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104 条记录 (耗时 0.049 秒)

    Carbamate caspase inhibitors and uses thereof
    31.
    发明授权
    Carbamate caspase inhibitors and uses thereof 失效
    氨基甲酸酯半胱天冬酶抑制剂及其用途

    公开(公告)号：US06689784B2

    公开(公告)日：2004-02-10

    申请号：US09821161

    申请日：2001-03-29

    申请人： David Bebbington ,  Ronald Knegtel ,  Michael Mortimore ,  David Kay ,  Julian M. C. Golec

    发明人： David Bebbington ,  Ronald Knegtel ,  Michael Mortimore ,  David Kay ,  Julian M. C. Golec

    IPC分类号： C07D20982

    CPC分类号： C07D403/12 ,  C07D209/08 ,  C07D209/86 ,  C07D221/12 ,  C07D223/26 ,  C07D223/28 ,  C07D279/30

    摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.

    摘要翻译： 本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R 1是氢，-CHN 2，R 1，CH 2 OR，CH 2 SR或-CH 2 Y; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4和R 5与中间的氮一起形成杂环，R如说明书中所述。 这些化合物是凋亡和IL-1β分泌的有效抑制剂。

    Hybrid refractive/diffractive achromatic lens for optical data storage systems
    33.
    发明授权
    Hybrid refractive/diffractive achromatic lens for optical data storage systems 失效
    用于光学数据存储系统的混合折射/衍射消色差透镜

    公开(公告)号：US5349471A

    公开(公告)日：1994-09-20

    申请号：US17712

    申请日：1993-02-16

    申请人： G. Michael Morris ,  David Kay ,  Dale Buralli ,  David Kubalak

    发明人： G. Michael Morris ,  David Kay ,  Dale Buralli ,  David Kubalak

    IPC分类号： G02B5/18 ,  G02B27/00 ,  G11B7/135 ,  G02B3/08 ,  G02B27/44

    CPC分类号： G02B5/1895 ,  G02B27/0037 ,  G02B27/4238 ,  G02B5/1876 ,  G11B7/1374 ,  G11B2007/13722

    摘要： A diffractive/refractive hybrid lens for use in an optical data storage system as an objective is provided by a convex-plano singlet having a refractive element defined by plano-convex surfaces and a diffractive element defined by a Fresnel zone-like pattern on the plano surface which together provide the total power of the lens. The refractive lens is made of a high index, high dispersion glass so that the curvature and thickness of the refractive lens is minimized while providing a large numerical aperture (at least 0.45) at the expense of increased longitudinal chromatic aberration, which are compensated by the diffractive element and without the need for one or more additional curved surfaces as in low index biaspheric glass objective lenses for chromatic and mono-chromatic aberration reduction, which increases the thickness and curvatures of the lens. The invention enables longitudinal chromatic aberration to be corrected for at least a 10 nm band width around a center wavelength over a 20 nm range, as results when different lasers are used and as laser power varies during optical data storage on an optical data storage device (an optical disk). The thin, light weight low curvature achromat has maximum tolerance for various possible manufacturing errors such as decentering, variations in thickness of the lens, tilt and focal length especially for on-axis field of view less than 2.degree. while providing a very high quality spot (Strehl ratio of at least 0.9.).

    摘要翻译： 用作光学数据存储系统作为目的的衍射/折射混合透镜由具有由平凸表面限定的折射元件和由平面上的菲涅耳带状图案限定的衍射元件的凸平面单重晶片提供 一起提供透镜的总功率的表面。 折射透镜由高折射率高分散玻璃制成，使得折射透镜的曲率和厚度最小化，同时以增加的纵向色差为代价提供大的数值孔径（至少为0.45），其由 并且不需要一个或多个附加的弯曲表面，如在用于彩色和单色像差降低的低折射率偏置玻璃物镜中，这增加了透镜的厚度和曲率。 本发明使得能够在20nm范围内围绕中心波长的至少10nm带宽校正纵向色差，这是因为当使用不同的激光器并且在​​光学数据存储装置中的光学数据存储期间激光功率变化时的结果 光盘）。 薄的，重量轻的低曲率消色差对于各种可能的制造误差具有最大公差，例如偏心，透镜厚度变化，倾斜和焦距，特别是对于小于2°的轴上视场，同时提供非常高的质量点 （Strehl比至少为0.9）。

    Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
    35.
    发明授权
    Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors 失效
    制备可用作蛋白激酶抑制剂的嘧啶衍生物的方法

    公开(公告)号：US08637666B2

    公开(公告)日：2014-01-28

    申请号：US13424736

    申请日：2012-03-20

    申请人： Jean-Damien Charrier ,  Steven Durrant ,  David Kay

    发明人： Jean-Damien Charrier ,  Steven Durrant ,  David Kay

    IPC分类号： C07D487/12

    CPC分类号： C07D487/14

    摘要： A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).

