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    9H-PYRIMIDO[4,5-B]INDOLES, 9H-PYRIDO[4',3':4,5]PYRROLO[2,3-D]PYRIDINES, AND 9H 1,3,6,9 TETRAAZA-FLUORENES AS CHK1 KINASE FUNCTION INHIBITORS
    1.
    发明申请
    9H-PYRIMIDO[4,5-B]INDOLES, 9H-PYRIDO[4',3':4,5]PYRROLO[2,3-D]PYRIDINES, AND 9H 1,3,6,9 TETRAAZA-FLUORENES AS CHK1 KINASE FUNCTION INHIBITORS 有权
    9H-吡咯并[4,5-B]吲哚，9H-吡啶并[4'，3'：4,5]吡咯并[2,3-D]吡啶和9,3,6,9四氢噻吩 - 激素功能抑制剂

    公开(公告)号：US20100210639A1

    公开(公告)日：2010-08-19

    申请号：US12665961

    申请日：2008-07-01

    申请人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61P35/00 ,  C12N5/00

    CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D487/14

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些三环化合物（本文称为TC化合物），特别是某些9H-嘧啶并[4,5-b]吲哚，9H-吡啶并[4' 3'：4,5]吡咯并[2,3-d]吡啶和9 H-1,3,6,9-四氮杂芴化合物，其特别地抑制检测点激酶1（CHK1）激酶功能。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。

    9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
    2.
    发明授权
    9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors 有权
    9H-嘧啶并[4,5-B]吲哚，9H-吡啶并[4'，3'：4,5]吡咯并[2,3-D]吡啶，和9H 1,3,6,9四氮杂芴作为CHK1 激酶功能抑制剂

    公开(公告)号：US08618121B2

    公开(公告)日：2013-12-31

    申请号：US12665961

    申请日：2008-07-01

    申请人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  Suki Klair ,  Jane Scanlon ,  Glynn Addison ,  Michael Cherry

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

    CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D487/14

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些三环化合物（本文称为TC化合物），特别是某些9H-嘧啶并[4,5-b]吲哚，9H-吡啶并[4' 3'：4,5]吡咯并[2,3-d]吡啶和9 H-1,3,6,9-四氮杂芴化合物，其特别地抑制检测点激酶1（CHK1）激酶功能。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。

    BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE
    7.
    发明申请
    BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE 有权
    双氰胺 - 氨基化合物及其用途

    公开(公告)号：US20100331328A1

    公开(公告)日：2010-12-30

    申请号：US12918266

    申请日：2009-02-19

    申请人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/497 ,  A61P35/00 ,  C12N5/00 ,  C07D241/26 ,  A61K31/4965 ,  C07D413/12

    CPC分类号： C07D471/04

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation:

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些双环芳基 - 芳基胺化合物（本文称为BCAA化合物），其特别地抑制检测点激酶1（CHK1）激酶功能 。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射：

    Bicyclylaryl-aryl-amine compounds and their use
    8.
    发明授权
    Bicyclylaryl-aryl-amine compounds and their use 有权
    双环芳基 - 芳基胺化合物及其用途

    公开(公告)号：US08530468B2

    公开(公告)日：2013-09-10

    申请号：US12918266

    申请日：2009-02-19

    申请人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    发明人： Ian Collins ,  John Charles Reader ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Michael Cherry

    IPC分类号： A61K31/497 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

    CPC分类号： C07D471/04

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation:

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些双环芳基 - 芳基胺化合物（本文称为BCAA化合物），其特别地抑制检测点激酶1（CHK1）激酶功能 。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即 通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射：

    Purine and deazapurine derivatives as pharmaceutical compounds
    10.
    发明授权
    Purine and deazapurine derivatives as pharmaceutical compounds 有权

    公开(公告)号：US08796293B2

    公开(公告)日：2014-08-05

    申请号：US12298462

    申请日：2007-04-25

    申请人： Thomas Glanmor Davies ,  Michelle Dawn Garrett ,  Robert George Boyle ,  Ian Collins

    发明人： Thomas Glanmor Davies ,  Michelle Dawn Garrett ,  Robert George Boyle ,  Ian Collins

    IPC分类号： A61K31/519 ,  A61K31/44 ,  C07D471/04 ,  C07D473/34

    CPC分类号： C07D471/04 ,  C07D473/34 ,  C07D487/04

    摘要： The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.