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    Cyclic oxyguanidine pyrazinones as protease inhibitors
    1.
    发明申请
    Cyclic oxyguanidine pyrazinones as protease inhibitors 有权

    公开(公告)号：US20030073702A1

    公开(公告)日：2003-04-17

    申请号：US10263663

    申请日：2002-10-04

    申请人： 3-Dimensional Pharmaceuticals, Inc.

    发明人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    IPC分类号： A61K031/4965 ,  C07D241/02

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: 1 wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

    Conductive microtiter plate
    2.
    发明申请
    Conductive microtiter plate 审中-公开
    导电微量滴定板

    公开(公告)号：US20030064508A1

    公开(公告)日：2003-04-03

    申请号：US10247745

    申请日：2002-09-20

    申请人： 3-DIMENSIONAL PHARMACEUTICALS, INC.

    发明人： Joseph Kwasnoski ,  Ernel O. Simpson ,  Edmund Graf

    IPC分类号： C12M001/34

    CPC分类号： B01L3/50851 ,  B01L2300/04 ,  B01L2300/0829 ,  B01L2300/12 ,  B01L2300/1805

    摘要： The present invention is a multi-well vessel such as a microtiter plate, made from a plastic material formulated for increased thermal conductivity. In a preferred embodiment, the plastic material is a thermally conductive formulation of a cyclic polyolefin, syndiotactic polystyrene, polycarbonate, or liquid crystal polymer, with a melting point greater than 130null C. and exhibiting very low intrinsic fluorescent properties. A conductive medium, such as conductive carbon black, is included in the formulation of the plastic material at about 5% or greater by weight to increase thermal conductivity. To further increase thermal conductivity, a thermally conductive ceramic filler, such as a Boron Nitride filler, may be added to the formulation. A polymeric surfactant may also be added to the formulation for increased performance. The invention may also include a flat piece of conductive material attached to the flat bottom of the plate to impart conductivity and flatness to the part. Alternatively, the flat bottom surface of the plate may be metallized or coated with a flat layer of conductive material. The plate may also include a transparent lid, or cover, preferably made from polycarbonates, polypropylenes, or cyclic olefins or from multi-layer films made from two or more clear materials with desired barrier properties. Additionally, a fluorescent grade of polymer, such an epoxy prepared with a fluorescent die, can be embedded at a particular position on the plate to help indicate when the lights on the test equipment are in operation.

    摘要翻译： 本发明是一种多孔容器，例如由配制用于增加导热性的塑料制成的微量滴定板。 在优选的实施方案中，塑料材料是环状聚烯烃，间同立构聚苯乙烯，聚碳酸酯或液晶聚合物的导热配方，其熔点大于130℃，表现出非常低的固有荧光性能。 导电性介质，例如导电炭黑，以约5％或更高的重量包含在塑料材料的制剂中以增加导热性。 为了进一步提高导热性，可以向制剂中加入导热陶瓷填料，例如氮化硼填料。 还可以将聚合物表面活性剂加入制剂中以提高性能。 本发明还可以包括附接到板的平坦底部的平坦导电材料片，以赋予该部件的导电性和平坦度。 或者，板的平坦底表面可以金属化或涂覆有导电材料的平坦层。 板还可以包括透明盖或盖，优选由聚碳酸酯，聚丙烯或环烯烃制成，或者由具有所需阻隔性能的两种或更多种透明材料制成的多层膜制成。 此外，荧光级别的聚合物，例如用荧光管芯制备的环氧树脂可以嵌入板上的特定位置，以帮助指示测试设备上的灯是否在运行。

    Substituted indoles and their use as integrin antagonists
    3.
    发明申请
    Substituted indoles and their use as integrin antagonists 有权
    取代的吲哚及其作为整联蛋白拮抗剂的用途

    公开(公告)号：US20020169200A1

    公开(公告)日：2002-11-14

    申请号：US10058215

    申请日：2002-01-29

    申请人： 3-Dimensional Pharmaceuticals, Inc.

    发明人： Tianbao Lu ,  Louis V. LaFrance ,  Thomas P. Markotan ,  Juan Jose Marugan ,  Victor J. Marder ,  David C. U'Prichard ,  Beth M. Anaclerio ,  Zihong Guo ,  Wenxi Pan ,  Kristi A. Leonard

    IPC分类号： A61K031/405 ,  C07D209/04

    CPC分类号： C07D213/74 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/14

    摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (nullv) integrins, for example nullvnull3 and nullvnull5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by nullvnull3 and nullvnull5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: 1 where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.

