公开(公告)号：US20120065202A1

公开(公告)日：2012-03-15

申请号：US13256345

申请日：2010-03-12

申请人： Rosemary Lynch ,  Andrew David Cansfield ,  Helen Sarah Niblock ,  Daniel Hardy ,  Jane Elizabeth Scanlon ,  Rita Adrego ,  Nigel Ramsden

发明人： Rosemary Lynch ,  Andrew David Cansfield ,  Helen Sarah Niblock ,  Daniel Hardy ,  Jane Elizabeth Scanlon ,  Rita Adrego ,  Nigel Ramsden

IPC分类号： A61K31/5377 ,  A61P37/00 ,  A61P29/00 ,  A61P25/28 ,  A61P37/06 ,  A61P35/00 ,  A61P9/00 ,  A61P3/00 ,  C07D487/04 ,  A61P37/08

CPC分类号： C07D413/04 ,  A61K31/5377 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to compounds of formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

摘要翻译： 本发明涉及式（I）化合物，其中X，R 1，R 2，T，m，n，o具有在说明书和权利要求书中引用的含义。 所述化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。 本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

公开(公告)号：US20120040967A1

公开(公告)日：2012-02-16

申请号：US13241887

申请日：2011-09-23

申请人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

发明人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

IPC分类号： A61K31/506 ,  C07D413/14 ,  C12N9/99 ,  A61K31/55 ,  A61K31/497 ,  A61P35/00 ,  C07D401/14 ,  A61K31/5377

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine 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，更具体地涉及某些联芳基胺化合物（本文称为BAA化合物），特别是某些吡嗪-2-基 - 吡啶-2-基 - 胺和吡嗪-2-基 - 嘧啶-4-基 - 胺化合物，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。

公开(公告)号：US20140179664A1

公开(公告)日：2014-06-26

申请号：US14234662

申请日：2012-07-24

申请人： Jay Freeman ,  Valerie Reader ,  Glynn Addison ,  Nigel Ramsden ,  Jane Elizabeth Scanlon ,  Richard John Harrison

发明人： Jay Freeman ,  Valerie Reader ,  Glynn Addison ,  Nigel Ramsden ,  Jane Elizabeth Scanlon ,  Richard John Harrison

IPC分类号： C07D491/107 ,  C07D403/14 ,  C07D413/14 ,  C07D403/12

CPC分类号： C07D491/107 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D491/10

摘要： The present invention relates to compounds of formula (I) wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

摘要翻译： 本发明涉及其中X1至X5，Z1至Z3，Y0，RY1，RY2和R具有在说明书和权利要求书中引用的含义的式（I）化合物。 所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。 本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

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：

公开(公告)号：US08058045B2

公开(公告)日：2011-11-15

申请号：US12680891

申请日：2008-10-06

申请人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

发明人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

IPC分类号： A61P35/00 ,  A61K31/55 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/497 ,  C07D401/14 ,  C07D413/14 ,  C12N9/99 ,  C12N5/02

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), 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) ionisiπq radiation, wherein: —X═ is independently —CRA5═ or —N═; and the rest of the substituents are as specified in the claims.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些联芳基胺化合物（本文称为BAA化合物），特别是某些吡嗪-2-基 - 吡啶-2-基 - 胺和吡嗪-2-基 （I）的嘧啶-4-基 - 胺化合物，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，其中：-X =独立地是-CRA5 =或-N =; 并且其余的取代基如权利要求中所述。

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：

公开(公告)号：US08785457B2

公开(公告)日：2014-07-22

申请号：US13256345

申请日：2010-03-12

申请人： Rosemary Lynch ,  Andrew David Cansfield ,  Helen Sarah Niblock ,  Daniel Hardy ,  Jane Elizabeth Scanlon ,  Rita Adrego ,  Nigel Ramsden

发明人： Rosemary Lynch ,  Andrew David Cansfield ,  Helen Sarah Niblock ,  Daniel Hardy ,  Jane Elizabeth Scanlon ,  Rita Adrego ,  Nigel Ramsden

IPC分类号： A61K31/5377 ,  C07D413/04

CPC分类号： C07D413/04 ,  A61K31/5377 ,  C07D471/04 ,  C07D487/04

摘要： The invention relates to compounds of formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. The compounds of formula (I) are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

摘要翻译： 本发明涉及式（I）化合物，其中X，R 1，R 2，T，m，n，o具有在说明书和权利要求书中引用的含义。 式（I）化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。 本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

公开(公告)号：US20140163023A1

公开(公告)日：2014-06-12

申请号：US14009846

申请日：2012-04-02

申请人： Rosemary Lynch ,  Andrew David Cansfield ,  Daniel Paul Hardy ,  Jane Elizabeth Scanlon ,  Rita Joana Rodrigues Adrego

发明人： Rosemary Lynch ,  Andrew David Cansfield ,  Daniel Paul Hardy ,  Jane Elizabeth Scanlon ,  Rita Joana Rodrigues Adrego

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The invention relates to compounds of formula (I) wherein X, R1, R2, T0, o have the meaning as cited in the description and the claims. The compounds of formula I are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds of formula I, the preparation of such compounds as well as the use as medicaments.

摘要翻译： 本发明涉及式（I）的化合物，其中X，R1，R2，T0，o具有在说明书和权利要求书中引用的含义。 式I的化合物可用作mTOR的抑制剂，用于治疗或预防mTOR相关疾病和病症。 本发明还涉及包含式I化合物，这些化合物的制备以及用作药物的药物组合物。

公开(公告)号：US08367658B2

公开(公告)日：2013-02-05

申请号：US13241887

申请日：2011-09-23

申请人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

发明人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

IPC分类号： A61K31/55 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/506

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine 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，更具体地涉及某些联芳基胺化合物（本文称为BAA化合物），特别是某些吡嗪-2-基 - 吡啶-2-基 - 胺和吡嗪-2-基 - 嘧啶-4-基 - 胺化合物，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。

公开(公告)号：US20100311730A1

公开(公告)日：2010-12-09

申请号：US12680891

申请日：2008-10-06

申请人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

发明人： Ian Collins ,  John Charles Reader ,  Thomas Peter Matthews ,  Kwai Ming Cheung ,  Nicolas Proisy ,  David Hugh Williams ,  Sukhbinder Singh Klair ,  Jane Elizabeth Scanlon ,  Nelly Piton ,  Glynn Jonathan Addison ,  Michael Cherry

IPC分类号： A61K31/55 ,  C07D401/14 ,  A61K31/506 ,  A61P35/00 ,  C12N9/99 ,  C12N5/02 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/497

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), 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) ionisiπq radiation. wherein: —X═ is independently —CRA5═ or —N═; and the rest of the substituents are as specified in the claims.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些联芳基胺化合物（本文称为BAA化合物），特别是某些吡嗪-2-基 - 吡啶-2-基 - 胺和吡嗪-2-基 （I）的嘧啶-4-基 - 胺化合物，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。 其中：-X =独立地为-CRA5 =或-N =; 并且其余的取代基如权利要求中所述。