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    Indolizine Derivatives as Ligands of the Crth2 Receptor
    2.
    发明申请
    Indolizine Derivatives as Ligands of the Crth2 Receptor 审中-公开
    吲哚啉衍生物作为Crth2受体的配体

    公开(公告)号：US20080306109A1

    公开(公告)日：2008-12-11

    申请号：US12065963

    申请日：2006-09-14

    申请人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana ,  Michael Colin Cramp ,  Trevor Keith Harrison ,  Rosa Arienzo ,  Paul Blaney ,  Yann Griffon ,  David Middlemiss

    发明人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana ,  Michael Colin Cramp ,  Trevor Keith Harrison ,  Rosa Arienzo ,  Paul Blaney ,  Yann Griffon ,  David Middlemiss

    IPC分类号： A61K31/44 ,  C07D455/02 ,  A61P43/00

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R1, R2. R3 and R4 each independently are hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1-C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1-C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl or a group —SO2R10; n is 0, 1 or 2; R5 is C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, C1-C6alkenyl, C1-C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1-C6alkyl or fully or partially fluorinated C1-C6alkyl; R7 and R8 are independently hydrogen or C1-C6alkyl, or R7 and R8 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —C(O)—, —NR6SO2— or —SO2NR6- wherein n is 0, 1 or 2.

    摘要翻译： 式（I）化合物是CRTH2拮抗剂，可用于治疗例如哮喘，慢性阻塞性肺病，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎。 式（I）其中R1，R2。 完全或部分氟化的C 1 -C 6烷基，卤素，-S（O）n R 10，-SO 2 N（R 10）2，-N（R 10）2，-C（O）N（ R 10）2，-NR 10 C（O）R 9，-CO 2 R 10，-C（O）R 9，-NO 2，-CN或-OR 11; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基或基团-SO 2 R 10; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，C 1 -C 6烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R6是氢，C1-C6烷基或完全或部分氟化的C1-C6烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或者R 7和R 8与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - C（O） - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。