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    Thiazole Compounds and Their Use as PGD2 Antagonists
    1.
    发明申请
    Thiazole Compounds and Their Use as PGD2 Antagonists 审中-公开
    噻唑化合物及其用作PGD2拮抗剂

    公开(公告)号：US20090221604A1

    公开(公告)日：2009-09-03

    申请号：US12065756

    申请日：2006-09-08

    申请人： Neil Victor Harris ,  George Hynd ,  Sophie Gardan

    发明人： Neil Victor Harris ,  George Hynd ,  Sophie Gardan

    IPC分类号： A61K31/496 ,  C07D417/04 ,  A61P35/00 ,  A61P17/00 ,  A61P11/06

    CPC分类号： C07D277/42 ,  C07D277/56 ,  C07D417/04

    摘要： A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O)n, where n=0, 1, or 2; L represents a direct bond, or an optionally substituted alkylene or alkenylene group; R1 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; R2 represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(═O)NHSO2Y or SO2NHC(═O)Y; and Y represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; or a N-oxide, pharmaceutically acceptable salt, solvate or prodrug thereof.

    摘要翻译： 用作PGD 2拮抗剂的化合物是结构式[1]，其中：A表示含有一个或两个氮原子的完全饱和或部分不饱和的单环5-7元环; B表示直接键，任选取代的亚甲基，任选取代的氮原子，氧或S（O）n，其中n = 0,1或2; L表示直接键或任选取代的亚烷基或亚烯基; R 1表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; R 2表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基 - 稠合环烷基; X表示羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺，磺酸或式C（-O）NHSO 2 Y或SO 2 NHC（-O）Y的基团; 并且Y表示任选取代的芳基或杂芳基或任选取代的烷基或环烷基; 或其N-氧化物，药学上可接受的盐，溶剂合物或前药。

    PYRROLO[1,2-A]QUINOXALINE DERIVATIVES AS ADENOSINE A3 RECEPTOR MODULATORS AND USES THEREOF
    2.
    发明申请
    PYRROLO[1,2-A]QUINOXALINE DERIVATIVES AS ADENOSINE A3 RECEPTOR MODULATORS AND USES THEREOF 审中-公开
    作为腺苷A3受体调节剂的吡咯并[1,2-A]喹啉衍生物及其用途

    公开(公告)号：US20090093476A1

    公开(公告)日：2009-04-09

    申请号：US12158035

    申请日：2006-12-19

    申请人： Stephan Schann ,  Stanislas Mayer ,  Sophie Gardan

    发明人： Stephan Schann ,  Stanislas Mayer ,  Sophie Gardan

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P1/00 ,  A61P37/00 ,  A61K31/5377

    CPC分类号： C07D487/04

    摘要： The present invention provides new compounds displaying high affinity for adenosine A3 receptors. It also provides modulators of adenosine A3 receptors. It further provides compounds for the treatment and/or prophylaxis of conditions and diseases where adenosine A3 receptor plays a role. Pharmaceutical compositions for the treatment and/or prophylaxis of conditions and diseases where adenosine A3 receptors play a role are also described.

    摘要翻译： 本发明提供了对腺苷A3受体显示高亲和力的新化合物。 它还提供了腺苷A3受体的调节剂。 它还提供用于治疗和/或预防腺苷A3受体起作用的病症和疾病的化合物。 还描述了用于治疗和/或预防腺苷A3受体起作用的病症和疾病的药物组合物。