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    Time resolved single-step protease activity quantification using nanoplasmonic resonator (NPR) sensor
    2.
    发明申请
    Time resolved single-step protease activity quantification using nanoplasmonic resonator (NPR) sensor 有权
    使用纳米弹性共振器（NPR）传感器的时间分辨单步蛋白酶活性定量

    公开(公告)号：US20110058164A1

    公开(公告)日：2011-03-10

    申请号：US12772118

    申请日：2010-04-30

    申请人： Xiang Zhang ,  Jonathan A. Ellman ,  Fanqing Frank Chen ,  Cheng Sun ,  Kai-Hang Su ,  Qi-Huo Wei

    发明人： Xiang Zhang ,  Jonathan A. Ellman ,  Fanqing Frank Chen ,  Cheng Sun ,  Kai-Hang Su ,  Qi-Huo Wei

    IPC分类号： G01J3/44

    CPC分类号： G01N21/658 ,  B82Y15/00 ,  B82Y20/00 ,  C12Q1/37

    摘要： A nanoplasmonic resonator (NPR) comprising a metallic nanodisk with alternating shielding layer(s), having a tagged biomolecule conjugated or tethered to the surface of the nanoplasmonic resonator for highly sensitive measurement of enzymatic activity. NPRs enhance Raman signals in a highly reproducible manner, enabling fast detection of protease and enzyme activity, such as Prostate Specific Antigen (paPSA), in real-time, at picomolar sensitivity levels. Experiments on extracellular fluid (ECF) from paPSA-positive cells demonstrate specific detection in a complex bio-fluid background in real-time single-step detection in very small sample volumes.

    摘要翻译： 纳米等离子体共振器（NPR）包括具有交替屏蔽层的金属纳米盘，其具有缀合或连接到纳米塑料谐振器表面的标记生物分子，用于酶活性的高度灵敏测量。 NPR以高度可重复的方式增强拉曼信号，能够以皮摩尔敏感度水平实时快速检测蛋白酶和酶活性，如前列腺特异抗原（paPSA）。 来自paPSA阳性细胞的细胞外液（ECF）的实验在非常小的样品体积中在实时单步检测中在复杂的生物流体背景中表现出特异性检测。

    Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
    3.
    发明授权
    Methods for treating neurodegenerative disorders using aspartyl protease inhibitors 失效
    使用天冬氨酰蛋白酶抑制剂治疗神经变性疾病的方法

    公开(公告)号：US07119105B2

    公开(公告)日：2006-10-10

    申请号：US10774262

    申请日：2004-02-05

    申请人： Jonathan A. Ellman ,  Gary Lynch ,  Irwin D. Kuntz ,  Xiaoning Bi ,  Christina E. Lee ,  A. Geoffrey Skillman ,  Tasir Haque

    发明人： Jonathan A. Ellman ,  Gary Lynch ,  Irwin D. Kuntz ,  Xiaoning Bi ,  Christina E. Lee ,  A. Geoffrey Skillman ,  Tasir Haque

    IPC分类号： A99Z99/00

    CPC分类号： C07D209/48 ,  A61K31/36 ,  A61K31/4035 ,  A61K31/423 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4525 ,  A61K31/454 ,  C07D263/58 ,  C07D317/58 ,  C07D317/60 ,  C07D317/62 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (τ-protein); and (iv) methods for treating neurodegenerative diseases. For instance, in one embodiment, the present invention provides a method for modulating the processing of an amyloid precursor protein (APP), the method comprising contacting a composition containing the APP with an aspartyl protease inhibitor having the formula: wherein: R1, R2 and R3 are members independently selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl, substituted aryloxyalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, heterocycles, substituted heterocycles, heterocyclicalkyl and substituted heterocyclicalkyl; and R5 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryloxyalkyl and substituted aryloxyalkyl; or R5 and R6 and the carbons to which they are bound join to form an optionally substituted carbocyclic or heterocyclic fused ring system having a total of 9- or 10-ring atoms within the fused ring system.

    摘要翻译： 本发明涉及（）非肽天冬氨酰蛋白酶抑制剂; （ii）调节淀粉样蛋白前体蛋白（APP）的加工的方法; （iii）调节tau蛋白（tau蛋白）的加工的方法; 和（iv）治疗神经变性疾病的方法。 例如，在一个实施方案中，本发明提供了调节淀粉样蛋白前体蛋白（APP）的加工的方法，所述方法包括将含有APP的组合物与具有下式的天冬氨酰蛋白酶抑制剂接触：其中： 1，R 2和R 3是独立地选自烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，芳氧基烷基 取代的芳氧基烷基，杂芳基，取代的杂芳基，杂芳基烷基，取代的杂芳基烷基，杂环，取代的杂环，杂环烷基和取代的杂环烷基; R 5和R 6独立地选自氢，卤素，烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，芳氧基烷基和取代的 芳氧基烷基; 或R 5和R 6和它们所连接的碳原子连接形成任选取代的碳环或杂环稠环体系，其具有总共9或10环 稠环体系内的原子。

    Pharmacophore recombination for the identification of small molecule drug lead compounds
    5.
    发明授权
    Pharmacophore recombination for the identification of small molecule drug lead compounds 失效
    用于鉴定小分子药物铅化合物的药代素重组

