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    • 2. 发明申请
    • Macrocyclic diaminopropanes as beta-secretase inhibitors
    • 大环二氨基丙烷作为β-分泌酶抑制剂
    • US20070037868A1
    • 2007-02-15
    • US11501328
    • 2006-08-09
    • Lawrence MarcinAndrew Good
    • Lawrence MarcinAndrew Good
    • A61K31/4025C07D413/02
    • C07D413/04
    • There is provided a series of novel macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5, n, L, Z, and as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    • 提供了一系列式(I)的新型大环二氨基丙烷或立体异构体; 或其药学上可接受的盐,其中R 1,R 2,R 4,R 5,n, L,Z和如本文所定义的其药物组合物和使用方法。 这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白(APP)的加工,更具体地,抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物,例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
    • 5. 发明授权
    • Color picture tube shadow mask having improved mask aperture pattern
    • 彩色显像管荫罩具有改进的面罩孔径图案
    • US5583391A
    • 1996-12-10
    • US558314
    • 1995-11-15
    • Andrew GoodBruce G. Marks
    • Andrew GoodBruce G. Marks
    • H01J29/07H01J31/20H01J29/80
    • H01J29/076
    • A color picture tube has a rectangular shadow mask mounted therein in spaced relation to a viewing screen. A major axis passes through the center of the mask and parallels the long sides thereof and a minor axis passes through the center of the mask and parallels the short sides thereof. The mask has an aperture array that includes slit-shaped apertures aligned in columns that essentially parallel the minor axis and end at a border of the aperture array. Adjacent apertures in each column are separated by tie bars in the mask that are longitudinally offset from column to adjacent column. The spacing from tie bar to tie bar in a column is the tie bar pitch at a location on the mask. A first set of the aperture columns, comprising every other column, has full length ultimate apertures at least at one end thereof, and a second set of the aperture columns, comprising every other column not in the first set, has partial length ultimate apertures at least at one end thereof. The ultimate apertures of all of the aperture columns end on smooth curved border lines. The tie bar pitch of the columns decreases from the center of the mask to the short sides thereof, with the tie bar pitch in the region of the short sides of the mask being optimized to minimize moire at the sides of the screen during tube operation. The tie bar pitch along each column varies also from the center of the mask to the long sides of the mask.
    • 彩色显象管具有安装在其中的与观看屏隔开的矩形荫罩。 长轴通过掩模的中心并平行于其长边,并且短轴通过掩模的中心并平行于其短边。 掩模具有孔径阵列,其包括在基本上平行于短轴并且在孔阵列的边界处终止的列中对齐的狭缝形孔。 每个柱中的相邻孔由掩模中由柱相邻的柱纵向偏移的连接条分开。 柱中的连杆与连杆之间的距离是在面罩上的位置处的连杆间距。 包括每隔一列的第一组孔径列至少在其一端具有全长极限孔,并且包括不在第一组中的每隔一列的第二组孔列具有部分长度的极限孔, 至少在一端。 所有孔径柱的最终孔径在平滑的弯曲边界线上终止。 柱的连接杆间距从掩模的中心减小到其短边,并且掩模的短边区域中的拉杆间距被优化以使侧面的莫尔+ E,acu + EE最小化 在管操作期间的屏幕。 沿着每一列的连接杆间距也从掩模的中心到掩模的长边也变化。
    • 6. 发明授权
    • Method of making color picture tube shadow mask having improved tie bar
locations
    • 制造具有改进的连杆位置的彩色显像管荫罩的方法
    • US5000711A
    • 1991-03-19
    • US547004
    • 1990-07-02
    • Bruce G. MarksAndrew Good
