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1. 发明授权

US08288425B2 Benzimidazoles 有权
标题翻译：苯并咪唑
公开(公告)号：US08288425B2
公开(公告)日：2012-10-16
申请号：US11029064
申请日：2005-01-04
申请人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
发明人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
IPC分类号： A61K31/4184 , C07D235/18
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

2. 发明授权

US06897208B2 Benzimidazoles 有权
标题翻译：苯并咪唑
公开(公告)号：US06897208B2
公开(公告)日：2005-05-24
申请号：US10279834
申请日：2002-10-24
申请人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
发明人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D521/00 , A61K31/33 , A61K31/415 , C07D231/00 , C07D235/00 , C07D487/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

3. 发明申请

US20060014756A1 Benzimidazoles 有权
标题翻译：苯并咪唑
公开(公告)号：US20060014756A1
公开(公告)日：2006-01-19
申请号：US11029064
申请日：2005-01-04
申请人： Michael Edwards , Paul Cox , Shelley Amendola , Stephanie Deprets , Timothy Gillespy , Christopher Edlin , Andrew Morley , Charles Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir Majid , John Reader , Lloyd Payne , Nawaz Khan , Michael Cherry
发明人： Michael Edwards , Paul Cox , Shelley Amendola , Stephanie Deprets , Timothy Gillespy , Christopher Edlin , Andrew Morley , Charles Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir Majid , John Reader , Lloyd Payne , Nawaz Khan , Michael Cherry
IPC分类号： A61K31/496 , A61K31/4184 , C07D43/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

4. 发明授权

US08367658B2 Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine compounds and their use 有权
标题翻译：吡嗪-2-基 - 吡啶-2-基胺和吡嗪-2-基 - 嘧啶-4-基胺化合物及其用途
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。

5. 发明申请

US20100311730A1 Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine Compounds and Their Use 有权
标题翻译：吡嗪-2-基 - 吡啶-2-基胺和吡嗪-2-基 - 嘧啶-4-基胺化合物及其用途
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。

6. 发明申请

US20100298301A1 OXAZOLE TYROSINE KINASE INHIBITORS 有权
标题翻译：奥昔洛霉激酶激酶抑制剂
公开(公告)号：US20100298301A1
公开(公告)日：2010-11-25
申请号：US12599653
申请日：2008-05-09
申请人： John Charles Reader , John Mark Ellard , Helen Boffey , Susanne Taylor , Andrew David Carr , Michael Cherry , Michelle Wilson , Richard Boakye Owoare
发明人： John Charles Reader , John Mark Ellard , Helen Boffey , Susanne Taylor , Andrew David Carr , Michael Cherry , Michelle Wilson , Richard Boakye Owoare
IPC分类号： A61K31/551 , C07D233/64 , C07D401/04 , C07D403/04 , C07D409/04 , C07D263/32 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D243/10 , C07D221/22 , A61K31/417 , A61K31/4439 , A61K31/421 , A61K31/5377 , A61K31/497 , A61K31/454 , A61K31/439 , A61P35/00 , A61P43/00
CPC分类号： C07D413/14 , C07D233/90 , C07D263/34 , C07D263/48 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/10 , C07D413/12 , C07D451/02 , C07D451/04 , C07D453/02 , C07D471/04
摘要： The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
摘要翻译：本发明提供了一种化合物，它是式（1）的酰胺或其盐，溶剂合物，N-氧化物或其互变异构体; 其中：a为0或1; b为0或1，条件是a和b之和为0或1; T是O或NH Ar1是含有至多4个选自O，N和S的杂原子的单环或双环5至10元芳基或杂芳基，并且任选被一个或多个取代基R 1取代; Ar2是含有至多4个选自O，N和S的杂原子并且任选被一个或多个取代基R 2取代的单环或双环5-至10-元芳基或杂芳基; 并且R 1和R 2如权利要求中所定义。化合物是激酶抑制剂，特别是FLT3，FLT4和Aurora激酶。

7. 发明申请

US20050176733A1 Chk-1 inhibitors 审中-公开
标题翻译： Chk-1抑制剂
公开(公告)号：US20050176733A1
公开(公告)日：2005-08-11
申请号：US11031544
申请日：2005-01-07
申请人： Robert Boyle , Hassan Imogai , Michael Cherry , Nawaz Khan
发明人： Robert Boyle , Hassan Imogai , Michael Cherry , Nawaz Khan
IPC分类号： C07D213/75 , C07D213/82 , C07D213/85 , C07D241/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/497 , A61K31/444 , C07D41/02 , C07D43/02
CPC分类号： C07D213/75 , C07D213/82 , C07D213/85 , C07D241/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： This invention provides compounds and methods for treating cancer. More particularly, the invention provides compounds that inhibit Chk-1. These compounds potentiate the action of DNA-damaging agents such as chemotherapy and radiation therapy.
摘要翻译：本发明提供了治疗癌症的化合物和方法。更具体地，本发明提供抑制Chk-1的化合物。这些化合物增强DNA损伤剂如化学疗法和放射治疗的作用。

8. 发明申请

US20050108688A1 Method and system for assigning and publishing applications 有权
标题翻译：用于分配和发布应用程序的方法和系统
公开(公告)号：US20050108688A1
公开(公告)日：2005-05-19
申请号：US11010499
申请日：2004-12-13
申请人： Mark Lucovsky , Michael Cherry , Daniel Plastina , Bharat Shah , Debi Mishra , David Kays , Markus Horstmann
发明人： Mark Lucovsky , Michael Cherry , Daniel Plastina , Bharat Shah , Debi Mishra , David Kays , Markus Horstmann
IPC分类号： G06F9/44 , G06F9/445
CPC分类号： G06F8/61
摘要： A method and system for managing and deploying applications across a computer network by assigning and publishing applications to user and computer policy recipients. Assigned applications are automatically applied via a script to the policy recipients, thereby ensuring that the recipient has an administrator-specified workstation configuration. Assigned applications are advertised so as to appear available to the user, by adding an application shortcut to the start menu, and by populating the machine registry with appropriate application information. Other applications may be published to users, whereby those applications are optionally available for use by users. Published application information is maintained in a centralized store of information on the network. Assigned and published applications may be installed on demand, such as when the application is activated.
摘要翻译：一种用于通过向用户和计算机策略接收者分配和发布应用程序来跨计算机网络管理和部署应用程序的方法和系统。分配的应用程序将通过脚本自动应用于策略收件人，从而确保收件人具有管理员指定的工作站配置。通过向开始菜单添加应用程序快捷方式，并通过使用适当的应用程序信息填充机器注册表，分配的应用程序将通告给用户。其他应用可以被发布给用户，由此这些应用可选地可供用户使用。发布的应用信息被维护在网络上的信息的集中存储中。分配和发布的应用程序可以按需安装，例如应用程序激活时。

9. 发明授权

US08530468B2 Bicyclylaryl-aryl-amine compounds and their use 有权
标题翻译：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：

10. 发明申请

US20100210639A1 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
标题翻译： 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。

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