BENZO [D]ISOXAZOL-3-OL DAAO INHIBITORS
    1.
    发明公开
    BENZO [D]ISOXAZOL-3-OL DAAO INHIBITORS 审中-公开
    苯并[d]异恶唑-3- OL-DAAO-INHIBITOREN

    公开(公告)号:EP1711478A2

    公开(公告)日:2006-10-18

    申请号:EP04815603.8

    申请日:2004-12-28

    申请人: Sepracor Inc.

    IPC分类号: C07D263/00

    CPC分类号: C07D261/20

    摘要: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: I wherein Z1 is N or CR3; Z2 is N or CR4; Z3 is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.

    PYRROLE AND PYRAZOLE DAAO INHIBITORS
    2.
    发明公开
    PYRROLE AND PYRAZOLE DAAO INHIBITORS 审中-公开
    吡咯和吡唑ALS抑制剂DAAO

    公开(公告)号:EP1709004A2

    公开(公告)日:2006-10-11

    申请号:EP04815792.9

    申请日:2004-12-28

    申请人: Sepracor Inc.

    IPC分类号: C07D231/54

    摘要: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof: (I) wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium , sodium , zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula (I).