Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors.
    1.
    发明申请
    Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors. 审中-公开
    三环化合物作为代谢型谷氨酸受体的变构调节剂。

    公开(公告)号:US20130210807A1

    公开(公告)日:2013-08-15

    申请号:US13809579

    申请日:2011-07-09

    摘要: The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3′ are —H or methyl, or R3 and R3 taken together form a double bond, or R3′ is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.

    摘要翻译: 本发明描述并要求结构式I,结构式II或结构式III的化合物:其中R1,R2,R3和R3'是-H或甲基,或R3和R3一起形成双键,或R3 '是-H并且R 2和R 3一起形成螺环丙基取代基,R 4是-H或-F,且R 5是-H,甲基,-C 1或-Br,其中R 1是-H,乙基, 异丙基 - ,环丙基 - ,甲基或甲氧基 - ,R 4为-H或-F,“Y”为:(a)-CH 2 - ; (b)-CR6H-0-CR7R8-,其中R6,R7和R8独立地是-H或甲基; (c)-CR 6 H-N(R 9)-CR 7 R 8 - ,其中R 6,R 7和R 8独立地为-H或甲基; (d)-CH 2 -C(R 9)(R 10)-C(R 7)(R 8) - ,其中R 7,R 8,R 9和R 10独立地为-H或 - 甲基,或者R 7和R 8均为-F,R 9和 R 10独立地是-H或 - 甲基,或者R 9和R 10都是-F,或者R 9和R 10一起是(0 =),它们与它们所连接的碳一起形成羰基。