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：US08324226B2

公开(公告)日：2012-12-04

申请号：US12738808

申请日：2008-10-23

申请人： Ian Collins ,  John Jamieson Caldwell ,  Antony William Oliver ,  Tony Michael Raynham ,  Emma Jane Welsh ,  Cornelius Albertus Johannes Matijssen

发明人： Ian Collins ,  John Jamieson Caldwell ,  Antony William Oliver ,  Tony Michael Raynham ,  Emma Jane Welsh ,  Cornelius Albertus Johannes Matijssen

IPC分类号： A01N43/54 ,  A61K31/517

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) 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 CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 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，更具体地涉及本文所述的某些氧苯基芳基化合物（本文称为OPA化合物），其特别地抑制了检测点激酶2（CHK2）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CHK2激酶功能，以及用于治疗由CHK2介导的疾病和病症，即 通过抑制CHK2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：US20110125980A1

公开(公告)日：2011-05-26

申请号：US13016996

申请日：2011-01-29

申请人： Jeffrey Brunet ,  Ian Collins ,  Yousuf Chowdhary ,  Eric Li ,  Alex Lemelev

发明人： Jeffrey Brunet ,  Ian Collins ,  Yousuf Chowdhary ,  Eric Li ,  Alex Lemelev

IPC分类号： G06F12/16

CPC分类号： G06F3/0605 ,  G06F3/0632 ,  G06F3/065 ,  G06F3/0676 ,  G06F3/0677 ,  G06F3/0679 ,  G06F11/1451 ,  G06F11/1456 ,  G06F11/1461

摘要： A data backup system is provided for backing up data files from a data source and for securing those data files against accidental modification or deletion. The system comprises storage and a data protection component that includes an application programming interface defining a command set. The system can also comprise a backup application that is configured to use the commands of the command set. The data protection component allows applications that use the commands of the command set, such as the backup application, to access the storage of the system. The data protection component prevents operating systems and applications that do not use the commands of the command set from accessing the storage. The data protection function of the data protection component can optionally be disabled to allow open access to the storage.

摘要翻译： 提供数据备份系统，用于从数据源备份数据文件，并保护这些数据文件免受意外修改或删除。 该系统包括存储和数据保护组件，其包括定义命令集的应用程序编程接口。 系统还可以包括配置为使用命令集的命令的备份应用程序。 数据保护组件允许使用命令集的命令（如备份应用程序）访问系统存储的应用程序。 数据保护组件防止不使用命令集命令的操作系统和应用程序访问存储。 可以选择禁用数据保护组件的数据保护功能，以允许对存储器的打开访问。

公开(公告)号：US07818160B2

公开(公告)日：2010-10-19

申请号：US11506386

申请日：2006-08-18

申请人： Ian Collins ,  Eric Li ,  Yousuf Chowdhary ,  Jeffrey Brunet

发明人： Ian Collins ,  Eric Li ,  Yousuf Chowdhary ,  Jeffrey Brunet

IPC分类号： G06F9/455 ,  G06F9/00 ,  G06F13/12

CPC分类号： G06F3/065 ,  G06F3/0605 ,  G06F3/0632 ,  G06F3/0676 ,  G06F3/0677 ,  G06F3/0679 ,  G06F11/1451 ,  G06F11/1456 ,  G06F11/1461

摘要： A data backup system comprises an emulation component and a storage device having logical storage areas. The emulation component is configured to represent a first logical storage area of the storage device, such as a solid state memory or a disk drive partition, as if it were an auto-launch device. Accordingly, a data source, such as a personal computer, will interact with the first logical storage area as if it were the auto-launch device. As some operating systems are configured to recognize auto-launch devices upon connection and automatically execute applications stored thereon, merely connecting the data backup system to a data source running such an operating system can cause a backup application stored by the first logical storage area to automatically execute on the data source to selectively back up data to a second logical storage area of the storage device.

摘要翻译： 数据备份系统包括具有逻辑存储区域的仿真部件和存储装置。 仿真部件被配置为表示诸如固态存储器或磁盘驱动器分区之类的存储设备的第一逻辑存储区域，如同它是自动发射设备。 因此，诸如个人计算机的数据源将与第一逻辑存储区域交互，如同它是自动发射设备。 由于一些操作系统被配置为在连接时识别自动发射设备并且自动执行存储在其上的应用，仅将数据备份系统连接到运行这样的操作系统的数据源可以使由第一逻辑存储区域存储的备份应用自动地 在数据源上执行选择性地将数据备份到存储设备的第二逻辑存储区域。

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。

公开(公告)号：US20100169560A1

公开(公告)日：2010-07-01

申请号：US12723635

申请日：2010-03-13

申请人： Jeffrey Brunet ,  Yousuf Chowdhary ,  Ian Collins ,  Eric Li

发明人： Jeffrey Brunet ,  Yousuf Chowdhary ,  Ian Collins ,  Eric Li

IPC分类号： G06F12/00 ,  G06F12/02 ,  G06F12/16

CPC分类号： G06F11/1451 ,  G06F3/0605 ,  G06F3/0632 ,  G06F3/065 ,  G06F3/0676 ,  G06F3/0677 ,  G06F3/0679 ,  G06F11/1456 ,  G06F11/1461 ,  G06F11/1464

摘要： A data backup system comprises a USB flash drive that includes an emulation component and a flash memory. The emulation component is configured to represent the flash memory as if it were an auto-launch device. Accordingly, a data source, such as a personal computer, will interact with the flash memory as if it were the auto-launch device. As some operating systems are configured to recognize auto-launch devices upon connection and automatically execute applications stored thereon, merely connecting the USB flash drive to a data source running such an operating system will cause a backup application stored by the flash memory to automatically execute on the data source. Here, the backup application is configured to selectively back up data files from the data source to a networked storage such as a server of a commercial service provider.

