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11 条记录 (耗时 0.062 秒)

    PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2
    10.
    发明申请
    PYRAZOLOPYRIDINES AS INHIBITORS OF THE KINASE LRRK2 审中-公开

    公开(公告)号：US20130267513A1

    公开(公告)日：2013-10-10

    申请号：US13697878

    申请日：2011-05-16

    申请人： Brayn Chan ,  Anthony Estrada ,  Zachary Sweeney ,  Edward Giles Mciver ,  Stephen Lewis

    发明人： Brayn Chan ,  Anthony Estrada ,  Zachary Sweeney ,  Edward Giles Mciver ,  Stephen Lewis

    IPC分类号： A61K31/437 ,  A61K31/5377 ,  A61K31/506 ,  C07D471/04

    CPC分类号： A61K31/437 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D471/04

    摘要： A compound of formula Ia or formula Ib, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; -0-C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; Q is CN, halogen, or is selected from C1-6-alkyl, C3-7-cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with one or more substituents A; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7-heterocycloalkyl and halogen, wherein said C1-6-alkyl, Cz-B-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-heterocycloalkyl ring; each R6 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; each R7 is selected from hydrogen, optionally substituted C1-6-alkyl and C3-7-cycloalkyl; each of R8 and R9 is independently hydrogen or optionally substituted C1-6-alkyl; or R8 and R9 together with the N to which they are attached form a C4-6-heterocycloalkyl; each R10 is selected from C3-7-cycloalkyl and optionally substituted C1-6-alkyl; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6-alkyl-C3-7-cycloalkyl, C4-7-heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted; A is selected from halogen, —NR4S02R5, —CN, —OR6, —NR4R5, —NR7R11, hydroxyl, —CF3, —CONR4R5, —NR4COR5, —NR7(CO)NR4R5, —N02, —C02H, —C02R6, —S02R6, —S02NR4R5, —NR4COR5, —NR4COOR5, 6-alkyl and —COR6. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formulae Ia and Ib.