    公开(公告)号：US06344330B1

    公开(公告)日：2002-02-05

    申请号：US09049754

    申请日：1998-03-27

    申请人： Jonathan A. Ellman ,  Ingrid Choong

    发明人： Jonathan A. Ellman ,  Ingrid Choong

    IPC分类号： A61K31335

    CPC分类号： C40B30/04 ,  G01N33/531 ,  G01N33/6845 ,  G01N2500/04 ,  Y10S530/807

    摘要： The present invention is directed to novel methods for identifying small molecule ligands that are capable of binding with high affinity to a biological target molecule of interest. High affinity binding ligands identified by the described methods find use, for example, as small molecule lead compounds that may they themselves be, or may give rise to, novel therapeutic drugs. More specifically, the subject invention is directed to methods for identifying a ligand that binds to a target biological molecule of interest, wherein a population of small organic compounds are selected and then “pre-screened” to identify those that are capable of binding to the molecular target. The small organic compounds that are identified during the pre-screening as being capable of binding to the target (or structurally related analogs thereof) are then coupled in various combinations with a linker element to provide a library of potential ligands for binding to the target molecule that is then screened to identify ligands having very high binding affinities for the molecular target. Ligands obtained by this method and methods for using those ligands for inhibiting the interaction between two biological molecules are also provided.

    摘要翻译： 本发明涉及用于鉴定能够以高亲和力结合到感兴趣的生物靶标分子的小分子配体的新方法。 通过所述方法鉴定的高亲和力结合配体可用于例如小分子铅化合物，它们本身可以是或可能产生新的治疗药物。 更具体地，本发明涉及用于鉴定与目标生物分子结合的配体的方法，其中选择小的有机化合物群体，然后“预筛选”以鉴定能够结合到 分子靶。 在预筛选期间鉴定为能够与靶标（或其结构相关的类似物）结合的小有机化合物然后以与接头元件的多种组合进行偶联以提供用于结合靶分子的潜在配体文库 然后筛选以鉴定对分子靶具有非常高的结合亲和力的配体。 还提供了通过该方法获得的配体和使用这些配体抑制两个生物分子之间相互作用的方法。

    Detection of protease and protease activity using a single nanoscrescent SERS probe
    8.
    发明授权
    Detection of protease and protease activity using a single nanoscrescent SERS probe 有权
    使用单个纳米SERS探针检测蛋白酶和蛋白酶活性

    公开(公告)号：US08361932B2

    公开(公告)日：2013-01-29

    申请号：US12299284

    申请日：2007-05-02

    申请人： Gang L. Liu ,  Jonathan A. Ellman ,  Luke P. Lee ,  Fanqing Frank Chen

    发明人： Gang L. Liu ,  Jonathan A. Ellman ,  Luke P. Lee ,  Fanqing Frank Chen

    IPC分类号： C40B30/04 ,  C40B40/10 ,  G01N33/573

    CPC分类号： C12Q1/37 ,  G01N33/57434 ,  G01N33/587 ,  G01N2333/96433 ,  G01N2333/96466 ,  G01N2333/974

    摘要： This invention pertains to the in vitro detection of proteases using a single peptide-conjugate nanocrescent surface enhanced Raman scattering (SERS) probes with at least nanomolar sensitivity. The probe enables detection of proteolytic activity in extremely small volume and at low concentration. In certain embodiments the probes comprise an indicator for the detection of an active protease, where the indicator comprises a nanocrescent attached to a peptide, where said peptide comprises a recognition site for the protease and a Raman tag attached to the peptide.

    摘要翻译： 本发明涉及使用具有至少纳摩尔灵敏度的单个肽 - 缀合的纳米新月面增强拉曼散射（SERS）探针的体外检测蛋白酶。 该探针能够以非常小的体积和低浓度检测蛋白水解活性。 在某些实施方案中，探针包含用于检测活性蛋白酶的指示剂，其中指示剂包含连接到肽的纳米新月形，其中所述肽包含蛋白酶的识别位点和与肽连接的拉曼标签。

    Method of Converting a Polyol to an Olefin
    9.
    发明申请
    Method of Converting a Polyol to an Olefin 有权
    将多元醇转化为烯烃的方法

    公开(公告)号：US20090287004A1

    公开(公告)日：2009-11-19

    申请号：US12509985

    申请日：2009-07-27

    申请人： Robert G. Bergman ,  Jonathan A. Ellman ,  Elena Arceo Rebollo ,  Peter C. Marsden

    发明人： Robert G. Bergman ,  Jonathan A. Ellman ,  Elena Arceo Rebollo ,  Peter C. Marsden

    IPC分类号： C07D307/06 ,  C07C29/00 ,  C07C1/207 ,  C07C51/00

    CPC分类号： C07C29/60 ,  C07C33/03

    摘要： A method of preparing an olefin comprising: reacting a polyol in the presence of a carboxylic acid, such that an olefin is produced by the deoxygenation of the polyol. The reacting step can comprise (a) providing a composition comprising the polyol, (b) heating the composition, and (c) introducing the carboxylic acid to the composition wherein the introducing step occurs prior to, at the same time as, or subsequent to the heating step. In one embodiment, the polyol is glycerol, the carboxylic acid is formic acid, and the olefin is allyl alcohol, which is produced at a yield of about 80% or greater.

    摘要翻译： 一种制备烯烃的方法，包括：在羧酸存在下使多元醇反应，使得通过多元醇的脱氧生成烯烃。 反应步骤可以包括（a）提供包含多元醇的组合物，（b）加热组合物，和（c）将羧酸引入到组合物中，其中引入步骤在同时或之后 加热步骤。 在一个实施方案中，多元醇是甘油，羧酸是甲酸，烯烃是以约80％或更高的产率生产的烯丙醇。