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    Phenylalanine Enamide Derivatives
    8.
    发明申请
    Phenylalanine Enamide Derivatives 失效
    苯丙氨酸酰胺衍生物

    公开(公告)号：US20090105291A1

    公开(公告)日：2009-04-23

    申请号：US12327311

    申请日：2008-12-03

    申请人： Stephen Brand ,  Stuart Bailey ,  Julien A. Brown ,  James A. Johnson ,  John R. Porter ,  John C. Head

    发明人： Stephen Brand ,  Stuart Bailey ,  Julien A. Brown ,  James A. Johnson ,  John R. Porter ,  John C. Head

    IPC分类号： A61K31/44 ,  C07D213/72 ,  C07D471/04 ,  A61K31/4545 ,  A61P29/00 ,  A61K31/4439 ,  A61K31/4375 ,  C07D401/02

    CPC分类号： C07D213/81 ,  C04B35/632 ,  C07C229/10 ,  C07C229/46 ,  C07C233/81 ,  C07C233/82 ,  C07C323/30 ,  C07C2601/04 ,  C07C2603/94 ,  C07C2603/96 ,  C07D213/79 ,  C07D213/89 ,  C07D311/96 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

    摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译： 描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R1是基团Ar1 L2Ar2Alk-，其中：Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH（R） - ， - CH-C（R） - 或其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    9.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号：US07501437B2

    公开(公告)日：2009-03-10

    申请号：US11692612

    申请日：2007-03-28

    申请人： Stephen Brand ,  Stuart Bailey ,  Julien A. Brown ,  James A. Johnson ,  John R. Porter ,  John C. Head

    发明人： Stephen Brand ,  Stuart Bailey ,  Julien A. Brown ,  James A. Johnson ,  John R. Porter ,  John C. Head

    IPC分类号： C07D471/04 ,  A61K31/4375

    CPC分类号： C07D213/81 ,  C04B35/632 ,  C07C229/10 ,  C07C229/46 ,  C07C233/81 ,  C07C233/82 ,  C07C323/30 ,  C07C2601/04 ,  C07C2603/94 ,  C07C2603/96 ,  C07D213/79 ,  C07D213/89 ,  C07D311/96 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

    摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk—in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译： 描述式（1）的苯丙氨酸烯酰胺衍生物：其中R1是Ar1L2Ar2Alk基团，其中：Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Methods and systems for identifying signals-of-interest
    10.
    发明授权
    Methods and systems for identifying signals-of-interest 有权
    用于识别感兴趣信号的方法和系统

    公开(公告)号：US06867728B1

    公开(公告)日：2005-03-15

    申请号：US10701473

    申请日：2003-11-06

    申请人： Craig A. Hanna ,  James A. Johnson

    发明人： Craig A. Hanna ,  James A. Johnson

    IPC分类号： G01S7/02 ,  G01S13/00

    CPC分类号： G01S7/021

    摘要： Signals-of-interest are identified by distinguishing such signals from signals constituting environmental or internal receiver noise. A received signal is rapidly sampled in order to set a dynamic, system threshold. Signals above the threshold constitute signals-of-interest.

    摘要翻译： 通过将这些信号与构成环境或内部接收机噪声的信号区分开来识别兴趣信号。 为了设置动态系统阈值，快速采样接收到的信号。 高于阈值的信号构成感兴趣的信号。