FLUORINE-CONTAINING AMINO ACID DERIVATIVES
    12.
    发明公开
    FLUORINE-CONTAINING AMINO ACID DERIVATIVES 有权
    FLUOR含有氨基衍生物

    公开(公告)号:EP1052246A4

    公开(公告)日:2001-11-07

    申请号:EP99901877

    申请日:1999-01-27

    CPC分类号: C07C229/50 C07C2602/18

    摘要: Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X represents hydrogen or fluorine; and R and R are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, dipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

    6-FLUOROBICYCLO 3. 1.0]HEXANE DERIVATIVES
    18.
    发明公开
    6-FLUOROBICYCLO 3. 1.0]HEXANE DERIVATIVES 有权
    6-氟[3.1.0]己烷衍生物

    公开(公告)号:EP1110943A4

    公开(公告)日:2002-07-10

    申请号:EP99931532

    申请日:1999-07-26

    摘要: Fluorobicyclo[3.1.0]hexane derivatives represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same wherein R?1 and R2¿ represent each hydrogen, alkyl, cycloalkyl, etc.; and Y?1 and Y2¿ represent each hydrogen, alkylthio, cycloalkylthio, alkoxy, etc., or one of Y?1 and Y2¿ represents hydrogen and the other represents hydroxy, alkoxy, cycloalkoxy, etc., or Y?1 and Y2¿ together represent oxygen or -X(CH¿2?)nX- (wherein X represents oxygen or sulfur; and n is 2 or 3). These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists, in treating and preventing psychiatric disorders such as schizophrenia, anxiety, depression and bipolar disturbance, and neurologic diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's disease, Parkinson's disease, movement disorder in association with muscular rigidity, brain ischemia, brain insufficiency, spinal cord lesion and head disorder.

    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES
    19.
    发明公开
    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES 失效
    4-四氢吡啶基嘧啶衍生物

    公开(公告)号:EP0976745A4

    公开(公告)日:2001-11-28

    申请号:EP98911002

    申请日:1998-03-25

    摘要: 4-Tetrahydropyridylpyrimidine derivatives of general formula (I); and medicinally acceptable salts thereof, wherein Ar is phenyl optionally substituted with one to three groups selected from among halogeno, C1-C5 alkyl, C1-C5 alkoxy and trifluoromethyl, thienyl or furanyl; R1 is hydrogen, C¿1?-C5 alkyl or amino optionally substituted with one or two C1-C5 alkyl groups; R?2 is C¿1-C5 alkyl, C4-C7 cycloalkylalkyl, C2-C5 alkenyl or C2-C5 alkynyl; and X?1, X2 and X3¿ are each independently hydrogen, halogeno, C¿1?-C5 alkyl, C1-C5 alkoxy, C1-C5 alkylthio or amino optionally substituted with one or two C1-C5 alkyl groups. These compounds are efficacious against diseases in which CRF is believed to be concerned, for example, melancholia, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immunologic diseases and so on.