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公开(公告)号：US08575150B2
公开(公告)日：2013-11-05
申请号：US13139830
申请日：2009-12-07
申请人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
发明人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
IPC分类号： C07D249/14 , A61K31/4196
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱Abeta42的产生，因此可用于治疗阿尔茨海默病和相关病症。
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公开(公告)号：US08183276B2
公开(公告)日：2012-05-22
申请号：US12526074
申请日：2008-02-05
IPC分类号： A01N43/50 , A61K31/415 , C07D233/00 , C07D233/56 , C07D233/58
CPC分类号： C07D487/04 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D491/04 , C07D495/04
摘要： The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.
摘要翻译： 本发明包括选择性减弱Aβ（1-42）产生并可用于治疗阿尔茨海默病的2- [4-（咪唑基） - 苯基]乙烯基 - 杂环衍生物。 还包括药物组合物和使用方法。
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公开(公告)号：US20120022044A1
公开(公告)日：2012-01-26
申请号：US13139830
申请日：2009-12-07
申请人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
发明人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
IPC分类号： A61K31/55 , C07D403/04 , C07D409/14 , A61P25/28 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D401/14 , C07D417/14
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱A＆bgr的产生42，因此可用于治疗阿尔茨海默病和相关病症。
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公开(公告)号：US20100324029A1
公开(公告)日：2010-12-23
申请号：US12526074
申请日：2008-02-05
IPC分类号： A61K31/422 , C07D413/10 , A61K31/4245 , C07D403/10 , A61K31/4184 , A61K31/4178 , A61K31/517 , C07D495/04 , A61K31/519 , C07D491/048 , C07D413/14 , C07D417/10 , A61K31/428 , A61K31/5415 , A61K31/4439 , A61P25/28
CPC分类号： C07D487/04 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D491/04 , C07D495/04
摘要： The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.
摘要翻译： 本发明包括选择性减弱Aβ（1-42）产生并可用于治疗阿尔茨海默病的2- [4-（咪唑基） - 苯基]乙烯基 - 杂环衍生物。 还包括药物组合物和使用方法。
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公开(公告)号：US20110313001A1
公开(公告)日：2011-12-22
申请号：US13133833
申请日：2009-12-07
申请人： Christian Fischer , Adam J. Schell , Benito Munoz
发明人： Christian Fischer , Adam J. Schell , Benito Munoz
IPC分类号： A61K31/4439 , A61P25/28 , C07D403/10 , A61K31/4192 , C07D401/10 , C07D413/14
CPC分类号： C07D403/10 , C07D401/10
摘要： According to the invention there is provided a compound of formula (I): (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译： 根据本发明，提供式（I）化合物：（I）或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱A＆bgr的产生42，因此可用于治疗阿尔茨海默病和相关病症。
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公开(公告)号：US10975084B2
公开(公告)日：2021-04-13
申请号：US16341313
申请日：2017-10-06
申请人： Merck Sharp & Dohme Corp. , Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
发明人： Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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公开(公告)号：US09145391B2
公开(公告)日：2015-09-29
申请号：US14116199
申请日：2012-05-04
申请人： Denis Deschenes , Michael D. Altman , John Michael Ellis , Christian Fischer , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Adam J. Schell , Graham F. Smith , Brandon M. Taoka , Corey Bienstock , Maria Emilia Di Francesco , Anthony Donofrio , Scott Peterson , Kerrie B. Spencer , James Patrick Jewell , Amjad Ali , David Jonathan Bennett , Qun Dang , John Wai
发明人： Denis Deschenes , Michael D. Altman , John Michael Ellis , Christian Fischer , Andrew M. Haidle , Solomon D. Kattar , Alan B. Northrup , Adam J. Schell , Graham F. Smith , Brandon M. Taoka , Corey Bienstock , Maria Emilia Di Francesco , Anthony Donofrio , Scott Peterson , Kerrie B. Spencer , James Patrick Jewell , Amjad Ali , David Jonathan Bennett , Qun Dang , John Wai
IPC分类号： C07D213/73 , C07D401/14 , C07D401/12 , C07D409/14 , C07D417/14 , C07D471/04
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14 , C07D417/14 , C07D471/04
摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
