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    Phenylalanine Enamide Derivatives
    97.
    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。

    SPIRO 2,4 PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
    98.
    发明申请
    SPIRO 2,4 PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES 有权
    SPIRO 2,4吡啶二胺化合物及其用途

    公开(公告)号：US20090062270A1

    公开(公告)日：2009-03-05

    申请号：US12260886

    申请日：2008-10-29

    申请人： Robin Cooper ,  Rajinder Singh ,  Jeffrey Clough

    发明人： Robin Cooper ,  Rajinder Singh ,  Jeffrey Clough

    IPC分类号： A61K31/538 ,  A61P37/00

    CPC分类号： C07D239/48 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

    摘要翻译： 本发明提供了用螺噻嘧啶二胺化合物治疗或预防自身免疫疾病的方法，以及治疗，预防或改善与这些疾病相关的症状的方法。 可以用化合物治疗或预防的自身免疫性疾病的具体实例包括类风湿性关节炎和/或其相关症状，系统性红斑狼疮和/或其相关症状和多发性硬化症和/或其相关症状。