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    Phenylalanine enamide derivatives
    27.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号：US07122556B2

    公开(公告)日：2006-10-17

    申请号：US10947032

    申请日：2004-09-22

    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： 描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R 1是基团Ar 1，L 2，Ar 2， > Alk-其中：Ar 1是任选取代的芳族或杂芳族基团; L 2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; 和Alk是其中R是羧酸（-CO 2 H 2 H）或其衍生物或生物固体的链; X是-O-或-S-原子或-N（R 2）基团，其中：R x，R y和 R“可以相同或不同，各自为氢原子或任选的取代基; 或R z是如前所定义的原子或基团，并且R x和R y连接在一起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。