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    • 6. 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。
    • 7. 发明申请
    • Macrocyclic heterocyclic aspartyl protease inhibitors
    • 大环杂环天门冬酰胺蛋白酶抑制剂
    • US20060281729A1
    • 2006-12-14
    • US11451064
    • 2006-06-12
    • Ulrich IserlohZhaoning ZhuAndrew StamfordJohannes Voigt
    • Ulrich IserlohZhaoning ZhuAndrew StamfordJohannes Voigt
    • A61K31/4188C07D487/02
    • C07D487/08
    • Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    • 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐,溶剂化物或酯,其中U,W,X,L,Y,M,Z,c,d,e,f,g, s,t,R 1,R 2,R 7,R 8,R 9, R 10,R 11,R 12,R 13,R 14, R 15,R 16,R 17和R 18如本说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m 1激动剂或m 2 N拮抗剂组合治疗认知或神经变性疾病的方法。
    • 10. 发明授权
    • Method for coating a rubber wiper blade
    • 橡胶刮水片涂布方法
    • US06287642B1
    • 2001-09-11
    • US09424729
    • 2000-03-14
    • Wolfgang LeutschJohannes RauschnabelJeanne ForgetJohannes Voigt
    • Wolfgang LeutschJohannes RauschnabelJeanne ForgetJohannes Voigt
    • C23C16513
    • C23C14/22B60S2001/3829C23C14/027C23C16/029C23C16/50
    • In the process for coating the elastomeric rubber wiper a vaporous coating material is generated and activated by a plasma and/or laser; a protective coating is formed on a rubber wiper surface by exposing it to the vaporous coating material by CVD and/or PVD methods and process parameters for the coating process are controlled so that the protective coating includes at least three coating layers and has a total thickness of from 200 nm to 2 &mgr;m. The coating layers include at least one thicker softer elastic coating layer with elastomeric properties similar to those of the rubber wiper and other thinner harder coating layers having wear-resistant properties. The other thinner harder coating layers have respective hardness increasing from an inner most one to an outermost one of the other thinner harder coating layers.
    • 在用于涂覆弹性体橡胶擦拭器的过程中,通过等离子体和/或激光产生并激活蒸汽涂层材料; 通过用CVD和/或PVD方法将橡胶擦拭表面暴露于气态涂料上,形成保护涂层,并且控制用于涂覆过程的工艺参数,使得保护涂层包括至少三个涂层并具有总厚度 为200〜2μm。 涂层包括至少一个较软的较软的弹性涂层,其具有与橡胶擦拭器和具有耐磨性能的其它较薄的较硬的涂层相似的弹性体性质。 其他较薄的较硬的涂层具有相应的硬度从另一较薄的较硬的涂层中的最内层到最外层的硬度。