    摘要翻译： 制备由结构式（I）表示的化合物或其药学上可接受的盐的方法，其中结构式（I）的变量如说明书和权利要求书中所述，包括以下步骤：a）使代表的化合物 通过结构式A：在合适的还原环化条件下，形成由结构式B表示的化合物：其中R10是LG1或-X1R1，-LG1是合适的离去基团; 和b）任选地，当结构式（B）的R 10是LG 1时，还包括用-X1R1替代结构式（B）的-LG1以形成由结构式（I）表示的化合物的步骤。

    Gate Valve
    37.
    发明申请
    Gate Valve 有权
    闸阀

    公开(公告)号：US20120085957A1

    公开(公告)日：2012-04-12

    申请号：US12900682

    申请日：2010-10-08

    申请人： Samir Dhawan ,  Jason Neal Whaley ,  David Kay ,  Randall Ferrain Weaver ,  Neil Colin Kennedy

    发明人： Samir Dhawan ,  Jason Neal Whaley ,  David Kay ,  Randall Ferrain Weaver ,  Neil Colin Kennedy

    IPC分类号： F16K3/00

    CPC分类号： F16K3/0236 ,  F16K3/0209 ,  F16K3/20

    摘要： A gate valve comprises a valve body having an internal working fluid passage and an internal gate chamber extending transverse to the working fluid passage. In addition, the gate valve comprises a gate disposed in the internal gate chamber and movable within the gate chamber between a closed position obstructing fluid flow through the working fluid passage and an open position allowing fluid flow through the working fluid passage. Further, the gate valve comprises an internal sealing arrangement coaxially disposed in the working fluid passage and extending between the valve body and the gate to form a barrier between the internal working fluid passage and the gate chamber. The internal sealing arrangement includes a frustoconical metal sealing surface adapted to sealingly engage an opposed mating frustoconical metal sealing surface on the valve body to form a first tapered metal-to-metal seal between the sealing arrangement and the valve body.

    摘要翻译： 闸阀包括具有内部工作流体通道的阀体和横向于工作流体通道延伸的内部门室。 此外，闸阀包括设置在内部门室中的门，并且可在门室内在阻塞流过工作流体通道的流体的关闭位置和允许流体流过工作流体通道的打开位置之间移动。 此外，闸阀包括同轴地设置在工作流体通道中并在阀体和门之间延伸的内部密封装置，以在内部工作流体通道和门室之间形成阻挡层。 内部密封装置包括截头圆锥形金属密封表面，其适于密封地接合阀体上相对的配合截头圆锥形金属密封表面，以在密封装置和阀体之间形成第一锥形金属对金属密封。

    Tetrahydropteridines useful as inhibitors of protein kinases
    39.
    发明授权
    Tetrahydropteridines useful as inhibitors of protein kinases 失效
    可用作蛋白激酶抑制剂的四氢喋啶

    公开(公告)号：US07763629B2

    公开(公告)日：2010-07-27

    申请号：US11786578

    申请日：2007-04-12

    申请人： Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

    发明人： Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

    IPC分类号： A61K31/505

    CPC分类号： C07D487/14

    摘要： The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

    摘要翻译： 本发明涉及可用作结构式（I）表示的蛋白激酶抑制剂的化合物：其中结构式（I）中的变量如本文所述。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。

    COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
    40.
    发明申请
    COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 失效
    化合物作为蛋白激酶抑制剂有用

    公开(公告)号：US20100099686A1

    公开(公告)日：2010-04-22

    申请号：US12448258

    申请日：2007-12-14

    申请人： Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

    发明人： Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

    IPC分类号： A61K31/4985 ,  C07D487/12 ,  C12N9/99 ,  A61P35/00

    CPC分类号： C07D475/00

    摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

    摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。