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    • 6. 发明申请
    • Chemical Compounds
    • 化学化合物
    • US20080275062A1
    • 2008-11-06
    • US10597473
    • 2005-01-28
    • David Harold DrewryDavid Kendall JungJames Andrew LinnRobert Neil HunterDennis LeeRobert A. StavengerClark Sehon
    • David Harold DrewryDavid Kendall JungJames Andrew LinnRobert Neil HunterDennis LeeRobert A. StavengerClark Sehon
    • A61K31/4409C07D213/04A61K31/415C07D231/10C07D239/42A61K31/505C07D239/24C07D231/56C07D401/10
    • C07D213/56C07D231/12C07D231/56C07D239/26C07D239/42C07D403/04
    • There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-4alkyl, C1-4alkanoyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy and C1-4alkoxycarbonyl; and X is indazolyl, pyrazolyl or a group: wherein G is CH or N; and Y1 and Y2 are independently hydrogen, halogen and a group NR5R6 (wherein R5 and R6 are independently hydrogen, C1-6alkyl or C2-6alkenyl).
    • 提供式(I)化合物及其盐,溶剂化物和生理功能衍生物:其中R1是氢或C 1-6烷基; n为1,2,3或4; R2是芳基,任选地被一个或两个选自卤素,羟基,氰基,C 1-4烷基,C 1-4烷氧基,C 1-4烷基, 烷基,卤代C 1-4烷基,卤代C 1-4烷氧基,芳基,芳氧基,C 1-4烷基, 烷氧基羰基,C 1-4烷基磺酰基和基团R 3 R 4 NSO 2(其中R 3和R 4独立地是氢或C 1-4烷基 )和5-或6-元杂芳基; 或n为0,并且R 1和R 2与它们连接的氮原子一起形成5-或6-元单环杂环或9-或10-元双环杂环,其中至少含有 R 1和R 2连接的氮原子是非芳族的,其中5或6元单环杂环或9或10元双环杂环任选被一个或两个选自以下的基团取代: 卤素,羟基,氰基,氧代,C 1-4烷基,C 1-4烷酰基,C 1-4烷氧基,卤代C 1-4烷基, 烷基,卤代C 1-4烷氧基,芳基,芳氧基和C 1-4烷氧基羰基; 并且X是吲唑基,吡唑基或基团:其中G是CH或N; 和Y 1和Y 2独立地是氢,卤素和基团NR 5 R 6(其中R 5和R 6独立地是氢,C 1-6烷基 或C 2-6烯基)。