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11 条记录 (耗时 0.027 秒)

    Prevention and treatment of cardiovascular pathologies
    1.
    发明申请
    Prevention and treatment of cardiovascular pathologies 审中-公开
    预防和治疗心血管病变

    公开(公告)号：US20060029986A1

    公开(公告)日：2006-02-09

    申请号：US11231256

    申请日：2005-09-20

    申请人： David Grainger ,  Paul Kemp

    发明人： David Grainger ,  Paul Kemp

    IPC分类号： G01N33/542 ,  G01N33/537

    CPC分类号： A61K9/0024 ,  A61K31/00 ,  A61K31/135 ,  A61K31/138 ,  A61K31/337 ,  A61K31/38 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/715 ,  A61K47/51 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6817 ,  A61K47/6831 ,  A61K47/6843 ,  A61K47/6927 ,  A61K47/6937 ,  A61K47/6957 ,  C07K14/71 ,  C07K16/22 ,  C07K2317/73 ,  G01N33/6893 ,  G01N33/74 ,  G01N2333/495 ,  G01N2800/32

    摘要： A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is 1, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro. Also provided is a therapeutic method comprising inhibiting smooth muscle cell proliferation associated with procedural vascular trauma employing the administration of tamoxifen or structural analogs thereof, including compounds of formula (I).

    摘要翻译： 一种治疗或预​​防心血管病变的方法，其通过给予式（I）化合物：其中Z为C-O或共价键; Y是H或O（C 1 -C 4）烷基，R 1和R 2各自独立地是（ C 1 -C 4烷基或与N一起为饱和杂环基，R 3是乙基或氯乙基，R 4 H或与R 3一起为-CH 2 - ， - CH 2 - 或-S-，R 5 是（O）（C 1 -C 4 - ）烷基或H，且R 6是1，O（C 1个C 1 -C 4烷基或H，条件是当R 4，R 5，R 5， 6是H，R 3不是乙基; 提供有效激活或刺激TGF-β的产生以治疗和/或预防诸如动脉粥样硬化，血栓形成，心肌梗死和中风的病症的药学上可接受的盐或其药学上可接受的盐。 有用的化合物包括异昔芬及其盐。 还提供了鉴定作为TGF-β激活剂或生产刺激剂的化合物的方法。 本发明的另一个实施方案是用于在体外测定TGF-β的测定或试剂盒。 还提供了一种治疗方法，其包括使用给予他莫昔芬或其结构类似物（包括式（I）的化合物）来抑制与程序性血管创伤相关的平滑肌细胞增殖。

    Hydroxyl functional surface coating
    3.
    发明申请
    Hydroxyl functional surface coating 失效
    羟基官能表面涂层

    公开(公告)号：US20050147758A1

    公开(公告)日：2005-07-07

    申请号：US11035849

    申请日：2005-01-13

    申请人： Guoqiang Mao ,  Steven Metzger ,  Michael Lochhead ,  David Goldberg ,  Charles Greef ,  David Grainger

    发明人： Guoqiang Mao ,  Steven Metzger ,  Michael Lochhead ,  David Goldberg ,  Charles Greef ,  David Grainger

    IPC分类号： G01N33/53 ,  G01N33/543 ,  G01N35/00 ,  B05D3/02

    CPC分类号： G01N33/54393 ,  A61L27/34 ,  A61L29/085 ,  A61L31/10 ,  G01N33/5306 ,  G01N2035/00158

    摘要： Compositions and methods of preparing functional thin films or surface coatings with low non-specific binding are described. The thin films contain specified functional groups and non-specific binding repellant components. The thin films are either covalently bound to or passively adsorbed to various solid substrates. The specified functional group provides specified activity for the thin film modified solid surfaces and non-specific binding repellant components significantly reduce the non-specific binding to the thin film modified solid surfaces. Non-specific binding repellant components do not affect specified functional group's activity in the thin films. In these methods, specified functional groups are anchored to the solid substrates through a spacer. Surface coatings are also described having both non-specific protein binding properties combined with functional groups for specific binding activity thereby providing surface coating that specifically recognize target proteins but limit binding to non-specific protein.

    摘要翻译： 描述了制备具有低非特异性结合的功能性薄膜或表面涂层的组合物和方法。 薄膜含有特定的官能团和非特异性结合驱避剂组分。 薄膜共价结合或被动地吸附到各种固体基质上。 指定的官能团为薄膜改性的固体表面和非特异性结合驱除剂组分提供了特定的活性，显着降低了与薄膜改性固体表面的非特异性结合。 非特异性结合驱避剂组分不影响薄膜中指定的官能团活性。 在这些方法中，指定的官能团通过间隔基团固定在固体基质上。 还描述了表面涂层具有与特异性结合活性的官能团结合的非特异性蛋白质结合特性，从而提供特异性识别靶蛋白但限制与非特异性蛋白结合的表面涂层。

