Compound having GPR54 agonistic activity
    1.
    发明授权
    Compound having GPR54 agonistic activity 有权
    具有GPR54激动作用的化合物

    公开(公告)号:US08183212B2

    公开(公告)日:2012-05-22

    申请号:US12298200

    申请日:2006-10-24

    CPC分类号: C07K5/0808 A61K38/00 C07K7/06

    摘要: The present invention provides a compound represented by the following formula (1); wherein R1 is an aryl group etc.; R2 is —CO—NH— etc.; R3 is a methyl group having an aromatic group or a cycloalkyl group; R4 is a hydrogen atom etc.; R5 is a methyl group having an aromatic group; and R6 is an amino group or an N-alkyl substituted amino group, having a low-molecular weight and a superior GPR54 agonist activity, and a pharmaceutical composition containing the compound.

    摘要翻译: 本发明提供由下式(1)表示的化合物。 其中R1是芳基等; R2是-CO-NH-等; R3是具有芳基或环烷基的甲基; R4是氢原子等。 R5是具有芳基的甲基; 和R6是具有低分子量和优异的GPR54激动剂活性的氨基或N-烷基取代的氨基,以及含有该化合物的药物组合物。

    METASTIN DERIVATIVE AND USE THEREOF
    3.
    发明申请
    METASTIN DERIVATIVE AND USE THEREOF 有权
    衍生物及其用途

    公开(公告)号:US20110039786A1

    公开(公告)日:2011-02-17

    申请号:US12990161

    申请日:2009-04-28

    摘要: The present invention provides a metastin derivative represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition containing it. The metastin derivative or a salt thereof is superior in blood stability, and has a cancer metastasis suppressive action or cancer growth suppressive action.

    摘要翻译: 本发明提供由式(I)表示的亚氨基衍生物:其中每个符号如说明书中所定义,或其盐或含有它的药物组合物。 所述转氨酶衍生物或其盐具有优异的血液稳定性,具有癌转移抑制作用或癌生长抑制作用。

    NOVEL COMPOUND HAVING GPR54 AGONISTIC ACTIVITY
    4.
    发明申请
    NOVEL COMPOUND HAVING GPR54 AGONISTIC ACTIVITY 有权
    具有GPR54激活活性的新化合物

    公开(公告)号:US20100160241A1

    公开(公告)日:2010-06-24

    申请号:US12298200

    申请日:2006-10-24

    CPC分类号: C07K5/0808 A61K38/00 C07K7/06

    摘要: The present invention provides a compound represented by the following formula (1); wherein R1 is an aryl group etc.; R2 is —CO—NH— etc.; R3 is a methyl group having an aromatic group or a cycloalkyl group; R4 is a hydrogen atom etc.; R5 is a methyl group having an aromatic group; and R6 is an amino group or an N-alkyl substituted amino group, having a low-molecular weight and a superior GPR54 agonist activity, and a pharmaceutical composition containing the compound.

    摘要翻译: 本发明提供由下式(1)表示的化合物。 其中R1是芳基等; R2是-CO-NH-等; R3是具有芳基或环烷基的甲基; R4是氢原子等。 R5是具有芳基的甲基; 和R6是具有低分子量和优异的GPR54激动剂活性的氨基或N-烷基取代的氨基,以及含有该化合物的药物组合物。

    Metastin derivatives and their use
    6.
    发明授权
    Metastin derivatives and their use 有权
    Metastin衍生物及其用途

    公开(公告)号:US06800611B2

    公开(公告)日:2004-10-05

    申请号:US10337105

    申请日:2003-01-06

    IPC分类号: A61K3807

    CPC分类号: C07K5/1016 A61K38/00

    摘要: The invention relates to metastin derivatives represented by the formula: X-AA1-AA2-AA3-AA4-Z (I), or a salt thereof, or a pro-drug thereof, which have cancer metastatis suppressing activity and cancer proliferation suppressing activity. The invention also relates to the use of these derivatives as drugs for preventing or treating cancers.

    摘要翻译: 本发明涉及具有癌症转移抑制活性和癌细胞增殖抑制活性的由式​​X-AA1-AA2-AA3-AA4-Z(I)表示的亚铁蛋白衍生物或其盐或其前体药物。 本发明还涉及这些衍生物作为预防或治疗癌症的药物的用途。

    Optical diffusion film
    9.
    发明授权
    Optical diffusion film 有权
    光扩散膜

    公开(公告)号:US08917452B2

    公开(公告)日:2014-12-23

    申请号:US13080822

    申请日:2011-04-06

    IPC分类号: G02B5/02 G02F1/1335

    摘要: Measurement reference lengths of length and width are set with respect to a convex structure, and an average of vertical distances between tip points and bottom points inside a measurement reference area is calculated as an average height. An average of horizontal distances between the tip points and bottom points is calculated as an average distance. A value obtained by dividing the average height by the average distance provides a gradient ratio. An inverse tangent of the gradient ratio provides an average gradient angle. When the average gradient angle ranges from 5 degrees to 15 degrees and a standard deviation of average gradient angle ranges from 30% to 40% of the average gradient angle, a regular reflectance at a regular reflection angle with respect to incident light of an angle of 30 degrees from a normal direction of the film surface is 1% or less.

    摘要翻译: 长度和宽度的测量参考长度相对于凸形结构设置,并且将测量参考区域内的尖点和底点之间的垂直距离的平均值计算为平均高度。 平均距离计算出尖点和底点之间的水平距离的平均值。 通过将平均高度除以平均距离而获得的值提供了梯度比。 梯度比的反正切提供平均梯度角。 当平均梯度角为5度至15度,平均梯度角的标准偏差范围为平均梯度角的30%至40%时,相对于角度为 从膜表面的法线方向30度为1%以下。

    Macrocyclic Sh2 Domain Binding Inhibitors
    10.
    发明申请
    Macrocyclic Sh2 Domain Binding Inhibitors 审中-公开
    大环Sh2结构域结合抑制剂

    公开(公告)号:US20080139456A1

    公开(公告)日:2008-06-12

    申请号:US11575723

    申请日:2005-09-30

    IPC分类号: A61K38/12 C07K5/12

    摘要: Disclosed are compounds for inhibiting the binding of an SH2 domain-containing protein, for example, a compound of formula (I): FORMULA (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is, for example, hydrogen, azido, amino, oxalylamino, carboxy alkyl, alkoxycarbonyl alkyl, aminocarbonyl alkyl, or alkyl carbonylamino; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof. Also disclosed are pharmaceutical compositions and methods of use of such compounds.

    摘要翻译: 公开了用于抑制含SH2结构域的蛋白质,例如式(I)的化合物:式(I)的化合物:其中R1是亲油性物质; R2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R3是例如氢,叠氮基,氨基,草酰氨基,羧基烷基,烷氧基羰基烷基,氨基羰基烷基或烷基羰基氨基; R6是连接体; AA是氨基酸; n为1〜6; 或其药学上可接受的盐,立体异构体,溶剂合物或水合物。 还公开了药物组合物和这些化合物的使用方法。