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    5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use
    4.
    发明授权
    5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use 有权
    5-（吡啶-2-基 - 氨基） - 吡嗪-2-腈化合物及其治疗用途

    公开(公告)号：US09040540B2

    公开(公告)日：2015-05-26

    申请号：US14356626

    申请日：2012-11-09

    Applicant: Cancer Research Technology Limited

    Inventor： Ian Collins ,  Michael Lainchbury ,  Thomas Peter Matthews ,  John Charles Reader

    IPC: A61K31/497 ,  C07D401/12 ,  C07D401/14

    CPC classification number: C07D401/14 ,  A61K9/0053 ,  A61K31/497 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D401/12

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, 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 thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及特别是抑制检测点激酶1（CHK1）激酶功能的某些吡啶基 - 氨基 - 吡嗪腈化合物。 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）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; 和（e）电离辐射。

    5-(Pyridin-2-yl-Amino)-Pyrazine-2-Carbonitrile Compounds and Their Therapeutic Use
    6.
    发明申请
    5-(Pyridin-2-yl-Amino)-Pyrazine-2-Carbonitrile Compounds and Their Therapeutic Use 有权
    5-（吡啶-2-基 - 氨基） - 吡嗪-2-腈化合物及其治疗用途

    公开(公告)号：US20140315925A1

    公开(公告)日：2014-10-23

    申请号：US14356626

    申请日：2012-11-09

    Applicant: Cancer Research Technology Limited

    Inventor： Ian Collins ,  Michael Lainchbury ,  Thomas Peter Matthews ,  John Charles Reader

    IPC: C07D401/12 ,  C07D401/14

    CPC classification number: C07D401/14 ,  A61K9/0053 ,  A61K31/497 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D401/12

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, 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 thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及特别是抑制检测点激酶1（CHK1）激酶功能的某些吡啶基 - 氨基 - 吡嗪腈化合物。 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）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; 和（e）电离辐射。

    Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors
    7.
    发明授权
    Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors 有权
    正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂

    公开(公告)号：US08809336B2

    公开(公告)日：2014-08-19

    申请号：US14017814

    申请日：2013-09-04

    Applicant: Astex Therapeutics Limited ,  The Institute of Cancer Research: Royal Cancer Hospital ,  Cancer Research Technology Limited

    Inventor： Valerio Berdini ,  Robert George Boyle ,  Gordon Saxty ,  David Winter Walker ,  Steven John Woodhead ,  Paul Graham Wyatt ,  Alastair Donald ,  John Caldwell ,  Ian Collins ,  Tatiana Faria Da Fonseca

    IPC: A61K31/497 ,  A61K31/52 ,  A61K31/519

    CPC classification number: C07D471/04 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  C07D473/34 ,  C07D487/04

    Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being 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 C1-4 alkylene 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 a 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, R3, R4, R6 and R8 are as defined in the claims.

    Abstract translation: 本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

    5-(Pyridin-2-yl-Amino)-Pyrazine-2-Carbonitrile Compounds and Their Therapeutic Use
    10.
    发明申请
    5-(Pyridin-2-yl-Amino)-Pyrazine-2-Carbonitrile Compounds and Their Therapeutic Use 有权
    5-（吡啶-2-基 - 氨基） - 吡嗪-2-腈化合物及其治疗用途

    公开(公告)号：US20150225372A1

    公开(公告)日：2015-08-13

    申请号：US14693307

    申请日：2015-04-22

    Applicant: Cancer Research Technology Limited

    Inventor： Ian Collins ,  Michael Lainchbury ,  Thomas Peter Matthews ,  John Charles Reader

    IPC: C07D401/14 ,  A61N5/10 ,  A61K45/06 ,  C07D401/12 ,  A61K31/497

    CPC classification number: C07D401/14 ,  A61K9/0053 ,  A61K31/497 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D401/12

    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, 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 thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    Abstract translation: 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及特别是抑制检测点激酶1（CHK1）激酶功能的某些吡啶基 - 氨基 - 吡嗪腈化合物。 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）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; 和（e）电离辐射。

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