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公开(公告)号：US5876946A
公开(公告)日：1999-03-02
申请号：US868280
申请日：1997-06-03
CPC分类号： C40B30/04 , C12Q1/25 , G01N33/54313 , G01N33/6845 , G01N33/6869 , G01N2500/00
摘要： A homogeneous high throughput assay is described which screens compounds for enzyme inhibition, or receptor or other target binding. Inhibition (or binding) by the library compounds causes a change in the amount of an optically detectable label that is bound to suspendable cells or solid supports. The amounts of label bound to individual cells or solid supports are microscopically determined, and compared with the amount of label that is not bound to individual cells or solid supports. The degree of inhibition or binding is determined using this data. Confocal microscopy, and subsequent data analysis, allow the assay to be carried out without any separation step, and provide for high throughput screening of very small assay volumes using very small amounts of test compound.
摘要翻译： 描述了筛选用于酶抑制的化合物或受体或其它靶结合的均匀高通量测定。 由文库化合物的抑制（或结合）导致与可悬浮细胞或固体支持物结合的光学可检测标记物的量的变化。 显微镜测定与单个细胞或固体支持物结合的标记物的量，并与不与单个细胞或固体支持物结合的标记物的量进行比较。 使用该数据确定抑制或结合的程度。 共聚焦显微镜和随后的数据分析允许在没有任何分离步骤的情况下进行测定，并且使用非常少量的测试化合物提供非常小的测定体积的高通量筛选。
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2.发明授权Fluorescent capture assay for kinase activity employing an anti-phosphotyrosine antibody as both the capture agent and detecting agent 失效使用抗磷酸酪氨酸抗体作为捕获剂和检测剂的荧光捕获测定激酶活性公开(公告)号：US06806056B2
公开(公告)日：2004-10-19
申请号：US10125784
申请日：2002-04-18
IPC分类号： G01N33567
CPC分类号： G01N33/573 , C12Q1/48 , G01N2333/91235
摘要： A method for determining the level of tyrosine kinase activity in a biological sample is disclosed. The method employs an anti-phosphotyrosine antibody as both the capture agent and the detecting agent. The detecting antibody is labeled with a fluorescent label, for instance, Cy5, Cy5.5 or Cy7 or a lanthanide ion, such as europium, as the signal generating entity. The method is particularly well suited to high throughput screening, for example, for compounds which modulate tyrosine kinase activity.
摘要翻译： 公开了确定生物样品中酪氨酸激酶活性水平的方法。 该方法采用抗磷酸酪氨酸抗体作为捕获剂和检测剂。 检测抗体用荧光标记（例如Cy5，Cy5.5或Cy7）或镧系元素离子如铕标记，作为信号发生实体。 该方法特别适用于高通量筛选，例如调节酪氨酸激酶活性的化合物。
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3.发明授权
公开(公告)号：US6156520A
公开(公告)日：2000-12-05
申请号：US911762
申请日：1997-08-15
CPC分类号： C40B30/04 , C12Q1/25 , G01N33/54313 , G01N33/6845 , G01N33/6869 , G01N2500/00
摘要： The present invention encompasses polypeptides that comprise a chemokine receptor binding sequence and are useful in determining the affinity of a compound for a chemokine receptor. Substitution of one of the amino acids of the C-terminal region of the polypeptide with a cysteine enables the polypeptide to be detectably labelled without loss of receptor binding activity and without the problems inherent in radioiodine labelling. Methods for use of the polypeptides in competitive binding assays are also disclosed.
摘要翻译： 本发明包括包含趋化因子受体结合序列并可用于测定化合物对趋化因子受体的亲和力的多肽。 用半胱氨酸取代多肽的C-末端区域的氨基酸之一使得能够可检测地标记多肽，而不损失受体结合活性，而没有放射性碘标记固有的问题。 还公开了在竞争性结合测定中使用多肽的方法。
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公开(公告)号：US20180000814A1
公开(公告)日：2018-01-04
申请号：US15623333
申请日：2017-06-14
IPC分类号： A61K31/485 , C12Q1/68
CPC分类号： A61K31/485 , C12Q1/6883 , C12Q2600/156
摘要： Provided herein are methods of treating Zellweger spectrum disorder (ZSD) in a subject in need thereof or improving peroxisome assembly in a cell in need thereof comprising administering to the subject a therapeutically effective amount of Compounds of Formula I or II.
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公开(公告)号：US08937067B2
公开(公告)日：2015-01-20
申请号：US13433656
申请日：2012-03-29
申请人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
发明人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
IPC分类号： A61K31/502 , C07D237/00 , C07D319/18 , C07D295/26 , C07D495/14 , A61P35/00
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
摘要翻译： 公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，
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6.发明申请COMPOUNDS AND METHODS OF USE THEREOF FOR TREATING NEURODEGENERATIVE DISORDERS 有权用于治疗神经损伤性疾病的化合物及其使用方法公开(公告)号：US20140187540A1
公开(公告)日：2014-07-03
申请号：US13985702
申请日：2012-02-15
申请人： Donald J. Zack , Cynthia Berlinicke , Laszlo Hackler , Zhiyong Yang , Joseph P. Steiner , Tomas Vojkovsky , Dana Ferraris , Barbara S. Slusher , James Inglese
发明人： Donald J. Zack , Cynthia Berlinicke , Laszlo Hackler , Zhiyong Yang , Joseph P. Steiner , Tomas Vojkovsky , Dana Ferraris , Barbara S. Slusher , James Inglese
IPC分类号： C07D403/12 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D453/02
摘要： Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
摘要翻译： 公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。
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公开(公告)号：US07037916B2
公开(公告)日：2006-05-02
申请号：US10340398
申请日：2003-01-10
申请人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
发明人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K31/52 , C07D413/00 , C07D239/02 , C70D473/00
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
摘要翻译： 公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。 化合物具有式I化合物。在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。 一个代表性的例子是：
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公开(公告)号：US20200046693A1
公开(公告)日：2020-02-13
申请号：US16417167
申请日：2019-05-20
IPC分类号： A61K31/485 , C12Q1/6883
摘要： Provided herein are methods of treating Zellweger spectrum disorder (ZSD) in a subject in need thereof or improving peroxisome assembly in a cell in need thereof comprising administering to the subject a therapeutically effective amount of Compounds of Formula I or II.
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9.发明授权公开(公告)号：US08741259B2
公开(公告)日：2014-06-03
申请号：US13125045
申请日：2008-10-20
申请人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
发明人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
IPC分类号： A61K51/00 , C07D239/88 , C07D217/24 , A61K31/47 , A61P35/00 , A61K31/167 , A61K31/517 , C07C233/01
CPC分类号： C07D405/06 , A61K31/517 , A61K49/0004 , A61K51/00 , C07D239/91 , C07D401/06 , C07D405/14 , C07D487/04
摘要： Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
摘要翻译： 公开了可用作选择性TSHR激动剂的氧代 - 氢喹唑啉。 该化合物可用于检测或治疗甲状腺癌或治疗骨退行性疾病。
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公开(公告)号：US20120245141A1
公开(公告)日：2012-09-27
申请号：US13433656
申请日：2012-03-29
申请人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
发明人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
IPC分类号： A61K31/496 , A61K31/495 , C07D243/08 , A61K31/551 , C07D405/12 , A61K31/453 , C07D405/14 , C07D319/18 , A61K31/357 , A61K31/4025 , A61K31/397 , C07D495/14 , A61K31/5025 , C07D215/22 , A61K31/4704 , A61P35/00 , A61P35/02 , C07D295/26
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
摘要翻译： 公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，
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