公开(公告)号：US20160304493A1

公开(公告)日：2016-10-20

申请号：US15191967

申请日：2016-06-24

Applicant: Cancer Research Technology Limited

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

IPC: C07D401/14 ,  C07D401/12 ,  A61K45/06 ,  A61K31/497 ,  A61K9/00

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.

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。

公开(公告)号：US09403797B2

公开(公告)日：2016-08-02

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

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。

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。

公开(公告)号：US09765059B2

公开(公告)日：2017-09-19

申请号：US15191967

申请日：2016-06-24

Applicant: Cancer Research Technology Limited

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

IPC: A61K31/497 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06 ,  A61N5/10 ,  A61K9/00

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.

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。