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1. 发明授权

US08841462B2 Bicyclic heterocycles as MEK kinase inhibitors 有权
标题翻译：双环杂环作为MEK激酶抑制剂
公开(公告)号：US08841462B2
公开(公告)日：2014-09-23
申请号：US12999003
申请日：2009-07-01
申请人： Robert A. Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
发明人： Robert A. Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
IPC分类号： C07D275/04 , C07D231/56 , C07D513/04 , C07D471/04 , A61K31/437 , A61K31/428 , A61K31/416
CPC分类号： C07D231/56 , C07D275/04 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

2. 发明申请

US20110190257A1 BICYCLIC HETEROCYCLES AS MEK KINASE INHIBITORS 有权
标题翻译：双相异构体作为MEK激酶抑制剂
公开(公告)号：US20110190257A1
公开(公告)日：2011-08-04
申请号：US12999003
申请日：2009-07-01
申请人： Robert Andrew Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
发明人： Robert Andrew Heald , Philip Jackson , Joseph P. Lyssikatos , Stephen Price , Pascal Pierre Alexandre Savy
IPC分类号： A61K31/397 , C07D471/02 , C07D231/56 , C07D277/62 , C07D275/06 , A61K31/437 , A61K31/416 , A61K31/428 , A61P35/00
CPC分类号： C07D231/56 , C07D275/04 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

3. 发明授权

US08492427B2 Isoindolones derivatives as MEK kinase inhibitors and methods of use 失效
标题翻译：异吲哚酮衍生物作为MEK激酶抑制剂和使用方法
公开(公告)号：US08492427B2
公开(公告)日：2013-07-23
申请号：US12998000
申请日：2009-07-01
申请人： Emanuela Gancia , Robert Andrew Heald , Philip Jackson , Stephen Price
发明人： Emanuela Gancia , Robert Andrew Heald , Philip Jackson , Stephen Price
IPC分类号： A61K31/437 , A61K31/4035 , A61K31/416 , A61K31/4985 , C07D231/54 , C07D241/00 , C07D221/00 , C07D209/44
CPC分类号： C07D209/46
摘要： The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的具有式（I）的异吲哚酮，更具体地涉及MEK激酶抑制活性。本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

4. 发明申请

US20110124622A1 ISOINDOLONES DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE 失效
标题翻译： ISOINDOLONES衍生物作为MEK激酶抑制剂和使用方法
公开(公告)号：US20110124622A1
公开(公告)日：2011-05-26
申请号：US12998000
申请日：2009-07-01
申请人： Emanuela Gancia , Robert Andrew Heald , Philip Jackson , Stephen Price
发明人： Emanuela Gancia , Robert Andrew Heald , Philip Jackson , Stephen Price
IPC分类号： A61K31/4035 , C07D209/46 , C07D405/10 , C07D471/04 , C07D487/04 , C07D209/96 , C07D413/10 , A61K31/437 , A61K31/4985 , A61K31/4245 , A61P35/00 , A61P29/00
CPC分类号： C07D209/46
摘要： The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的具有式（I）的异吲哚酮，更具体地涉及MEK激酶抑制活性。本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

5. 发明授权

US07915300B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US07915300B2
公开(公告)日：2011-03-29
申请号：US10584930
申请日：2005-01-06
申请人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
发明人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
IPC分类号： A61K31/407 , A61K31/34 , C07D487/04 , C07D307/00
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：式II的化合物，其中R 1和R 2中的一个是卤素，另一个是H或卤素; R3是C1-C4直链或支链，任选氟化的烷基; R4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O）取代的，单环或双环的碳环或杂环; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

6. 发明申请

US20050144178A1 Distributing files across multiple, permissibly heterogeneous, storage devices 审中-公开
标题翻译：在多个可允许的异构存储设备之间分发文件
公开(公告)号：US20050144178A1
公开(公告)日：2005-06-30
申请号：US10832808
申请日：2004-04-27
申请人： David Chrin , Philip Jackson , Steven Orszag
发明人： David Chrin , Philip Jackson , Steven Orszag
IPC分类号： G06F17/30 , H04L12/24
CPC分类号： G06F16/10 , Y10S707/99953
摘要： A file system (i) permits storage capacity to be added easily, (ii) can be expanded beyond a given unit, (iii) is easy to administer and manage, (iv) permits data sharing, and (v) is able to perform effectively with very large storage capacity and client loads. State information from a newly added unit is communicated (e.g., automatically and transparently) to central administration and management operations. Configuration and control information from such operations is communicated (e.g., automatically) back down to the newly added units, as well as existing units. In this way, a file system can span both local storage devices (like disk drives) and networked computational devices transparently to clients. Such state and configuration and control information can include globally managed segments as the building blocks of the file system, and a fixed mapping of globally unique file identifiers (e.g., Inode numbers) and/or ranges thereof, to such segments.
摘要翻译：文件系统（i）允许容易地添加存储容量，（ii）可以扩展到给定单元之外，（iii）易于管理和管理，（iv）允许数据共享，以及（v）能够执行有效地具有非常大的存储容量和客户端负载。来自新添加的单元的状态信息被传达（例如，自动和透明地）到中央管理和管理操作。来自这些操作的配置和控制信息被传送（例如，自动地）回到新添加的单元以及现有单元。以这种方式，文件系统可以跨越本地存储设备（如磁盘驱动器）和联网计算设备透明地覆盖客户端。这种状态和配置和控制信息可以包括作为文件系统的构建块的全局管理的段，以及全球唯一的文件标识符（例如，Inode号）和/或其范围的固定映射到这些段。

