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    IKK-BETA SERINE-THREONINE PROTEIN KINASE INHIBITORS
    4.
    发明授权
    IKK-BETA SERINE-THREONINE PROTEIN KINASE INHIBITORS 有权
    IKK-β-SERIN - 苏氨酸蛋白激酶抑制剂

    公开(公告)号：EP2078007B1

    公开(公告)日：2011-08-31

    申请号：EP07824358.1

    申请日：2007-10-29

    申请人： Chroma Therapeutics Limited

    发明人： MOFFAT, David, Festus, Charles ,  DAVIES, Stephen, John ,  CHARLTON, Michael, Hugh ,  HIRST, Simon, Christopher ,  ONIONS, Stuart, Thomas ,  WILLIAMS, Jonathon, Gareth

    IPC分类号： C07D333/38 ,  A61K31/381

    CPC分类号： C07D333/38

    摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) 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) a radical of formula R1R2CHNH-Y-L1-X1-(CH2)Z- wherein: z is 0 or 1; 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; R2 is the side chain of a natural or non- natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -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 linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.

    ENZYME INHIBITORS
    5.
    发明授权
    ENZYME INHIBITORS 有权
    酶抑制剂

    公开(公告)号：EP1879895B1

    公开(公告)日：2011-06-08

    申请号：EP06726982.9

    申请日：2006-05-04

    申请人： Chroma Therapeutics Limited

    发明人： DAVIDSON, Alan Hornsby ,  PATEL, Sanjay Ratilal ,  MAZZEI, Francesca Ann ,  DAVIES, Stephen John ,  DRUMMOND, Alan Hastings ,  MOFFAT, David Festus C. ,  BAKER, Kenneth William John ,  DONALD, Alistair David Graham

    IPC分类号： C07D487/04 ,  C07D295/18 ,  C07D217/12 ,  C07D333/62 ,  A61K31/4045 ,  A61K31/4353 ,  A61K31/4965 ,  A61P35/00

    CPC分类号： C07C237/40 ,  C07C259/06 ,  C07C275/24 ,  C07C311/46 ,  C07C317/50 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/416 ,  C07D209/42 ,  C07D213/40 ,  C07D217/02 ,  C07D217/22 ,  C07D217/26 ,  C07D295/185 ,  C07D295/192 ,  C07D333/70 ,  C07D471/04

    摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -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 , Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5 - 13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula -X2-Q1- or -Q1-X2- wherein X2 is -O-, S- or NRA- wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5 - 13 ring members, AIk1 and AIk2 independently represent optionally substituted divalent C3-C7 cycloalkyl radicals, or optionally substituted straight or branched, C1-C6 alkylene, C2-C6 alkenylene ,or C2-C6 alkynylene radicals which may optionally contain or terminate in an ether (-O-), thioether (-S-) or amino (-NRA-) link wherein RA is hydrogen or optionally substituted C1-C3 alkyl; 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; z is 0 or 1 ; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals R1R2NH-Y-L1-X1-[CH2]Z- and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONHOH, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the hydroxamic acid group, is equivalent to that of an unbranched saturated hydrocarbon chain of from 3-10 carbon atoms.

    INHIBITORS OF P38 MAP KINASE
    6.
    发明公开
    INHIBITORS OF P38 MAP KINASE 有权
    P38 MAP激酶抑制剂

    公开(公告)号：EP2245012A1

    公开(公告)日：2010-11-03

    申请号：EP09713855.6

    申请日：2009-02-27

    申请人： Chroma Therapeutics Limited

    发明人： MOFFAT, David, Festus, Charles ,  DAVIES, Stephen, John ,  PINTAT, Stéphane

    IPC分类号： C07D213/73 ,  A61K31/44 ,  A61P1/00 ,  A61P29/00 ,  A61P37/00

    CPC分类号： C07D213/73

    摘要： 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; -X
    1 -L
    1 -Y- is a linker radical or bond; R
    1 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 R
    2 and R
    3 are as defined in the claims.

    INHIBITORS OF IKK- BETA SERINE-THREONINE PROTEIN KINASE
    7.
    发明公开
    INHIBITORS OF IKK- BETA SERINE-THREONINE PROTEIN KINASE 有权
    IKK-β丝氨酸 - 苏氨酸蛋白激酶的抑制剂

    公开(公告)号：EP2086956A1

    公开(公告)日：2009-08-12

    申请号：EP07824361.5

    申请日：2007-10-29

    申请人： Chroma Therapeutics Limited

    发明人： MOFFAT, David, Festus, Charles ,  DAVIES, Stephen, John ,  CHARLTON, Michael, Hugh ,  HIRST, Simon, Christopher ,  ONIONS, Stuart, Thomas ,  WILLIAMS, Jonathon, Gareth

    IPC分类号： C07D333/38 ,  A61K31/381

    CPC分类号： C07D333/38

    摘要： 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 (C1C6)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 (CrC6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and AIk2 are as defined in the claims.

    摘要翻译： 式（IA）或（IB）化合物是IkB激酶（IKK）活性的抑制剂，并且可用于治疗其中R 7为氢或任选取代的（C 1 -C 6）烷基的自身免疫疾病和炎性疾病; 环A是5-13个环原子的任选取代的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R为式（X）或（Y）的基团，R 1为羧酸基团（-COOH），或可被一种或多种细胞内酯酶酶解为羧酸基团的酯基; 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; （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 - （Alk1）m（Q）n（Alk2）p-的连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。