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    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation
    1.
    发明申请
    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation 失效
    基于嘧啶的非核苷酸组合物和抑制血小板聚集的方法

    公开(公告)号：US20060258614A1

    公开(公告)日：2006-11-16

    申请号：US11413600

    申请日：2006-04-28

    申请人： James Douglass ,  Paul Watson ,  Sammy Shaver ,  Krzysztof Bednarski

    发明人： James Douglass ,  Paul Watson ,  Sammy Shaver ,  Krzysztof Bednarski

    IPC分类号： A61K31/7072 ,  A61K31/513 ,  C07H19/12 ,  C07D405/02

    CPC分类号： C07D493/04 ,  C07D405/04 ,  C07H19/12

    摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide pyrimidine-based compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae I and Ia-Ic, or tautomers, salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and Ia-Ic.

    摘要翻译： 本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。 该方法还涉及治疗血栓形成或相关病症的方法。 该方法包括向受试者施用包含有效量的非核苷酸嘧啶类化合物，优选P2Y 12受体拮抗剂化合物的药物组合物，其中所述量有效抑制血小板聚集。 可用于本发明的化合物包括通式I和Ia-Ic的化合物，或其互变异构体，盐，水合物和溶剂合物。 本发明还提供式I和Ia-1c的新型化合物。

    P2Y6 receptor agonists for treating lung diseases
    3.
    发明申请
    P2Y6 receptor agonists for treating lung diseases 有权
    用于治疗肺部疾病的P2Y6受体激动剂

    公开(公告)号：US20070015726A1

    公开(公告)日：2007-01-18

    申请号：US11478338

    申请日：2006-06-28

    申请人： Jose Boyer ,  Sammy Shaver ,  James Douglass ,  Catherine Redick

    发明人： Jose Boyer ,  Sammy Shaver ,  James Douglass ,  Catherine Redick

    IPC分类号： A61K31/7072 ,  A61K31/7076

    CPC分类号： A61K31/7072 ,  A61K31/708 ,  A61K31/7084

    摘要： This invention is directed to a method of enhancing or facilitating the clearance of the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5′-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof.

    摘要翻译： 本发明涉及增强或促进受试者中肺粘液分泌物清除的方法。 本发明还涉及促进受试者中肺粘液分泌物水合的方法。 本发明进一步涉及预防或治疗与人或其他哺乳动物的肺或气道功能受损有关的疾病或病症的方法。 该方法包括向受试者施用包含治疗有效量的P2Y 6受体激动剂化合物的药物组合物，其中所述量有效激活管腔上的P2Y 6受体 肺上皮表面。 可用于本发明的P2Y 6受体激动剂化合物包括单核苷5'-二磷酸酯，二核苷单磷酸酯，二核苷二磷酸酯或通式I的二核苷三磷酸盐，或其盐，溶剂合物，水合物。

    Drug-eluting stents coated with P2Y12 receptor antagonist compound
    5.
    发明申请
    Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
    药物洗脱支架涂有P2Y12受体拮抗剂化合物

    公开(公告)号：US20060122143A1

    公开(公告)日：2006-06-08

    申请号：US11267834

    申请日：2005-11-04

    申请人： Jose Boyer ,  James Douglass ,  Sammy Shaver

    发明人： Jose Boyer ,  James Douglass ,  Sammy Shaver

    IPC分类号： A61K31/7076 ,  A61K31/7072 ,  C07H19/04 ,  A61K31/675

    CPC分类号： C07H19/04 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207 ,  C07H21/00

    摘要： The present invention provides a P2Y12 receptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

    摘要翻译： 本发明提供P2Y 12受体拮抗剂化合物洗脱支架，其中支架涂覆有一种或多种P2Y 12受体拮抗剂化合物或其药学上可接受的盐，溶剂化物， 或其水合物。 当支架置于狭窄或损伤的动脉血管中时，治疗有效量的P2Y 12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y 12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

    Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound
    6.
    发明申请
    Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound 失效
    涂有非核苷酸P2Y12受体拮抗剂化合物的药物洗脱支架

    公开(公告)号：US20060121086A1

    公开(公告)日：2006-06-08

    申请号：US11267941

    申请日：2005-11-04

    申请人： Jose Boyer ,  James Douglass ,  Sammy Shaver

    发明人： Jose Boyer ,  James Douglass ,  Sammy Shaver

    IPC分类号： A61K31/519 ,  A61K31/52 ,  A61F2/00

    CPC分类号： A61K31/519 ,  A61F2/82 ,  A61F2250/0067 ,  A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61K31/727 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides a drug-eluting stent, wherein the stent is coated with one or more non-mucleotide P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

