NR 3 - 其中R 3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和p独立地为0或1，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。

    Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity
    6.
    发明授权
    Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
    喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂

    公开(公告)号：US08148531B2

    公开(公告)日：2012-04-03

    申请号：US11918898

    申请日：2006-05-04

    申请人： Alan Hornsby Davidson ,  Stephen John Davies ,  David Festus Charles Moffat

    发明人： Alan Hornsby Davidson ,  Stephen John Davies ,  David Festus Charles Moffat

    IPC分类号： C07D215/00

    CPC分类号： C07D215/42 ,  C07D215/233 ,  C07D215/36 ,  C07D215/44 ,  C07D239/90 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or —NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; 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-C7 cycloalkyl, 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 D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.

    摘要翻译： 式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如 索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（= O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q为≡N-，═CH-或≡C（X1） - 其中X1为氰基，环丙基或卤素; 连接基团L2如权利要求中所定义; 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C 1 -C 6烷基，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基，杂芳基（C 1 -C 6烷基） - ，（C = O）R 3， - （C = O）OR 3 ，或 - （C = O）NR 3，其中R3是氢或任选取代的（C1-C6）烷基，C3-C7环烷基，芳基，芳基（C1-C6烷基） - ，杂芳基或杂芳基（C1-C6烷基） ; R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。

    Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity
    8.
    发明申请
    Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
    喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂

    公开(公告)号：US20090131461A1

    公开(公告)日：2009-05-21

    申请号：US11918898

    申请日：2006-05-04

    申请人： Alan Hornsby Davidson ,  Stephen John Davies ,  David Festus Charles Moffat

    发明人： Alan Hornsby Davidson ,  Stephen John Davies ,  David Festus Charles Moffat

    IPC分类号： A61K31/517 ,  C07D215/20 ,  A61K31/47 ,  C07D401/02 ,  A61P35/00 ,  A61P37/00 ,  A61K31/506 ,  C07D239/72

    CPC分类号： C07D215/42 ,  C07D215/233 ,  C07D215/36 ,  C07D215/44 ,  C07D239/90 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X is cyano, cyclopropyl or halo; linker radicals L are as defined in the claims; 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-C7 cycloalkyl, 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 D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.

    摘要翻译： 式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如 索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（-O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q是-N-，-CH-或-C（X1） - ，其中X是氰基，环丙基或卤素; 连接基自由基L如权利要求中所定义; 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（C 1 -C 6烷基） - ， - （CO）R 3， - （CO）OR 3或 - （ CO）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基或杂芳基（C 1 -C 6烷基） R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。

    Hydroxamates as inhibitors of histone deacetylase
    9.
    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

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

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

    IPC分类号： C07D345/00 ,  C07D239/42

    CPC分类号： C07D239/42

    摘要： 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—.

    摘要翻译： 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。