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    IMIDAZODIAZEPINE DERIVATIVES
    71.
    发明专利
    IMIDAZODIAZEPINE DERIVATIVES 未知

    公开(公告)号：AU1271088A

    公开(公告)日：1988-09-15

    申请号：AU1271088

    申请日：1988-03-04

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO ,  MEIER MARC

    IPC: C07D487/04 ,  C07D487/14 ,  C07D487/22 ,  C07D495/14 ,  A61K31/55

    Abstract: A compound for treating disorders of the central nervous system, which is of the formula wherein A taken together with the two carbon atoms denoted by alpha and beta is one of the following groups: R1 is one of the following groups: -CH=CH-R6 (d)and -C 3BOND C-R6, (e) R2 is hydrogen, R3 is lower alkyl, or R2 and R3 together are dimethylene or trimethylene, R4 and R5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C3-C7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by gamma when R2 and R3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R6 is different from hydrogen.

    72.
    发明专利
    未知

    公开(公告)号：NO157620B

    公开(公告)日：1988-01-11

    申请号：NO820622

    申请日：1982-02-26

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO

    IPC: C07D209/38 ,  C07D265/26 ,  C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D495/22

    Abstract: There is provided compounds which exhibit pronounced anticonvulsive and anxiolytic activities of the formula I wherein A together with the two carbon atoms denoted as alpha and beta is the group (a) (b) (c) (d) B is dimethylene, trimethylene or propenylene, R1 is hydrogen, halogen, trifluoromethyl, amino, nitro, cyano or lower alkyl and R2 is hydrogen, halogen, trifluoromethyl, amino, nitro, cyano, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl, and the carbon atom denoted as gamma has the (S)-or (R,S)-configuration, and the pharmaceutically acceptable acid addition salts thereof.

    78.
    发明专利
    未知

    公开(公告)号：DK90286A

    公开(公告)日：1986-08-29

    申请号：DK90286

    申请日：1986-02-27

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO

    IPC: A61K31/55 ,  A61P25/20 ,  C07D243/00 ,  C07D333/00 ,  C07D487/14 ,  C07D495/22 ,  C07D

    Abstract: Compounds which are imidazodiazepine derivatives of the formula I wherein A together with the carbon atoms denoted by alpha and beta signifies the group one of R1 and R2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R3 and R4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by gamma , and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.

    IMIDAZODIAZEPINES
    79.
    发明专利
    IMIDAZODIAZEPINES 未知

    公开(公告)号：AU552046B2

    公开(公告)日：1986-05-22

    申请号：AU8066582

    申请日：1982-02-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO

    IPC: A61K31/55 ,  A61P33/10 ,  A61P39/02 ,  A61P43/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14

    Abstract: There is presented imidazodiazepines of the formula I wherein A together with the two carbon atoms denoted as alpha and beta is a pyridine ring, X is an oxygen or sulphur atom, R1 is hydrogen, halogen, lower alkyl, lower alkoxymethyl or the group-COOR3 and R2 and R3 each are lower alkyl, and their pharmaceutically acceptable acid addition salts. The compounds are useful in the antagonization of the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity, for example as antidotes in the case of intoxications with 1,4-benzodiazepines which have tranquillizing activity. Also presented are methods to produce such imidazodiazepines.

    IMIDAZODIAZEPINES
    80.
    发明专利
    IMIDAZODIAZEPINES 未知

    公开(公告)号：AU551891B2

    公开(公告)日：1986-05-15

    申请号：AU8066982

    申请日：1982-02-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO

    IPC: C07D209/38 ,  C07D265/26 ,  C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D495/22

    Abstract: There is provided compounds which exhibit pronounced anticonvulsive and anxiolytic activities of the formula I wherein A together with the two carbon atoms denoted as alpha and beta is the group (a) (b) (c) (d) B is dimethylene, trimethylene or propenylene, R1 is hydrogen, halogen, trifluoromethyl, amino, nitro, cyano or lower alkyl and R2 is hydrogen, halogen, trifluoromethyl, amino, nitro, cyano, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl, and the carbon atom denoted as gamma has the (S)-or (R,S)-configuration, and the pharmaceutically acceptable acid addition salts thereof.

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