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    TARGETED DRUG DELIVERY VIA MIXED PHOSPHATE DERIVATIVES
    31.
    发明申请
    TARGETED DRUG DELIVERY VIA MIXED PHOSPHATE DERIVATIVES 审中-公开
    目标药物通过混合磷酸盐衍生物递送

    公开(公告)号：WO1992017185A1

    公开(公告)日：1992-10-15

    申请号：PCT/US1992002239

    申请日：1992-03-27

    Applicant: UNIVERSITY OF FLORIDA ,  BODOR, Nicholas, S.

    Inventor： UNIVERSITY OF FLORIDA

    IPC: A61K31/70

    CPC classification number: C07H19/10 ,  A61K47/54 ,  C07F9/091 ,  C07F9/094 ,  C07F9/5532 ,  C07F9/5535 ,  C07F9/5537 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/5765 ,  C07F9/59 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/65068 ,  C07F9/650952 ,  C07F9/6512 ,  C07F9/6547 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65611 ,  C07F9/65613 ,  C07F9/65616 ,  C07H19/04 ,  C07H19/20 ,  C07J51/00 ,  C07J63/008 ,  C07J71/0031

    Abstract: The invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the (a) moiety; R1 is C1-C8 alkyl, C6-C10 aryl or C7-C12 aralkyl, with the proviso that when [D] is the residue of a drug having a reactive hydroxyl functional group, said functional group being attached directly to the phosphorus atom of the (a) moiety via an oxygen-phosphorus bond, then R1, taken together with the adjacent oxygen atom, can also be the residue of a drug having a reactive hydroxyl functional group, said functional group being attached directly to the phosphorus atom of the (b) moiety via an oxygen-phosphorus bond, -OR1 being the same as or different from [D]; R2 is hydrogen, C1-C8 alkyl, C6-C10 aryl, C4-C9 heteroaryl, C3-C7 cycloalkyl, C3-C7 cycloheteroalkyl or C7-C12 aralkyl; and R3 is selected from the group consisting of C1-C8 alkyl; C2-C8 alkenyl having one or two double bonds; (C3-C7 cycloalkyl)-CrH2r- wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C1-C4 alkyl substituents on the ring portion; (C6-C10 aryloxy)C1-C8 alkyl; 2-, 3- or 4-pyridyl; and phenyl-CrH2r- wherein r is zero, one, two or three and phenyl is unsubstituted, or is substituted by 1 to 3 alkyl each having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2 to 8 carbon atoms or alkanoylamino having 2 to 6 carbon atoms. The compounds are adapted for targeted drug delivery, especially to the brain.

    Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中[D]是具有反应性官能团的药物的残基，所述官能团直接或通过桥接基团经由氧 - 磷 与（a）部分的磷原子键合; R1是C1-C8烷基，C6-C10芳基或C7-C12芳烷基，条件是当[D]是具有反应性羟基官能团的药物的残基时，所述官能团直接连接到 （a）部分通过氧 - 磷键，则R1与相邻的氧原子一起也可以是具有反应性羟基官能团的药物的残基，所述官能团直接连接到（ b）通过氧 - 磷键的部分，-OR1与[D]相同或不同; R2是氢，C1-C8烷基，C6-C10芳基，C4-C9杂芳基，C3-C7环烷基，C3-C7环杂烷基或C7-C12芳烷基; 并且R 3选自C 1 -C 8烷基; 具有一个或两个双键的C 2 -C 8烯基; （C 3 -C 7环烷基）-Cr H 2r-，其中r是0,1,2或3，环烷基部分是未取代的或在环部分带有1或2个C 1 -C 4烷基取代基; （C 6 -C 10芳氧基）C 1 -C 8烷基; 2-，3-或4-吡啶基; 和苯基-CrH 2r-，其中r为0,1,2或3，苯基未取代，或被1至3个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，卤素，三氟甲基， 2至8个碳原子或具有2至6个碳原子的烷酰基氨基。 这些化合物适用于靶向药物递送，特别适用于大脑。

    SURFACE MODIFIED SURGICAL INSTRUMENTS, DEVICES, IMPLANTS, CONTACT LENSES AND THE LIKE
    34.
    发明申请
    SURFACE MODIFIED SURGICAL INSTRUMENTS, DEVICES, IMPLANTS, CONTACT LENSES AND THE LIKE 审中-公开
    表面修饰手术仪器，器械，植入物，接触镜和类似物

    公开(公告)号：WO1992005697A1

    公开(公告)日：1992-04-16

    申请号：PCT/US1991006733

    申请日：1991-09-20

    Applicant: UNIVERSITY OF FLORIDA

    Inventor： UNIVERSITY OF FLORIDA ,  GOLDBERG, Eugene, P. ,  YAHIAOUI, Ali

    IPC: A01N01/02

    CPC classification number: A61F2/0077 ,  A61F2/14 ,  A61F2/1664 ,  A61F2002/009 ,  A61L2400/18 ,  A61L2430/16 ,  Y10S623/92 ,  Y10T428/3179 ,  Y10T428/31794 ,  Y10T428/31797

    Abstract: An improved method for modifying the plastic surfaces of articles adapted for contacting living tissue by the gamma or electron beam irradiation induced chemical graft coating thereon of a monomer comprising N-vinylpyrrolidone, 2-hydroxyethylmethacrylate or a mixture of the two to form a hydrophilic graft polymer coating, the improvement comprising pre-soaking the ocular implant material in a monomer or a solution comprising a monomer prior to conducting the gamma- or electron beam-irradiation induced graft polymerization in a second solution of a monomer.

