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公开(公告)号:US20150197505A1
公开(公告)日:2015-07-16
申请号:US14405773
申请日:2013-06-05
申请人: IRM LLC
发明人: Gerald Lelais , Robert Epple , Thomas H. Marsilje, III , Pierre-Yves Michellys , Matthew McNeill , Yun Long , Wenshuo Lu , Bei Chen , Badry Bursulaya Bursulaya , Songchun Jiang
IPC分类号: C07D401/14 , C07D403/14 , A61K31/551 , A61K31/4545 , C07D413/14 , C07D413/04 , A61K31/553 , C07D471/04 , C07D403/04 , C07D513/04 , C07D405/14 , C07D417/14 , A61K31/4184 , A61K31/454 , C07D401/04 , A61K45/06 , A61K31/55
CPC分类号: C07D401/14 , A61K31/4184 , A61K31/454 , A61K31/4545 , A61K31/55 , A61K31/551 , A61K31/553 , A61K45/06 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
摘要: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.
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公开(公告)号:US20080032917A1
公开(公告)日:2008-02-07
申请号:US11619155
申请日:2007-01-02
申请人: Jun Li , Jennifer Harris , Christine Tumanut
发明人: Jun Li , Jennifer Harris , Christine Tumanut
CPC分类号: C12Q1/37 , C12Q1/18 , G01N2333/18 , G01N2500/02
摘要: The invention provides substrate specificity profiles for flaviviral proteases (e.g., dengue proteases or West Nile protease). Optimal flaviviral protease substrate sequences, both to the prime side and non-prime side of the flaviviral protease recognition site, are disclosed herein. The flaviviral protease substrate sequences are used in designing substrates, inhibitors, and prodrugs. Flaviviral protease inhibitors based on substrate specificity are also provided.
摘要翻译: 本发明提供黄病毒蛋白酶(例如登革热蛋白酶或西尼罗河蛋白酶)的底物特异性谱。 本文公开了黄病毒蛋白酶识别位点的最优侧和非质量侧的最佳黄病毒蛋白酶底物序列。 黄病毒蛋白酶底物序列用于设计底物,抑制剂和前药。 还提供了基于底物特异性的黄病毒蛋白酶抑制剂。
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3.
公开(公告)号:US20060171923A1
公开(公告)日:2006-08-03
申请号:US10849567
申请日:2004-05-18
申请人: Sheng Chao , Jeremy Caldwell
发明人: Sheng Chao , Jeremy Caldwell
CPC分类号: C12Q1/6897 , C12Q1/702
摘要: This invention relates to the discovery that the transcription factors Pbx1 and HMG1 are involved in retrovirus, e.g., HIV, replication. Thus, the invention provides methods of identifying modulators of these proteins. Such modulators can be used as reagents in in vitro assays to modulate expression of retroviral sequences and may be used to inhibit HIV replication in vivo.
摘要翻译: 本发明涉及转录因子Pbx1和HMG1参与逆转录病毒例如HIV复制的发现。 因此,本发明提供鉴定这些蛋白质的调节剂的方法。 这种调节剂可用作体外测定中的试剂以调节逆转录病毒序列的表达,并可用于抑制体内HIV复制。
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公开(公告)号:US20060009642A1
公开(公告)日:2006-01-12
申请号:US11223429
申请日:2005-09-09
申请人: Sheng Ding , Qiang Ding , Nathanael Gray , Peter Schultz
发明人: Sheng Ding , Qiang Ding , Nathanael Gray , Peter Schultz
IPC分类号: C07D473/24 , C07D473/16
CPC分类号: C07D473/16 , C07D473/06 , C07D473/18
摘要: The invention provides general methods for preparing 2,9-, 2,6,9-, O6-aryl- and O6-alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.
摘要翻译: 本发明提供了一种制备组合中的2,9-,2,6,9-六-O-芳基和O-6 - 烷基取代的嘌呤的一般方法, 无痕的时尚。 在一些实施方案中,所述方法涉及N9上的2-氟-6-苯基亚磺酰基嘌呤在溶液中的醇的Mitsunobu烷基化,随后用树脂结合的胺C2-捕获嘌呤核心,随后氧化和置换C6磺酰基 与胺和苯胺。
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公开(公告)号:US20050014724A1
公开(公告)日:2005-01-20
申请号:US10849079
申请日:2004-05-19
申请人: Thomas Marsilje , Nathanel Gray , Tao Jiang , Wenshuo Lu , Shifeng Pan
发明人: Thomas Marsilje , Nathanel Gray , Tao Jiang , Wenshuo Lu , Shifeng Pan
IPC分类号: A61K20060101 , A61K31/195 , A61K31/216 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/675 , C07C323/63 , C07D205/04 , C07D207/12 , C07D211/32 , C07D241/04 , C07F9/22 , C07F9/28
CPC分类号: C07C323/32 , C07C317/32 , C07C2601/14 , C07D205/04
摘要: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
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公开(公告)号:US20050009052A1
公开(公告)日:2005-01-13
申请号:US10830708
申请日:2004-04-22
申请人: Frantisek Supek , Nicholas Gekakis
发明人: Frantisek Supek , Nicholas Gekakis
IPC分类号: C12P19/34 , C12Q20060101 , C12Q1/68 , G01N33/50
CPC分类号: G01N33/5011
摘要: The present invention is based on a novel cell tagging approach called “Differential Tag Length” method (DTLA) that allows the quantitative analysis of a mixture of multiple cell types (e.g., strains) grown in very small cultivation volumes. DTLA can also be fully automated and adapted for a high-throughput format. The invention provides methods for detecting proliferation of a mixture of cell types in a culture, for screening a library of compounds to identify those compounds that modulate proliferation of a cell, and for detecting the presence or absence of targets in a sample. The invention also provides kits comprising at least first polynucleotide tag and a second polynucleotide tag.
