利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

13 条记录 (耗时 0.017 秒)

    INHIBITORS OF PLK
    5.
    发明公开
    INHIBITORS OF PLK 审中-公开
    PLK抑制剂

    公开(公告)号：EP2296662A1

    公开(公告)日：2011-03-23

    申请号：EP09735114.2

    申请日：2009-04-23

    申请人： Chroma Therapeutics Ltd.

    发明人： MOFFAT, David, Festus, Charles ,  PATEL, Sanjay, Ratilal ,  BAKER, Kenneth, William, John ,  NORTH, Carl, Leslie

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

    CPC分类号： C07D475/00

    摘要： Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R
    1 is hydrogen, or an optionally substituted (C
    1 -C
    6) aIkyl, (C
    2 -C
    6 )alkenyl, (C
    2 - C
    6 )alkynyl or (C
    3 -C
    6 )cycloalkyl group; R
    2 is hydrogen, or an optionally substituted (C
    1 - C
    6 )alkyl, (C
    2 -C
    6 )alkenyl, (C
    2 -C
    6 )alkynyl or (C
    3 -C
    6 )cycloalkyl group; R
    3 is hydrogen, -CN, hydroxyl, halogen, optionally substituted (C
    1 C
    6 )alkyl, (C
    2 -C
    6 )alkenyl, (C
    2 -C
    6 )alkynyl or (C
    3 -C
    6 )cycloalkyl, -NR
    5 R
    6 or C
    1 -C
    4 alkoxy, wherein R
    5 and R
    6 are independently hydrogen or optionally substituted (C
    1 -C
    6 )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-L
    1 -Y
    1 - wherein L
    1 and Y
    1 are as defined in the claims and R is an carbon-linked, alpha alpha disubstituted amino acid or amino acid ester residue.

    INHIBITORS OF IKK- SERINE-THREONINE PROTEIN KINASE
    8.
    发明公开
    INHIBITORS OF IKK- SERINE-THREONINE PROTEIN KINASE 有权
    IKK-丝氨酸 - 苏氨酸蛋白激酶的抑制剂

    公开(公告)号：EP2297128A1

    公开(公告)日：2011-03-23

    申请号：EP08737089.6

    申请日：2008-04-23

    申请人： Chroma Therapeutics Ltd.

    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 ,  A61P25/28 ,  A61P37/00

    CPC分类号： C07D333/38

    摘要： Cyclopentyl (2S,4
    E )-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl (2S,4
    E )-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl (2S,4
    E )-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl
    O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl
    O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienylJphenyl}-L-homoserinate; Cyclopentyl
    N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and
    tert -Butyl
    N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.

    摘要翻译： （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基]苯基}戊-4-烯酸环戊酯; 5- {3- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基]苯基} -L-正缬氨酸环戊酯; （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -5-甲基苯基}戊-4-烯酸环戊酯; （2S，4E）-2-氨基-5- {5- [4-氨基甲酰基-5-（氨基甲酰氨基）-2-噻吩基] -2-甲基苯基}戊-4-烯酸环戊酯; O- [3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸环戊酯; N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸环戊酯; 和N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸，并用于抑制IKKβ活性 。

    SUBSTITUTED THIOPHENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS
    9.
    发明公开
    SUBSTITUTED THIOPHENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS 审中-公开
    取代噻吩羧AS IKK-BETA-SERIN-，苏氨酸蛋白激酶抑制剂

    公开(公告)号：EP2285797A1

    公开(公告)日：2011-02-23

    申请号：EP09733957.6

    申请日：2009-04-23

    申请人： Chroma Therapeutics Ltd.

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

    IPC分类号： C07D333/38 ,  A61K31/381

    CPC分类号： C07D333/38

    摘要： Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R
    7 is hydrogen or optionally substituted (C
    1 -C
    6 )alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R
    1 C( R
    2 )(R
    3 )NH-Y-L
    1 -X1-(CH
    2 )
    z - wherein 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 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R
    2 and R
    3 is hydrogen, or R
    2 and R
    3 taken together with the carbon atom to which they are attached form a C
    3 -C
    7 cycloalkyl ring, and z, Y, L
    1 and X
    1 are as defined in the claims.

    IMAGING AGENTS
    10.
    发明公开
    IMAGING AGENTS 审中-公开
    造影剂

    公开(公告)号：EP2651454A1

    公开(公告)日：2013-10-23

    申请号：EP11808255.1

    申请日：2011-12-16

    申请人： Chroma Therapeutics Ltd.

    发明人： CHARLTON, Michael Hugh ,  MOFFAT, David Festus Charles ,  DAVIES, Steven John ,  DRUMMOND, Alan Hastings

    IPC分类号： A61K49/00 ,  C07D271/12 ,  C07F5/02

    CPC分类号： A61K49/0021 ,  C07D271/12 ,  C07F5/003 ,  C07F5/02 ,  G01N33/582

    摘要： An imaging agent for cells which produces an intracellular imaging signal proportional to the amount of hCE-1 in the cells independently of the amount of hCE-2 and/or hCE-3 in the cells, said imaging agent being a covalent conjugate of (a) an imaging agent and (b) an alpha mono- or di-substituted amino acid ester, wherein (a) is directly linked to (b), or (a) is indirectly linked to (b) by a linker radical, and wherein said direct or indirect linkage is via the amino group of (b), and wherein the amino group is not directly linked to a carbonyl group, and wherein the said alpha mono- or di-substituted amino acid ester part is selectively hydrolysable to the corresponding carboxylic acid part by the intracellular carboxylesterase enzyme hCE-1 relative to the intracellular enzymes hCE-2 or hCE-3.