Pharmaceutically Active Diazepanes
    1.
    发明申请
    Pharmaceutically Active Diazepanes 审中-公开
    药用活性二氮杂环庚烷

    公开(公告)号:US20080300237A1

    公开(公告)日:2008-12-04

    申请号:US11911876

    申请日:2006-04-19

    IPC分类号: A61K31/551 C07D243/08

    摘要: Leukocyte Function-Associated Antigen One (LFA-1) is a cell adhesion molecule selectively expressed on leukocytes, and plays a major role in the activation and trafficking of T lymphocytes in the tissue at sites of inflammation. In the last decade a large body of preclinical data has accumulated to establish the importance of LFA-1 as a biological target, 10 particularly in chronic, T-cell driven inflammatory conditions. The present invention provides pharmaceutically active 1,4-diazepan-2-ones of formula I useful for the treatment of conditions related to LFA-1 activity.

    摘要翻译: 白细胞功能相关抗原一(LFA-1)是在白细胞上选择性表达的细胞粘附分子,在炎症部位组织中T淋巴细胞的活化和运输中起主要作用。 在过去十年中,积累了大量临床前数据,以确定LFA-1作为生物靶标的重要性,特别是在慢性,T细胞驱动的炎症病症中。 本发明提供可用于治疗与LFA-1活性相关的病症的式I的药学活性的1,4-二氮杂环庚烷-2-酮。

    Cermide Kinase Modulation
    8.
    发明申请
    Cermide Kinase Modulation 审中-公开
    金属激酶调制

    公开(公告)号:US20090170914A1

    公开(公告)日:2009-07-02

    申请号:US12295375

    申请日:2007-03-28

    IPC分类号: A61K31/423 C07D277/82

    CPC分类号: C07D277/82

    摘要: A compound of formula (I) wherein R1 is a straight chain, branched or cyclic aliphatic, aromatic or heterocyclyl group comprising at least 8 carbon atoms, e.g. 8 to 22, R2 is a straight chain, branched or cyclic aliphatic, aromatic or heterocyclic group comprising from 1 to 12 carbon atoms, and ring A is heterocycyl, fused with the phenyl ring to which ring A is attached comprising 5 or 6 ring members, and 1 to 4 heteroatoms selected from N, S, O; wherein certain compounds are excluded by proviso and the use of such compounds without proviso as pharmaceuticals in disorders which are mediated by ceramide kinase.

    摘要翻译: 式(I)的化合物,其中R 1是包含至少8个碳原子的直链,支链或环状脂族,芳族或杂环基,例如 8至22中,R 2是包含1至12个碳原子的直链,支链或环状脂族,芳族或杂环基团,并且环A是杂环基,与环A连接的苯环稠合,包含5或6个环成员 和1至4个选自N,S,O的杂原子; 其中某些化合物被排除在条件之外,并且在没有附带条件下使用这些化合物作为由神经酰胺激酶介导的病症中的药物。