    • Bruce G. MarksAndrew Good
    • H01J9/14
    • H01J9/142
    • An improved method of making a color picture tube shadow mask includes first constructing an apertured flat mask which is formed into a domed contoured mask. The mask has a rectangular periphery with two long sides and two short sides. The mask has a major axis, which passes through the center of the mask and parallels the long sides, and a minor axis, which passes through the center of the mask and parallels said short sides. The mask includes slit-shaped apertures aligned in columns that essentially parallel the minor axis. Adjacent apertures in each column are separated by tie bars in the mask, with the spacing between tie bars in a column being the tie bar pitch at a particular location on the mask. The improvement comprises a first step of calculating the desired tie bar shadow locations at several discrete areas, for a given scan line pitch, as viewed from a distance in front of a viewing screen of a tube. The desired tie bar shadow locations are those locations that will give an optimized compromise for moire at each of the discrete areas. Next, the corresponding tie bar shadow locations on the screen are determined, taking into account the angles of the screen slope at the discrete areas. The corresponding tie bar pitches are then determined on a formed contoured shadow mask, taking into account the mask to screen spacing at each of the discrete areas. Then, the tie bar pitches on the unformed flat mask are calculated, by subtracting the stretch caused by the mask formign step. The stretch is determined by actual measurements of vertical pitch at the discrete areas on the apertured formed mask and by comparing these measurements with measurements made on the flat mask prior to forming. Finally, a least squares fitting is performed on the calculated flat mask tie bar pitches, to obtain the locations of tie bars at all areas on the flat mask.
    • 制造彩色显像管荫罩的改进方法包括首先构造形成为圆顶形轮廓掩模的有孔平面掩模。 面具具有两个长边和两个短边的矩形周边。 掩模具有长轴,其穿过掩模的中心并且平行于长边,并且短轴穿过掩模的中心并平行于所述短边。 掩模包括在基本上平行于短轴的列中对准的狭缝状孔。 每个柱中的相邻孔径由掩模中的连接条分开,柱中的连接杆之间的间距是掩模上特定位置处的连杆间距。 改进包括对于给定的扫描线间距,在从管的观察屏幕前方的距离观察时,在几个离散区域处计算期望的连接条阴影位置的第一步骤。 所需的连接条阴影位置是将为每个离散区域的莫尔条件提供优化折中的位置。 接下来,考虑到离散区域处的屏幕斜率的角度,确定屏幕上的对应的连接条影子位置。 然后在形成的轮廓的荫罩上确定对应的拉杆间距,同时考虑到每个离散区域处的屏蔽间隔。 然后,通过减去由掩模形成步骤引起的拉伸来计算未形成的平面掩模上的拉杆间距。 通过在孔形成的掩模上的离散区域处的垂直间距的实际测量并且通过将这些测量与在形成之前在平面掩模上进行的测量进行比较来确定拉伸。 最后,对所计算的平面罩连杆杆间距进行最小二乘拟合,以获得平面罩上所有区域的连杆的位置。
    • 10. 发明申请
    • Novel Compounds and Uses Thereof
    • 新型化合物及其用途
    • US20160137646A1
    • 2016-05-19
    • US14894214
    • 2014-05-30
    • Ben C. ASKEWAndrew GOODKala Pharmaceuticals, Inc.
    • Winston Zapanta OngPawel Wojciech NowakBen C. AskewAndrew Good
    • C07D487/04C07D519/00
    • C07D487/04C07D519/00
    • The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    • 本发明提供式(I) - (IV)中任一项的新化合物及其药物组合物。 还提供了包含粘液穿透的式(I) - (IV)中任一项的化合物及其药物组合物的颗粒(例如纳米颗粒)。 本发明还提供了用于使用本发明化合物及其药物组合物用于治疗和/或预防与生长因子信号传导途径的异常或病理性血管生成和/或异常信号传导相关的疾病的方法和试剂盒(例如,血管内皮生长因子 VEGF)),例如增殖性疾病(例如癌症,良性肿瘤,炎症性疾病,自身免疫性疾病)和眼部疾病(例如,黄斑变性,青光眼,糖尿病性视网膜病变,视网膜母细胞瘤,水肿,葡萄膜炎,干眼症,睑炎炎, 手术炎症)。