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68 条记录 (耗时 0.045 秒)

    N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
    51.
    发明授权
    N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists 失效
    N，N'-二取代胍及其作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5190976A

    公开(公告)日：1993-03-02

    申请号：US844498

    申请日：1992-03-02

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： C07D215/40 ,  A01N37/52 ,  A61K31/155 ,  A61K31/365 ,  A61K31/37 ,  A61K31/47 ,  A61P25/00 ,  A61P25/28 ,  C07C279/18 ,  C07D311/18

    CPC分类号： C07C279/18 ,  A61K31/155 ,  A61K31/365 ,  A61K31/47

    摘要： N,N'-disubstituted guanidines exhibiting a high binding affinity to phencyclidine (PCP) receptors are disclosed. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors or glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, brain or spinal cord ischemia, brain or spinal cord trauma, as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 公开了对苯环利定（PCP）受体表现出高结合亲和力的N，N'-二取代的胍。 这些N，N'-二取代的胍衍生物作为非竞争性抑制剂或通过NMDA受体产生的谷氨酸盐诱导的反应，作为NMDA受体 - 离子通道复合物的离子通道的阻断剂。 因此，这些化合物发挥神经保护性质，并且可用于治疗缺氧，脑或脊髓缺血，脑或脊髓创伤中的神经元丧失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化， 亨廷顿氏病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    Amplifier molecules for diagnosis and therapy derived from 3,5-bis[1-(3-amino-2,2-bis (aminomethyl)-propyl) oxymethyl] benzoic acid
    55.
    发明授权
    Amplifier molecules for diagnosis and therapy derived from 3,5-bis[1-(3-amino-2,2-bis (aminomethyl)-propyl) oxymethyl] benzoic acid 失效
    用于诊断和治疗的放大器分子衍生自3,5-双[1-（3-氨基-2,2-双（氨基甲基） - 丙基）氧甲基]苯甲酸

    公开(公告)号：US5252317A

    公开(公告)日：1993-10-12

    申请号：US887542

    申请日：1992-05-22

    申请人： John F. W. Keana

    发明人： John F. W. Keana

    IPC分类号： A61K49/18 ,  A61K49/20 ,  C07C291/04 ,  C12N9/96 ,  C07C69/80 ,  C07D207/38 ,  C07D209/48

    CPC分类号： A61K49/20 ,  A61K49/1812 ,  C07C291/04 ,  Y10S435/806 ,  Y10S436/803 ,  Y10T436/24

    摘要： Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.

    摘要翻译： 公开了放大器分子：具有分支结构的各种有机化合物，其末端具有可以化学连接药理活性基团的胺基团。 合成了许多MRI对比增强剂，每种都包含多个活性基团，如稳定的氮氧化物和三价金属阳离子的络合物。 使用具有不同支化结构的许多放大器成功地进行了这种合成，表明了合成具有各种药理学活性基团的放大器的相关化学物质的一般用途。 还合成放大器，其具有以化学反应性基团如异硫氰酸酯终止的接头，其使放大器具有双功能性：可附着于聚合物，生物大分子或具有多个反应性位点的其它生物相容性实体，例如末端胺。 通过这样的化学，放大器可附着于单体抗体，用于在体内所需位点浓集药理活性基团。

    Mannich base N-oxide drugs
    56.
    发明授权
    Mannich base N-oxide drugs 有权
    曼尼希碱N-氧化物药物

    公开(公告)号：US08410075B2

    公开(公告)日：2013-04-02

    申请号：US12563543

    申请日：2009-09-21

    申请人： John F. W. Keana ,  Paul Westberg ,  John Curd ,  Alshad S. Lalani

    发明人： John F. W. Keana ,  Paul Westberg ,  John Curd ,  Alshad S. Lalani

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07C291/04 ,  C07D405/04 ,  C07H19/06

    摘要： Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.

    摘要翻译： 公开了含有酸性N-H基团的药物的曼尼希碱N-氧化物。 还公开了包含治疗有效量的曼尼希碱N-氧化物或N-氧化物重排产物，其药学上可接受的盐或前药的药物组合物。 此外，公开了单独或与一种或多种其它活性剂或处理组合使用化合物的方法。

    Chemical functionalization of surfaces
    57.
    发明授权
    Chemical functionalization of surfaces 失效
    表面化学官能化

    公开(公告)号：US6022597A

    公开(公告)日：2000-02-08

    申请号：US966058

    申请日：1997-11-07

    申请人： Mingdi Yan ,  John F. W. Keana

    发明人： Mingdi Yan ,  John F. W. Keana

    IPC分类号： C08J5/06 ,  G03F7/008 ,  G03F7/16 ,  B05D3/06

    CPC分类号： C08J5/06 ,  G03F7/008 ,  G03F7/165 ,  C08J2321/00

    摘要： Methods for covalently modifying surfaces of various substrates are disclosed, along with various substrates having surfaces modified by such methods. Candidate surfaces include various polymeric, siliceous, metallic, allotrophic forms of carbon, and semiconductor surfaces. The surfaces are exposed to a reagent, having molecules each comprising a nitrenogenic group and a functionalizing group, in the presence of energized charged particles such as electrons and ions, photons, or heat, which transform the nitrenogenic reagent to a nitrene intermediate. The nitrene covalently reacts with any of various chemical groups present on the substrate surface, thereby effecting nitrene addition of the functionalizing groups to the substrate surface. The functionalizing groups can then participate in downstream chemistry whereby any of a large variety of functional groups, including biological molecules, can be covalently bonded to the surface, thereby dramatically altering the chemical behavior of the surface. Such functionalizations of the surface can be done in a single reactive step or in multiple reactive steps.