摘要翻译: 本发明基于称为“差异标签长度”(DTLA)的新型细胞标记方法,其允许定量分析以非常小的培养体积生长的多种细胞类型(例如菌株)的混合物。 DTLA也可以完全自动化并适应高吞吐量格式。 本发明提供了用于检测培养物中细胞类型混合物的增殖的方法,用于筛选化合物文库以鉴定调节细胞增殖的那些化合物,以及用于检测样品中靶标的存在或不存在。 本发明还提供了包含至少第一个多核苷酸标签和第二个多核苷酸标签的试剂盒。
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公开(公告)号:US20030225205A1
公开(公告)日:2003-12-04
申请号:US10379607
申请日:2003-05-08
发明人: Robert Epple , William Greenberg , Romas Kudirka
IPC分类号: C12Q001/68 , C07H019/16 , C07H019/06 , C08G063/48
摘要: The present invention provides combinatorial libraries of nucleoside analog compounds and methods of making the libraries. In addition, the present invention provides methods of assaying the libraries for agonists or antagonists of a broad array of targets of therapeutic importance.
摘要翻译: 本发明提供核苷类似物化合物的组合文库和制备文库的方法。 此外,本发明提供了测定具有治疗重要性的广泛靶标的激动剂或拮抗剂的文库的方法。
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公开(公告)号:US20020090320A1
公开(公告)日:2002-07-11
申请号:US09981313
申请日:2001-10-15
发明人: Kristina Marie Burow , Jeremy S. Caldwell , Robert Charles Downs , Scott Allan Lesley , James Kevin Mainquist , Andrew J. Meyer , Daniel G. Sipes , Mark Richard Weselak
IPC分类号: G01N035/00
CPC分类号: B01L9/523 , B01J2219/00587 , B01J2219/00689 , B01J2219/00691 , B01J2219/00707 , B01J2219/0072 , B01L2300/0829 , B01L2300/0893 , G01N35/0099 , G01N35/025 , G01N35/026 , G01N35/028 , G01N35/04 , G01N35/1074 , G01N2015/1006 , G01N2035/00306 , G01N2035/00366 , G01N2035/0405 , G01N2035/0427 , G01N2035/1037 , G01N2500/10 , G01N2500/20 , Y02A50/58 , Y10T436/114165 , Y10T436/2575
摘要: Briefly, the present invention provides a system and method for high throughput processing using sample holders. The system has a plurality of work perimeters, with a rotational robot preferably associated with each work perimeter. At least one transfer station area is provided between adjacent work perimeters to facilitate robotic transfer of sample holders from one work perimeter to another area. Each work perimeter typically includes a plurality of defined station locations, with each station location positioned to be accessible by the robot associated with that area. In addition, each station location is typically configured to receive a device, such as an automated instrument or a holding nest. Device components are arranged at selected station locations according to specific application requirements to provide a flexible, robust, reliable, and accurate high throughput processing system.
摘要翻译: 简而言之,本发明提供了一种使用样品保持器进行高通量处理的系统和方法。 该系统具有多个工作周边,其中旋转机器人优选地与每个工作周界相关联。 在相邻的工作周边之间提供至少一个传送站区域,以便于将样品架从一个工作周边机器人传送到另一个区域。 每个工作周界通常包括多个定义的站位置,其中每个站位置定位成由与该区域相关联的机器人可访问。 此外,每个站位置通常被配置为接收诸如自动化仪器或保持嵌套之类的设备。 设备组件根据特定的应用要求安排在选定的站位置,以提供灵活,稳健,可靠,准确的高吞吐量处理系统。
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9.
公开(公告)号:US20050037390A1
公开(公告)日:2005-02-17
申请号:US10862013
申请日:2004-06-04
申请人: Fred King , Sumit Chanda , Jeremy Caldwell , John Hogenesch
发明人: Fred King , Sumit Chanda , Jeremy Caldwell , John Hogenesch
CPC分类号: G01N33/5023 , G01N33/74 , G01N33/746 , G01N2333/505 , G01N2500/10
摘要: This invention provides novel Epo-modulating polypeptides. The invention also provides methods for screening modulators of Epo expression. The methods comprise first screening test agents for modulators of an Epo-modulating polypeptide and then further screening the identified modulating agents for modulators of Epo expression. The invention further provides methods and pharmaceutical compositions for modulating Epo expression in cells and for treating diseases and conditions due to Epo deficiency.
摘要翻译: 本发明提供新型的Epo调节多肽。 本发明还提供了筛选Epo表达调节剂的方法。 所述方法包括首先筛选Epo调节多肽的调节剂的测试剂,然后进一步筛选鉴定的调节剂用于Epo表达的调节剂。 本发明还提供用于调节细胞中Epo表达并用于治疗由于Epo缺乏引起的疾病和病症的方法和药物组合物。
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公开(公告)号:US20030191312A1
公开(公告)日:2003-10-09
申请号:US10270030
申请日:2002-10-12
发明人: Sheng Ding , Qiang Ding , Nathanael S. Gray
IPC分类号: C07D473/18 , C07D473/16 , A61K031/522 , A61K031/52
CPC分类号: C07D239/42 , C07D239/94 , C07D241/20 , C07D241/44 , C07D473/16 , C07D473/18 , C07D473/34
摘要: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
摘要翻译: 已经证明了溶液相的一般方法以及各种取代的杂芳基的固相合成。 这些取代的杂芳基可以通过在升高的温度下用胺进行芳族取代或通过苯胺,硼酸和酚通过钯催化的交叉偶联反应进一步精制。
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