    SWIMMING AID
    5.
    发明申请
    SWIMMING AID 审中-公开
    游泳援助

    公开(公告)号：US20130052894A1

    公开(公告)日：2013-02-28

    申请号：US13498123

    申请日：2010-09-23

    申请人： David Grainger ,  Gurmail Singh Sidhu

    发明人： David Grainger ,  Gurmail Singh Sidhu

    IPC分类号： A63B31/10 ,  A63B31/00

    CPC分类号： A63B31/10 ,  A63B31/14

    摘要： A swimming aid is provided that includes an expandable element and a securing element for securing the swimming aid to a user. The expandable element moves between a collapsed configuration and an expanded configuration. The swimming aid is constructed and arranged such that movement through water in a first direction causes the expandable element to move to the expanded configuration and movement in a second direction, substantially opposite to the first direction, causes the expandable element to move to the collapsed configuration.

    摘要翻译： 提供了一种游泳辅助装置，其包括可膨胀元件和用于将游泳辅助件固定到使用者的固定元件。 可扩展元件在折叠配置和扩展配置之间移动。 游泳辅助装置被构造和布置成使得在第一方向上通过水的运动使得可扩张元件移动到膨胀构型并且在与第一方向基本相反的第二方向上的移动使得可扩张元件移动到收缩构型 。

    Anti-Inflammatory Agents
    8.
    发明申请
    Anti-Inflammatory Agents 失效
    抗炎药

    公开(公告)号：US20080076755A1

    公开(公告)日：2008-03-27

    申请号：US11573851

    申请日：2005-08-10

    申请人： David Grainger ,  David Fox

    发明人： David Grainger ,  David Fox

    IPC分类号： A61K31/439 ,  A61K31/55 ,  A61P11/06 ,  A61P17/06 ,  A61P29/00 ,  A61P31/12 ,  A61P37/00 ,  C07D221/02 ,  C07D221/04 ,  C07D487/00 ,  C07D487/08

    CPC分类号： A61K31/55 ,  A61K31/439 ,  C07D451/14

    摘要： The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is —C —(Y)k—(R1)n or SO2—(Y)k (R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group.

    摘要翻译： 本发明提供了通式（I）化合物或其药学上可接受的盐的化合物，组合物和用途，用于制备旨在治疗炎性病症的药物，其中y为1至8的整数; z为1〜8的整数; 条件是y和z不能都等于1; X是-C - （Y） - （R 1）n - 或SO 2 - （Y） （R 1）N k为0或1; Y是环烷基或聚环烷基（例如金刚烷基，金刚烷甲基，双环辛基，环己基，环丙基）; 或Y是环烯基或多环烯基。

    Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
    9.
    发明申请
    Prevention and treatment of cardiovascular pathologies with tamoxifen analogues 审中-公开
    用他莫昔芬类似物预防和治疗心血管病变

    公开(公告)号：US20060135560A1

    公开(公告)日：2006-06-22

    申请号：US10729056

    申请日：2003-12-05

    申请人： David Grainger ,  James Metcalfe ,  Lawrence Kunz ,  Robert Schroff

    发明人： David Grainger ,  James Metcalfe ,  Lawrence Kunz ,  Robert Schroff

    IPC分类号： A61K31/445 ,  A61K31/40 ,  A61K31/138

    CPC分类号： A61K31/445 ,  A61K31/135 ,  A61K31/138 ,  A61K31/38 ,  A61K31/40 ,  G01N2800/32 ,  G01N2800/324 ,  Y10S514/866

    摘要： A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to elevate the level of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene, toremifene or salts thereof. Further provided is a method for identifying an agent that elevates the level of TGF-beta. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro. Also provided is a therapeutic method comprising inhibiting smooth muscle cell proliferation associated with procedural vascular trauma employing the administration of tamoxifin or structural analogs thereof, including compounds of formula (I).

    摘要翻译： 一种治疗或预​​防心血管病变的方法，其通过给予式（I）化合物：其中Z为C-O或共价键; Y是H或O（C 1 -C 4）烷基，R 1和R 2各自独立地是（ C 1 -C 4烷基或与N一起为饱和杂环基，R 3是乙基或氯乙基，R 4 H，R 5是I，O（C 1 -C 4 -C 4）烷基或H和R 6 是（O）（C 1 -C 4）烷基或H，条件是当R 4，R 0 > 5，且R 6为H，R 3不为乙基; 提供有效地提高TGF-β水平以治疗和/或预防诸如动脉粥样硬化，血栓形成，心肌梗塞和中风的病症的药学上可接受的盐或其药学上可接受的盐。 有用的化合物包括异昔芬，托瑞米芬或其盐。 还提供了用于鉴定提高TGF-β水平的试剂的方法。 本发明的另一个实施方案是用于在体外测定TGF-β的测定或试剂盒。 还提供了一种治疗方法，其包括使用给予他莫昔芬或其结构类似物（包括式（I）的化合物）来抑制与程序性血管创伤相关的平滑肌细胞增殖。