    Abstract translation: 一种用于改变适于通过γ或电子束照射使生物体组织接触的制品的塑料表面的改进方法，其中包含N-乙烯基吡咯烷酮，甲基丙烯酸2-羟乙酯或其混合物的单体以形成亲水性接枝聚合物 改进包括在将单体或包含单体的溶液预先浸入眼睛植入材料中，然后在单体的第二溶液中进行γ-电子束或电子束照射诱导的接枝聚合。

    AUTOMATED METHOD FOR DIGITAL IMAGE QUANTITATION
    36.
    发明申请
    AUTOMATED METHOD FOR DIGITAL IMAGE QUANTITATION 审中-公开
    用于数字图像量化的自动化方法

    公开(公告)号：WO1991019457A1

    公开(公告)日：1991-12-26

    申请号：PCT/US1991004120

    申请日：1991-06-11

    Applicant: UNIVERSITY OF FLORIDA ,  GEISER, Edward, A. ,  WILSON, David, C. ,  GIBBY, Gordon, L.

    Inventor： UNIVERSITY OF FLORIDA

    IPC: A61B08/00

    CPC classification number: G01S7/52036

    Abstract: A method for quantitatively analyzing digital images of approximately elliptical body organs, and in particular, echocardiographic images. The invention automatically determines the center-point of an elliptical organ and search region for border discrimination by finding the maximum value produced by a series of circular arc filters applied to the image data. The positions of the organ border (10, 11, 12, 13) are then approximated by generating histograms along each of a number of circular segments (1, 2, 3, 4, 5, 6, 7, 8) based on the center-point. The approximated borders are then compared on a best-fit basis to a set of paired elliptical arcs used to model the borders. The image may then be displayed with the modeled border superimposed on the image. A flattened interventricular septum and signal loss across the septum are also determined for echocardiographic images. Cross-correlation is used on histograms generated for selected sectors of image data frames taken at different times to detect organ wall motion in each of the different sectors.

    Abstract translation: 一种用于定量分析近似椭圆体器官的数字图像的方法，特别是超声心动图像。 本发明通过找到应用于图像数据的一系列圆弧滤波器产生的最大值，自动确定用于边界识别的椭圆器官和搜索区域的中心点。 然后通过基于中心的多个圆形段（1,2,3,4,5,6,7,8）中的每一个生成直方图来逼近器官边界（10,11,12,13）的位置 -点。 然后将近似边界以最佳拟合为基础与用于对边界建模的成对椭圆弧进行比较。 然后，图像可以与叠加在图像上的模拟边界一起显示。 超声心动图也确定了隔膜间隔平缓和信号损失。 对于在不同时间拍摄的图像数据帧的选定扇区生成的直方图使用互相关来检测每个不同扇区中的器官壁运动。

    MONOCLONAL ANTIBODY FOR USE IN DETECTION AND TREATMENT OF CHILDHOOD LEUKEMIA
    38.
    发明申请
    MONOCLONAL ANTIBODY FOR USE IN DETECTION AND TREATMENT OF CHILDHOOD LEUKEMIA 审中-公开
    用于检测和治疗儿童白血病的单克隆抗体

    公开(公告)号：WO1990010692A1

    公开(公告)日：1990-09-20

    申请号：PCT/US1990001392

    申请日：1990-03-14

    Applicant: UNIVERSITY OF FLORIDA

    Inventor： UNIVERSITY OF FLORIDA ,  CASSANO, William, F.

    IPC: C12N05/20

    CPC classification number: A61K35/28 ,  A61K38/00 ,  A61K47/6867 ,  C07K16/3061 ,  G01N33/57426

    Abstract: The subject invention pertains to a novel cell line and the monoclonal antibody produced by the cell line. Advantageously, the novel monoclonal antibody binds specifically with the acute lymphocytic leukemia antigen. Thus, this antibody can be used in the detection of childhood leukemia as well as in therapeutic procedures such as bone marrow purging. The novel monoclonal antibody can also be used to construct hybrid toxin proteins which can selectively seek out and eliminate target cells.

    Abstract translation: 本发明涉及新细胞系和由细胞系产生的单克隆抗体。 有利地，新型单克隆抗体与急性淋巴细胞白血病抗原特异性结合。 因此，该抗体可用于检测儿童期白血病以及治疗过程如骨髓清除。 新型单克隆抗体也可用于构建可以选择性寻找和消除靶细胞的杂合毒素蛋白质。

    COMPOSITION AND METHOD FOR ENHANCING PERMEABILITY OF TOPICAL DRUGS
    39.
    发明申请
    COMPOSITION AND METHOD FOR ENHANCING PERMEABILITY OF TOPICAL DRUGS 审中-公开
    用于增强局部药物渗透性的组合物和方法

    公开(公告)号：WO1990003163A1

    公开(公告)日：1990-04-05

    申请号：PCT/US1989003677

    申请日：1989-08-29

    Applicant: UNIVERSITY OF FLORIDA

    Inventor： UNIVERSITY OF FLORIDA ,  BODOR, Nicholas, S. ,  LOFTSSON, Thorsteinn

    IPC: A61K09/06

    CPC classification number: A61K47/12 ,  A61K47/186

    Abstract: A composition and method for enhancing permeability of topical drugs wherein the agent which enhances the permeability of the drug is selected from the group consisting of (1) a choline ester having the formula: [CH3(CH2)n-COOCH2CH2N+(CH3)3]X- or [CH¿3?(CH2)mCH=CH(CH2)n-COOCH2CH2N?+(CH¿3)3]X-, wherein m and n are integers in the range of from 0 to 30 and X- is a pharmaceutically acceptable anion and (2) a mixture of the choline ester and an acid having the formula: CH¿3?(CH2)n-COOH or CH3(CH2)mCH=CH(CH2)n-COOH or a pharmaceutically acceptable salt thereof.

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