Macrocyclic beta-secretase inhibitors
    6.
    发明申请
    Macrocyclic beta-secretase inhibitors 有权
    大环β-分泌酶抑制剂

    公开(公告)号:US20060040948A1

    公开(公告)日:2006-02-23

    申请号:US11189346

    申请日:2005-07-26

    IPC分类号: A61K31/496 C07D491/14

    CPC分类号: C07D498/04 C07D413/06

    摘要: 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.

    摘要翻译: 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。

    Macrocyclic heterocyclic aspartyl protease inhibitors
    7.
    发明申请
    Macrocyclic heterocyclic aspartyl protease inhibitors 有权
    大环杂环天门冬酰胺蛋白酶抑制剂

    公开(公告)号:US20060281729A1

    公开(公告)日:2006-12-14

    申请号:US11451064

    申请日:2006-06-12

    IPC分类号: A61K31/4188 C07D487/02

    CPC分类号: C07D487/08

    摘要: 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.

    摘要翻译: 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。

    Method and device for vacuum-coating a substrate
    9.
    发明授权
    Method and device for vacuum-coating a substrate 有权
    用于真空涂覆基材的方法和装置

    公开(公告)号:US06372303B1

    公开(公告)日:2002-04-16

    申请号:US09446054

    申请日:2000-04-05

    IPC分类号: C23C1626

    摘要: A method is proposed for vacuum-coating a substrate using a plasma-CVD method. In order to control ion bombardment during the vacuum coating, a substrate voltage produced independently from a coating plasma is applied to the substrate. The substrate voltage is modified during the coating. The substrate voltage is a direct voltage that is pulsed in bipolar fashion with a frequency of 0.1 kHz to 10 MHz. A wear-resistant and friction-reducing multilayer structure of alternating hard material individual layers and carbon or silicon individual layers is proposed.

    摘要翻译: 提出了使用等离子体CVD法对基板进行真空镀膜的方法。 为了控制真空镀膜中的离子轰击,将独立于涂覆等离子体产生的基板电压施加到基板上。 衬底电压在涂层期间被修改。 衬底电压是以0.1kHz至10MHz的频率以双极方式脉冲的直流电压。 提出了一种耐磨和减摩的多层结构,交替硬质材料单层和碳或硅单层。

    Method for coating a rubber wiper blade
    10.
    发明授权
    Method for coating a rubber wiper blade 有权
    橡胶刮水片涂布方法

    公开(公告)号:US06287642B1

    公开(公告)日:2001-09-11

    申请号:US09424729

    申请日:2000-03-14

    IPC分类号: C23C16513

    摘要: 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.

    摘要翻译: 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。