中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

43 records (took 0.023 seconds)

    Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase
    23.
    发明申请
    Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase 失效
    IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂

    公开(公告)号：US20100069473A1

    公开(公告)日：2010-03-18

    申请号：US12447271

    申请日：2007-10-29

    Applicant: David Festus Charles Moffat ,  Stephen John Davies ,  Michael Hugh Charlton ,  Simon Christopher Hirst ,  Stuart Thomas Onions ,  Jonathon Gareth Williams

    Inventor： David Festus Charles Moffat ,  Stephen John Davies ,  Michael Hugh Charlton ,  Simon Christopher Hirst ,  Stuart Thomas Onions ,  Jonathon Gareth Williams

    IPC: A61K31/381 ,  C07D333/36 ,  C12N9/99 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P11/00 ,  A61P17/00 ,  A61P3/10

    CPC classification number: C07D333/38

    Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) 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; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; 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)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.

    Abstract translation: 式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：其中R 7为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R是式（X）或（Y）的基团，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; R 6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 = O）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; Y1是一个键， - （C = O） - ， - S（O 2） - ， - C（= O）O-，-OC（= O） - ， - （C = O）NR 3 - ， - NR 3 （O） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（C = O）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6） 式 - （Alk1）m（Q）n（Alk2）p的二价连接基团其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

    HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY
    24.
    发明申请
    HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY 有权
    作为HDAC酶活性抑制剂的羟基酸衍生物

    公开(公告)号：US20090298924A1

    公开(公告)日：2009-12-03

    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: A61K31/381 ,  C07C229/36 ,  A61K31/235 ,  C07D333/70 ,  C12N9/99

    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(O)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;

    Abstract translation: 式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症：其中Y 1为键， - （CO） - ， - S（O 2） - ， - C ）-O-，-OC（-O） - ， - （CO）NR 3 - ， - NR 3（CO） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（CO）NR 5 - 其中R 3和R 5独立地是氢或任选取代的（C 1 -C 6）烷基，L 1是式 - （Alk 1）m（O）n（Alk 2）p的二价基团其中m，n，p，Alk1，Alk2和Q 如权利要求中所定义; z为0或1; A表示任选取代的单环，双环或三环碳环或杂环系; - [连接子] - 表示二价连接基团; 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; 并且B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B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;

    DHFR enzyme inhibitors
    27.
    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

    Applicant: Alan Hornsby Davidson

    Inventor： Alan Hornsby Davidson

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

    CPC classification number: C07D239/95 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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
    28.
    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

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

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

    IPC: C07D215/00

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

    Abstract: 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.

    Abstract translation: 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。

    Inhibitors of IKK-beta serine-threonine protein kinase
    29.
    发明授权
    Inhibitors of IKK-beta serine-threonine protein kinase 失效
    IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂

    公开(公告)号：US08106091B2

    公开(公告)日：2012-01-31

    申请号：US12447271

    申请日：2007-10-29

    Applicant: David Charles Festus Moffat ,  Stephen John Davies ,  Michael Hugh Charlton ,  Simon Christopher Hirst ,  Stuart Thomas Onions ,  Jonathon Gareth Williams

    Inventor： David Charles Festus Moffat ,  Stephen John Davies ,  Michael Hugh Charlton ,  Simon Christopher Hirst ,  Stuart Thomas Onions ,  Jonathon Gareth Williams

    IPC: A61K31/381 ,  C07D333/36

    CPC classification number: C07D333/38

    Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) 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; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; 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)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.

    Abstract translation: 式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：其中R 7为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R是式（X）或（Y）的基团，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; R 6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 = O）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; Y1是一个键， - （C = O） - ， - S（O 2） - ， - C（= O）O-，-OC（= O） - ， - （C = O）NR 3 - ， - NR 3 （O） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（C = O）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6） 式 - （Alk1）m（Q）n（Alk2）p的二价连接基团其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

    P38 MAP kinase inhibitors
    30.
    发明授权
    P38 MAP kinase inhibitors 有权
    P38 MAP激酶抑制剂

    公开(公告)号：US08044211B2

    公开(公告)日：2011-10-25

    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: C07D213/72 ,  C07D239/02 ,  A61K31/505 ,  A61K31/44

    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)z—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包括类风湿性关节炎和COPD的炎性病症：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）z-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。

Patent Agency Ranking