7. 发明授权

US5393418A Water intake, in particular for industrial installations 失效
标题翻译：取水量，特别是工业设施
公开(公告)号：US5393418A
公开(公告)日：1995-02-28
申请号：US912713
申请日：1992-07-13
申请人： Philip Jackson
发明人： Philip Jackson
IPC分类号： E03B3/36 , E02B8/02 , E02B9/04 , E03B5/00 , F04D29/60 , B01D35/02
CPC分类号： E02B9/04 , E02B8/026 , F04D29/605 , Y02E10/22
摘要： A water intake comprises a common frame and assembled thereto and-forming therewith an integral self-contained unit a pump adapted to be immersed and a trash rake and an associated grid on the suction side of the pump and/or a filter on the discharge side of the pump.
摘要翻译：进水口包括共同的框架并组装在其上并与其形成一体的独立单元，适于被浸入的泵，以及在泵的吸入侧上的垃圾耙和相关栅格和/或排出侧的过滤器的泵。

8. 外观设计

USD312330S Mouthpiece for resuscitation 失效
公开(公告)号：USD312330S
公开(公告)日：1990-11-20
申请号：US117142
申请日：1987-11-04
申请人： Philip Jackson
设计人： Philip Jackson

9. 发明授权

US4889629A Filter panel with parallel passages and mechanical filter screen comprising same 失效
标题翻译：具有平行通道的过滤面板和包括该通道的机械过滤网
公开(公告)号：US4889629A
公开(公告)日：1989-12-26
申请号：US143528
申请日：1988-01-13
申请人： Philip Jackson
发明人： Philip Jackson
IPC分类号： E02B5/08 , B01D29/00 , B01D33/00 , B01D39/10
CPC分类号： B01D39/10 , B01D33/327 , B01D2201/62
摘要： A filter panel comprises a plurality of substantially coplanar openings. It incorporates a two-dimensional array of parallel elongate passages. Each passage delimits a respective one of the openings. The array is substantially coplanar with the openings and the passages are substantially perpendicular to the array. Each opening is convergent from an interior profile both from the inlet and outlet side of the panel.
摘要翻译：过滤器面板包括多个基本上共面的开口。它包含平行细长通道的二维阵列。每个通道限定相应的一个开口。阵列基本上与开口共面，并且通道基本上垂直于阵列。每个开口从面板的入口侧和出口侧的内部轮廓收敛。

10. 发明授权

US4814076A Self-cleaning filter for insertion into a pressurized pipe 失效
标题翻译：用于插入加压管道的自清洁过滤器
公开(公告)号：US4814076A
公开(公告)日：1989-03-21
申请号：US143634
申请日：1988-01-13
申请人： Philip Jackson
发明人： Philip Jackson
IPC分类号： B01D35/02 , B01D29/01 , B01D33/00 , B01D35/16 , B01D46/04
CPC分类号： B01D33/15
摘要： A filter that can be inserted into a pressurized pipe comprises a filter body designed to be connected to each of two consecutive section of the pipe. Inside the filter body is a generally circular filter member which is rotatable about an axis of the filter body, into which it projects cantilever-fashion. A rim on the filter member carries a rack meshing with a drive wheel. A suction unit on the upstream side of the filter member and disposed along a radius of the filter member is connected to a take-off pipe.
摘要翻译：可以插入加压管道的过滤器包括设计成连接到管道的两个连续部分中的每一个的过滤器主体。过滤器本体内部是大致圆形的过滤器构件，其可以围绕过滤体的轴线旋转，其中悬臂方式突出。过滤器构件上的边缘带有与驱动轮啮合的齿条。在过滤构件的上游侧并沿着过滤构件的半径设置的抽吸单元连接到排出管。

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