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    • 64. 发明授权
    • Cyclic amine bace-1 inhibitors having a heterocyclic substituent
    • 具有杂环取代基的环胺类bace-1抑制剂
    • US07910590B2
    • 2011-03-22
    • US12490884
    • 2009-06-24
    • Ying HuangGuoqing LiUlrich IserlohAndrew StamfordCorey StricklandJohannes H. VoigtJianping Pan
    • Ying HuangGuoqing LiUlrich IserlohAndrew StamfordCorey StricklandJohannes H. VoigtJianping Pan
    • A61K31/496A61K31/506
    • C04B35/632C07D207/277C07D401/12C07D401/14C07D403/12C07D403/14C07D405/14C07D409/14C07D413/12C07D413/14C07D417/14
    • Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R 14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
    • 公开了下式的新化合物或其药学上可接受的盐或溶剂合物,其中R 1是X是-O - , - C(R 14)2 - 或-N(R) - ; Z是-C(R 14)2 - 或-N(R) - ; t为0,1,2或3; 每个R和R 2独立地为H,烷基,环烷基,环烷基烷基,芳基,杂芳基,杂环烷基,芳基烷基,杂芳基烷基,杂环烷基烷基,烯基或炔基; 每个R 14是H,烷基,烯基,炔基,卤素,-CN,卤代烷基,环烷基,环烷基烷基,芳基,杂芳基,杂环烷基,芳基烷基,杂芳基烷基,杂环烷基烷基,-OR 35,-N(R 24)(R 25)或-SR 35; R41是烷基,环烷基,-SO2(烷基),-C(O) - 烷基,-C(O) - 环烷基或 - 烷基-NH-C(O)CH3; 其余变量如本说明书中所定义。 还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法,其包含式I化合物与用于治疗认知或神经变性的其它药剂 疾病
    • 67. 发明申请
    • Macrocyclic beta-secretase inhibitors
    • 大环β-分泌酶抑制剂
    • US20060040948A1
    • 2006-02-23
    • US11189346
    • 2005-07-26
    • Andrew StamfordYing HuangGuoqing LiCorey StrickandJohannes Voigt
    • Andrew StamfordYing HuangGuoqing LiCorey StrickandJohannes Voigt
    • A61K31/496C07D491/14
    • C07D498/04C07D413/06
    • Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    • 公开了下式的新化合物或其药学上可接受的盐或溶剂化物,其中R 1,R 2,R 3,n和X 如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经变性疾病的方法,其包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自β-分泌酶抑制剂的化合物的组合,所述β-分泌酶抑制剂除 式I,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂,非甾体抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂和抗淀粉样蛋白抗体。
    • 68. 发明授权
    • Link prediction based re-beamforming triggering algorithm for 60 ghz communication links
    • 基于链路预测的60Ghz通信链路的重新波束成形触发算法
    • US09369188B2
    • 2016-06-14
    • US13993196
    • 2011-12-13
    • Guoqing LiDmitry Akhmetov
    • Guoqing LiDmitry Akhmetov
    • H04B7/06H04B7/04
    • H04B7/0408H04B7/0617
    • A system and method are provided to trigger re-beamforming based on an algorithm that assesses various link characteristics. The algorithm is based on the ability of a 60 GHz receiving device to track and feedback a Received Signal Strength Indication (RSSI) to a 60 GHz data packet transmitter. By automatically analyzing RSSI values across a range of data packets, including consecutive data packets, a link degradation trend is predicted. When link degradation crosses, or is predicted to cross, a predetermined threshold, re-beamforming is triggered by the algorithm. Variables in the algorithm and the predetermined thresholds used by the algorithm can be automatically or manually modified to maintain a balance between appropriately triggering the re-beamforming when the conditions arise without unnecessarily triggering the re-beamforming thereby causing unneeded interruptions in regular data flow.
    • 提供了一种基于评估各种链路特性的算法来触发重新波束形成的系统和方法。 该算法基于60GHz接收设备跟踪并将接收信号强度指示(RSSI)反馈到60GHz数据分组发射机的能力。 通过自动分析包括连续数据包在内的数据包范围内的RSSI值,可以预测链路退化趋势。 当链路劣化交叉或被预测为交叉预定阈值时,由该算法触发重新波束形成。 可以自动地或手动地修改算法中使用的算法和预定阈值的变量,以便在条件出现时适当地触发重新波束形成之间保持平衡,而不必不必要地触发重新波束形成,从而导致规则数据流中不必要的中断。