    摘要翻译： 公开了共价修饰各种基材的表面的方法，以及具有通过这些方法修饰的表面的各种基材。 候选表面包括各种聚合物，硅质，金属，同位素形式的碳和半导体表面。 表面暴露于试剂，其具有各自包含硝基衍生基团和官能化基团的分子，在激发带电粒子例如电子和离子，光子或热的存在下，其将硝化试剂转化为硝酸中间体。 所述氮烯与存在于所述基材表面上的各种化学基团共价反应，由此将所述官能团添加到所述基材表面上。 官能化基团然后可以参与下游化学，由此可以将大量各种官能团（包括生物分子）中的任何一个共价键合到表面，从而显着地改变表面的化学行为。 表面的这种功能化可以在单个反应步骤中或在多个反应步骤中进行。

    Molecularly imprinted materials, method for their preparation and devices employing such materials
    58.
    发明授权
    Molecularly imprinted materials, method for their preparation and devices employing such materials 失效
    分子印迹材料，其制备方法和使用这种材料的装置

    公开(公告)号：US5587273A

    公开(公告)日：1996-12-24

    申请号：US476918

    申请日：1995-06-07

    申请人： Mingdi Yan ,  John F. W. Keana ,  Martin N. Wybourne ,  Christophe J. P. Sevrain

    发明人： Mingdi Yan ,  John F. W. Keana ,  Martin N. Wybourne ,  Christophe J. P. Sevrain

    IPC分类号： G01N21/78 ,  C08F8/34 ,  C08K5/00 ,  C08L101/00 ,  G01N27/22 ,  G01N33/543 ,  G03F7/012 ,  G03F7/20 ,  G03C5/00

    CPC分类号： G01N33/54373 ,  C08F8/32 ,  G03F7/012 ,  G03F7/2041 ,  C08F2810/20 ,  G01N2600/00 ,  Y10S430/143

    摘要： A molecularly imprinted substrate and sensors employing the imprinted substrate for detecting the presence or absence of analytes are described. One embodiment of the invention comprises first forming a solution comprising a solvent and (a) a polymeric material capable of undergoing an addition reaction with a nitrene, (b) a crosslinking agent (c) a functionalizing monomer and (d) an imprinting molecule. A silicon wafer is spincoated with the solution. The solvent is evaporated to form a film on the silicon wafer. The film is exposed to an energy source to crosslink the substrate, and the imprinting molecule is then extracted from the film. The invention can be used to detect an analyte by forming films which are then exposed to a reaction energy to form a crosslinked substrate. The imprinting molecules are extracted from the crosslinked substrate. The film is exposed to one or more of the imprinting molecules for a period of time sufficient to couple the imprinting molecules to the film. The presence of the molecules is then detected. The invention also provides a molecularly imprinted polymeric material and sensors employing the molecularly imprinted polymeric material.

    摘要翻译： 描述了分子印迹的基底和采用印迹底物检测分析物存在或不存在的传感器。 本发明的一个实施方案包括首先形成包含溶剂的溶液和（a）能够与硝酸进行加成反应的聚合物，（b）交联剂（c）官能化单体和（d）压印分子。 用溶液旋涂硅晶片。 蒸发溶剂以在硅晶片上形成膜。 该膜暴露于能量源以使基底交联，然后从膜中提取压印分子。 本发明可用于通过形成膜然后暴露于反应能量以形成交联的底物来检测分析物。 印记分子从交联底物中提取出来。 将该膜暴露于一个或多个刻印分子一段足以使压印分子与膜结合的时间。 然后检测分子的存在。 本发明还提供了使用分子印迹聚合物材料的分子印迹聚合物材料和传感器。

    Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy
    59.
    发明授权
    Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy 失效
    衍生自二亚乙基三胺五乙酸的放大器分子，用于增强诊断和治疗

    公开(公告)号：US5412148A

    公开(公告)日：1995-05-02

    申请号：US133652

    申请日：1993-10-06

    申请人： John F. W. Keana

    发明人： John F. W. Keana

    IPC分类号： A61K49/18 ,  A61K49/20 ,  C07C291/04 ,  C07C229/04 ,  C07C229/16 ,  C07C275/16 ,  C07F5/00 ,  C07F11/00

    CPC分类号： A61K49/20 ,  A61K49/1812 ,  C07C291/04 ,  Y10S435/806 ,  Y10S436/803 ,  Y10T436/24

    摘要： Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.

    摘要翻译： 公开了放大器分子：具有分支结构的各种有机化合物，其末端具有可以化学连接药理活性基团的胺基团。 合成了许多MRI对比增强剂，每种都包含多个活性基团，如稳定的氮氧化物和三价金属阳离子的络合物。 使用具有不同支化结构的许多放大器成功地进行了这种合成，表明了合成具有各种药理学活性基团的放大器的相关化学物质的一般用途。 还合成放大器，其具有以化学反应性基团如异硫氰酸酯终止的接头，其使放大器具有双功能性：可附着于聚合物，生物大分子或具有多个反应性位点的其它生物相容性实体，例如末端胺。 通过这样的化学，放大器可附着于单体抗体，用于在体内所需位点浓集药理活性基团。