    摘要翻译： 本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新型取代的吲哚化合物，例如阿尔法博3和阿尔法肽5整联蛋白，其药学上可接受的盐及其药物组合物。 这些化合物可以用于治疗由α1和α2融合蛋白介导的病理状态，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。 化合物具有以下通式：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，D，X，W，a，m，n， j，k和v在本文中定义。

    MICROTITER PLATE WITH INTEGRAL HEATER
    4.
    发明申请
    MICROTITER PLATE WITH INTEGRAL HEATER 有权
    带整体加热器的微型板

    公开(公告)号：US20020070208A1

    公开(公告)日：2002-06-13

    申请号：US10012560

    申请日：2001-12-12

    申请人： 3-Dimensional Pharmaceuticals, Inc.

    发明人： Joseph Kwasnoski ,  F. Raymond Salemme

    IPC分类号： H05B003/06

    CPC分类号： B01L3/50851 ,  Y10S435/809

    摘要： A microtiter plate system includes an integral heater. In an embodiment, the integral heater includes a heater plate. In another embodiment, the integral heater includes resistive heater wires positioned beneath and/or between the wells of a microtiter plate. In an embodiment, the microtiter plate system includes optically clear well bottoms that permit sensing and measurement of samples through the optically clear well bottoms. In an implementation, an optically clear heater is positioned beneath the optically clear well bottoms. In an alternative implementation, resistive heater wires are positioned between the wells. In an embodiment, the microtiter plate system includes a microtiter plate lid with an integral heater, which can be implemented using a heater plate, resistive wires, and the like. In an embodiment, the microtiter plate system includes an integral non-contact heater, such as a ferrous plate and/or ferrous particles, powder and/or fibers, which generate heat when subjected to an electromagnetic field. An electromagnetic field can be generated by an inductive coil or the like. In an embodiment, the microtiter plate system includes an integral non-contact heater which generates heat when subjected to microwave radiation from a microwave generator. In an embodiment, the microtiter plate system includes an integral thermostat that maintains a substantially constant temperature in the microtiter plate system.

    摘要翻译： 微量滴定板系统包括一体式加热器。 在一个实施例中，一体式加热器包括加热板。 在另一个实施例中，积分加热器包括位于微量滴定板的孔之下和/或之间的电阻加热丝。 在一个实施方案中，微量滴定板系统包括光学透明的井底，其允许通过光学透明的井底检测和测量样品。 在一个实施方案中，光学透明加热器位于光学透明井底下方。 在替代实施例中，电阻加热器线定位在井之间。 在一个实施方案中，微量滴定板系统包括具有整体加热器的微量滴定板盖，其可以使用加热板，电阻丝等实现。 在一个实施方案中，微量滴定板系统包括一体的非接触式加热器，例如铁质板和/或亚铁颗粒，粉末和/或纤维，其在经受电磁场时产生热量。 可以通过感应线圈等产生电磁场。 在一个实施方案中，微量滴定板系统包括一个整体的非接触式加热器，其在受到来自微波发生器的微波辐射时产生热量。 在一个实施方案中，微量滴定板系统包括在微量滴定板系统中保持基本恒定的温度的整体恒温器。

    N,N-disulfonylated aminobenzene carboxlic acids and the use thereof as thrombin inhibitors
    7.
    发明授权
    N,N-disulfonylated aminobenzene carboxlic acids and the use thereof as thrombin inhibitors 失效
    N，N-二磺酰化氨基苯羧酸及其作为凝血酶抑制剂的用途

    公开(公告)号：US5559150A

    公开(公告)日：1996-09-24

    申请号：US470578

    申请日：1995-06-06

    申请人： Richard M. Soll

    发明人： Richard M. Soll

    IPC分类号： C07C311/48 ,  A61K31/19 ,  C07C311/21 ,  C07C317/26 ,  C07D213/42

    CPC分类号： C07C311/48

    摘要： The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; and n is from zero to five. The compounds of the invention are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.

    摘要翻译： 本发明涉及非肽类凝血酶抑制剂的新型化合物。 该化合物具有以下结构：其中， 其中R1是烷基，取代的烷基，环烷基，芳基，取代的芳基，杂芳基或取代的杂芳基之一; n为0至5。 本发明的化合物可用于治疗动脉和静脉血栓闭塞障碍，炎症，癌症和神经变性疾病。