    摘要翻译： 本发明提供药物洗脱支架，其中支架涂覆有一种或多种非核苷酸P2Y 12受体拮抗剂化合物或其药学上可接受的盐，溶剂合物或水合物。 当支架置于狭窄或损伤的动脉血管中时，治疗有效量的P2Y 12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y 12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

    Orally bioavailable compounds and methods for inhibiting platelet aggregation
    7.
    发明申请
    Orally bioavailable compounds and methods for inhibiting platelet aggregation 失效
    口服生物可利用的化合物和抑制血小板聚集的方法

    公开(公告)号：US20070093446A1

    公开(公告)日：2007-04-26

    申请号：US11595837

    申请日：2006-11-09

    申请人： James Douglass ,  Paul Watson ,  Carl Samuelson ,  Christopher Crean

    发明人： James Douglass ,  Paul Watson ,  Carl Samuelson ,  Christopher Crean

    IPC分类号： A61K31/7076 ,  A61K31/52 ,  C07H19/16 ,  C07D473/02

    CPC分类号： A61K31/519 ,  A61F2250/0067 ,  A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61K31/727 ,  A61K45/06 ,  C07H19/16 ,  A61K2300/00

    摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae III, IIIa, and IIIb, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae IIIa and IIIb, which are potent and have a good oral bioavailability.

    摘要翻译： 本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。 该方法还涉及治疗血栓形成或相关病症的方法。 该方法包括向受试者施用包含有效量的非核苷酸化合物，优选P2Y 12受体拮抗剂化合物的药物组合物，其中所述量有效抑制血小板聚集。 可用于本发明的化合物包括通式III，IIIa和IIIb的化合物，或其盐，水合物和溶剂化物。 本发明还提供新的式IIIa和IIIb化合物，它们是有效的并且具有良好的口服生物利用度。

    Method and apparatus for automated image analysis of biological specimens
    9.
    发明申请
    Method and apparatus for automated image analysis of biological specimens 有权
    生物标本自动图像分析的方法和装置

    公开(公告)号：US20070053569A1

    公开(公告)日：2007-03-08

    申请号：US11594374

    申请日：2006-11-07

    申请人： James Douglass ,  Thomas Riding ,  James Ring

    发明人： James Douglass ,  Thomas Riding ,  James Ring

    IPC分类号： G06K9/00

    CPC分类号： G01N1/312 ,  G01N15/1468 ,  G01N15/1475 ,  G01N2015/1472 ,  G01N2015/1488 ,  G01N2015/1497 ,  G02B21/244 ,  G02B21/367 ,  G06K9/00127 ,  G06K9/00134 ,  G06T7/60

    摘要： A method and apparatus for automated cell analysis of biological specimens automatically scans at a low magnification to acquire images which are analyzed to determine candidate cell objects of interest. The low magnification images are converted from a first color space to a second color space. The color space converted image is then low pass filtered and compared to a threshold to remove artifacts and background objects from the candidate object of interest pixels of the color converted image. The candidate object of interest pixels are morphologically processed to group candidate object of interest pixels together into groups which are compared to blob parameters to identify candidate objects of interest which correspond to cells or other structures relevant to medical diagnosis of the biological specimen. The location coordinates of the objects of interest are stored and additional images of the candidate cell objects are acquired at high magnification. The high magnification images are analyzed in the same manner as the low magnification images to confirm the candidate objects of interest which are objects of interest. A high magnification image of each confirmed object of interest is stored for later review and evaluation by a pathologist.

    摘要翻译： 用于生物标本的自动细胞分析的方法和装置以低倍率自动扫描以获取被分析以确定感兴趣的候选细胞对象的图像。 低倍率图像从第一颜色空间转换为第二颜色空间。 然后将色彩空间转换的图像进行低通滤波，并将其与阈值进行比较，以从彩色转换图像的候选对象像素中去除伪影和背景对象。 候选对象像素被形态地处理以将候选对象对象像素组合成为与斑点参数进行比较的组，以识别对应于与生物样本的医学诊断相关的细胞或其他结构的候选对象。 存储感兴趣对象的位置坐标，并以高倍率获取候选单元对象的附加图像。 以与低倍率图像相同的方式分析高倍率图像，以确认作为感兴趣对象的感兴趣的候选对象。 存储每个确认的感兴趣对象的高放大图像以供病理学家进行后续检查和评估。