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    • 4. 发明申请
    • Screening method and anti-tumor drug candidate obtained therefrom
    • 从其获得的筛选方法和抗肿瘤药物候选物
    • US20060057649A1
    • 2006-03-16
    • US10494989
    • 2003-07-22
    • Stuart MaudsleyRobert Millar
    • Stuart MaudsleyRobert Millar
    • G01N33/574
    • G01N33/74C07K14/72G01N2333/72G01N2500/00
    • A method for identifying a test compound that has an anti-tumoral effect whilst not significantly activating unrelated transduction signals, the method comprising the steps of: (a) selecting at least one test compound; (b) assaying the compound for anti-tumoral effect; (c) selecting at least one distinct intracellular event which is modulated, at least partially, by the GnRH receptor; (d) testing for the ability of said test compound not to modulate the selected intracellular event; and (e) selecting the test compound which selectively demonstrates an anti-tumoral effect and does not modulate said other selected intracellular event. A method according to any one of the preceding claims, the method comprising: (a) selecting at least one test compound; (b) determining whether the test compound activates signalling via Gαi; (d) testing for the ability of said test compound not to modulate signalling via Gαq; and (e) selecting the test compound which selectively activates signalling via Gαi and does not modulate signalling via Gαq. Compounds selected by the methods, including Ac-D-Nal(2)-D-4-ClPhe-D-Pal-Ser-1-MePal-D-IsopropylLys-Leu-IsopropylLys-Pro-D-AlaNH2, are useful in combating cancer and reproductive tissue hyperplasias.
    • 一种用于鉴定具有抗肿瘤作用而不显着激活不相关的转导信号的测试化合物的方法,所述方法包括以下步骤:(a)选择至少一种测试化合物; (b)测定该化合物的抗肿瘤作用; (c)选择至少部分由GnRH受体调节的至少一个不同的细胞内事件; (d)测试所述测试化合物不调节选择的细胞内事件的能力; 和(e)选择选择性地显示抗肿瘤作用并且不调节所述其它选择的细胞内事件的测试化合物。 6.根据前述权利要求中任一项所述的方法,所述方法包括:(a)选择至少一种测试化合物; (b)确定测试化合物是否通过Galphai激活信号传导; (d)测试所述测试化合物不通过Galphaq调节信号传导的能力; 和(e)选择通过Galphai选择性激活信号传导并且不通过Galphaq调节信号传导的测试化合物。 通过方法选择的化合物,包括Ac-D-Nal(2)-D-4-ClPhe-D-Pal-Ser-1-MePal-D-IsopropylLys-Leu-异丙基-Lys-Pro-D-AlaNH 2 / SUB>可用于对抗癌症和生殖组织增生。
    • 7. 发明授权
    • Gear box idle lubrication system
    • 齿轮箱怠速润滑系统
    • US5031725A
    • 1991-07-16
    • US447178
    • 1989-12-01
    • Robert Millar
    • Robert Millar
    • F16H57/04F16N7/36
    • F16N7/36F16H57/0434F16N2210/12
    • In order to provide lubrication of the bearings (16) and clutch (22) of an output shaft (14), even when the output shaft (14) is driven externally, a gear box (10) has a primary lubrication system (24) for circulating a lubricant (26) from a sump (28) into a lubricating flow path (30). The lubricating flow path (30) extends into and through a cavity (20) containing the bearings (16) and clutch (22) which support the output shaft (14) which is selectively operably interconnectable with a rotary input (12) and the primary lubrication system (24) is operable only with the rotary input (12). In addition to the primary lubrication system (24) for circulating the lubricant (26) from the sump (28) into the lubricating flow path (30), and to ensure lubrication whenever the output shaft (14) rotates, the output shaft (14) includes a pump (32) at one end of the lubricating flow path (30 ) to draw lubricant (26) from the sump (28) to lubricate the bearings (16) and clutch (22) and the pump (32) is adapted to return the lubricant (26) to the sump (28).
    • 为了提供输出轴(14)的轴承(16)和离合器(22)的润滑,即使当输出轴(14)从外部被驱动时,齿轮箱(10)具有主润滑系统(24) 用于将润滑剂(26)从贮槽(28)循环到润滑流路(30)中。 润滑流动路径(30)延伸进入并穿过包含支撑输出轴(14)的轴承(16)和离合器(22)的空腔(20),离合器(22)选择性地可操作地与旋转输入(12)相互连接,并且主要 润滑系统(24)仅可与旋转输入(12)一起操作。 除了用于将润滑剂(26)从贮槽(28)循环到润滑流路(30)中的主润滑系统(24)之外,并且当输出轴(14)旋转时确保润滑,输出轴(14) )包括在润滑流路(30)的一端处的泵(32),用于从贮槽(28)吸取润滑剂(26)以润滑轴承(16)和离合器(22),并且泵(32)适于 以将润滑剂(26)返回到贮槽(28)。