摘要翻译： 本发明提供了式I的新型嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，或其前药，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎和癌症。
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公开(公告)号：US20130096084A1
公开(公告)日：2013-04-18
申请号：US13703250
申请日：2011-06-22
申请人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
发明人： Yongqi Deng , Liang Zhu , Gerald W. Shipps, JR. , Sie-Mun Lo , Binyuan Sun , Xiaohua Huang , Corey Bienstock , Alan B. Cooper , Xiaolei Gao , Xin Yao , Hugh Y. Zhu , Joseph M. Kelly , Sobhana Babu Boga , Abdul-Basit Alhassan , Jayaram R. Tagat , Umar Faruk Mansoor , Kevin J. Wilson , Brendan M. O'Boyle , Matthew Hersh Daniels , Adam Schell , Phieng Siliphaivanh , Christian Fischer
IPC分类号： C07D401/14 , A61K45/06 , C07D405/14 , A61K31/454 , A61K31/55 , A61K31/551 , C07D401/12 , C07D409/14 , C07D417/14 , A61K31/506 , C07D471/04 , C07F7/18 , A61K31/695 , C07D413/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D401/14 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/1804
摘要： The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
摘要翻译： 本发明提供了式I化合物：（式I应在此插入）或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2和R 3如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。
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公开(公告)号：US08248072B1
公开(公告)日：2012-08-21
申请号：US13082006
申请日：2011-04-07
IPC分类号： G01V3/00
CPC分类号： G01N24/08 , G01N24/085 , G01N24/088 , G01R33/4625 , G01R33/543
摘要： An automated screening device that performs standardized system suitability tests and evaluations and measures components of a submitted sample to assist in the quality control screening of raw materials, ingredients, pharmaceuticals, chemicals, polymers, food products, petroleum and many other materials. After determining the performance suitability of an NMR spectrometer, the system permits samples to be submitted for screening. An NMR spectrum of a sample is acquired and a qualitative analysis unit identifies at least one reference NMR spectrum corresponding a compound present in the sample and a quantitative analysis unit integrates relative signal intensity signals of the sample spectrum in regions of peak intensity in the one reference NMR spectrum and compares integration results to a number of atoms in each region in order to confirm identification of the compound.
摘要翻译： 一种自动筛选装置，执行标准化的系统适用性测试和评估并测量提交样品的组成部分，以协助对原材料，成分，药物，化学品，聚合物，食品，石油和许多其他材料进行质量控制筛选。 在确定NMR光谱仪的性能适用性后，系统允许样品提交进行筛选。 获得样品的NMR光谱，并且定性分析单元鉴定对应于样品中存在的化合物的至少一个参考NMR光谱，并且定量分析单元将样品光谱的相对信号强度信号在一个参考中的峰强度区域中积分 NMR谱，并将整合结果与每个区域中的多个原子进行比较，以确认化合物的鉴定。
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10.发明授权公开(公告)号：US07076383B2
公开(公告)日：2006-07-11
申请号：US10921108
申请日：2004-08-19
IPC分类号： G01R23/16
CPC分类号： G01R33/4625 , Y10T436/24
摘要： The invention refers to a method of resonance spectroscopy for the analysis of statistical properties of samples, comprising the following steps: a) recording of a complex resonance frequency spectrum of each sample by means of phase sensitive quadrature detection; b) numerical differentiation of the recorded complex resonance frequency spectra versus frequency; c) determination of the absolute value of each differentiated complex resonance frequency spectrum (=fingerprint); d) allocation of each fingerprint to a point of a multidimensional point set; and e) performing a pattern analysis of the generated points for characterizing the statistical properties of the samples. The inventive method tolerates unintended variances of measurement in the recorded resonance frequency spectra, in particular caused by phase errors, and allows reliable automated spectral analysis.
摘要翻译： 本发明涉及一种用于分析样品的统计性质的共振光谱法，包括以下步骤：a）通过相敏检测记录每个样品的复共振频谱; b）记录的复共振频谱与频率的数值分化; c）确定每个微分复合共振频谱（=指纹）的绝对值; d）将每个指纹分配到多维点集的点; 以及e）对生成的点执行模式分析，以表征样本的统计特性。 本发明的方法容忍记录的共振频谱中的非预期的测量方差，特别是由相位误差引起的，并且允许可靠的自动光谱分析。
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