摘要翻译： 数据备份系统包括包括仿真部件和闪存的USB闪存驱动器。 仿真组件配置为将闪存表示为自动启动设备。 因此，诸如个人计算机的数据源将与闪存相互作用，就像它是自动发射设备一样。 由于一些操作系统被配置为在连接时识别自动启动设备并且自动执行存储在其上的应用，仅将USB闪存驱动器连接到运行这样的操作系统的数据源将导致由闪存存储的备份应用程序自动执行 数据源。 这里，备份应用被配置为选择性地将数据文件从数据源备份到诸如商业服务提供商的服务器的联网存储器。

公开(公告)号：US07696322B2

公开(公告)日：2010-04-13

申请号：US10900928

申请日：2004-07-28

申请人： Gregory T. Bleck ,  Dona York ,  Ian Collins

发明人： Gregory T. Bleck ,  Dona York ,  Ian Collins

IPC分类号： C12P21/08 ,  C07K16/00 ,  A61K39/395 ,  C12P21/04 ,  C07H21/04

CPC分类号： G01N33/53 ,  A61K2039/505 ,  C07K16/00 ,  C07K2317/31 ,  C07K2319/00

摘要： The present invention provides novel antibodies. In particular, the present invention provides fusion antibodies comprising antibody heavy and light chain fusions. The present invention further provides multivalent antibodies comprising multiple fusion antibody chains. The present invention further provides methods of generating splice resistant antibody genes.

摘要翻译： 本发明提供新型抗体。 特别地，本发明提供了包含抗体重链和轻链融合物的融合抗体。 本发明还提供了包含多个融合抗体链的多价抗体。 本发明还提供了产生抗拼接抗体基因的方法。

公开(公告)号：US20090253718A1

公开(公告)日：2009-10-08

申请号：US12298117

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： A61K31/522 ,  A61K31/52 ,  A61P35/04 ,  A61P35/00 ,  A61K31/519

CPC分类号： C07D473/34 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04

摘要： The invention provides a compound having 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); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4 alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents 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.

摘要翻译： 本发明提供具有式（I）的化合物或其盐，溶剂化物，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（R6） A是在R 1和NR 2 R 3之间延伸的最大链长度为5个原子并且在E和NR 2 R 3之间延伸的4个原子的最大链长度的任选取代的饱和C 1-7烃连接基团，连接基团中的一个碳原子是任选的 用氧或氮代替; E是单环或双环碳环或杂环基或非环基X-G，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链，其中一个碳原子任选被O，S或NH取代; R1是氢或芳基或杂芳基; R2和R3各自为氢，任选取代的C 1-4烃基或任选取代的C 1-4酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR2R3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代; 或NR2R3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 并且R 4，R 5，R 6，R 7和R 8各自独立地选自氢和权利要求中定义的各种取代基，其中所述化合物用于：（a）治疗或预防其中调节 表示ROCK激酶或蛋白激酶p70S6K的抑制作用） 和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。

公开(公告)号：US20090247538A1

公开(公告)日：2009-10-01

申请号：US11577963

申请日：2005-10-25

申请人： 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

发明人： 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分类号： A61K31/52 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519 ,  C12N9/99 ,  C12Q1/48

CPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  C07D473/34 ,  C07D487/04

摘要： 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, NR2R, 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.

摘要翻译： 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（R6） 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，NR2R，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。

公开(公告)号：US20090184940A1

公开(公告)日：2009-07-23

申请号：US12397121

申请日：2009-03-03

申请人： Christopher J. Silk ,  David T.E. Ely ,  Andrew M. Errington ,  Ian Collins ,  Geoffrey Foote ,  Julian Haines ,  Robert Bolender ,  Gareth J. McCaughan

发明人： Christopher J. Silk ,  David T.E. Ely ,  Andrew M. Errington ,  Ian Collins ,  Geoffrey Foote ,  Julian Haines ,  Robert Bolender ,  Gareth J. McCaughan

IPC分类号： G06F3/041

CPC分类号： G06F3/046 ,  G06F1/3203 ,  G06F1/3262 ,  G06F3/03545 ,  G06F3/03547 ,  G06F2203/0339

摘要： A low-cost x-y digitizing system for use in consumer electronic devices, such as portable digital assistants, mobile telephones, web browsers and the like. The digitizer includes a resonant stylus, an excitation winding for energizing the resonant stylus and a set of sensor windings for sensing the signal generated by the stylus, from which the x-y position of the stylus is determined. A novel stylus design is described together with novel digitizer windings and novel excitation and processing circuitry.

摘要翻译： 用于消费电子设备（例如便携式数字助理，移动电话，网络浏览器等）的低成本x-y数字化系统。 该数字转换器包括一个共振触控笔，一个用于激励谐振触控笔的激励绕组和一组用于感测由触笔产生的信号的传感器绕组，由此确定触笔的x-y位置。 新颖的触控笔设计与新型数字转换器绕组和新颖的激励和处理电路一起描述。