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    IMIDAZODIAZEPINES
    81.
    发明专利
    IMIDAZODIAZEPINES 未知

    公开(公告)号：AU551811B2

    公开(公告)日：1986-05-15

    申请号：AU8066682

    申请日：1982-02-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUNKELER WALTER ,  KYBURZ EMILIO

    IPC: A61K31/55 ,  A61P33/10 ,  A61P39/02 ,  A61P43/00 ,  C07D243/14 ,  C07D487/04 ,  C07D495/14

    Abstract: There is provided imidazodiazepines of the formula 1 wherein A together with the two carbon atoms denoted as alpha and beta is the group X is an oxygen or sulphur atom and R1 is hydrogen or lower alkyl, and either R2 is hydrogen, trifluoromethyl, halogen, cyano or nitro and R3 is hydrogen or R2 is hydrogen and R3 is trifluoromethyl, halogen, cyano, nitro or 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 the above imidazodiazepines.

    82.
    发明专利
    未知

    公开(公告)号：FI860587A0

    公开(公告)日：1986-02-10

    申请号：FI860587

    申请日：1986-02-10

    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.

    IMIDAZODIAZEPINE DERIVATIVES
    88.
    发明专利
    IMIDAZODIAZEPINE DERIVATIVES 未知

    公开(公告)号：CA1143728A

    公开(公告)日：1983-03-29

    申请号：CA360028

    申请日：1980-09-10

    Applicant: HOFFMANN LA ROCHE

    Inventor： GERECKE MAX ,  HAEFELY WILLY ,  HUNKELER WALTER ,  KYBURZ EMILIO ,  MOHLER HANNS ,  PIERI LORENZO ,  POLC PETAR

    IPC: A61K31/55 ,  A61K31/551 ,  A61P33/10 ,  A61P39/02 ,  C07D243/14 ,  C07D243/16 ,  C07D243/18 ,  C07D243/24 ,  C07D265/26 ,  C07D333/42 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D495/22 ,  C07D498/04 ,  C07D487/00

    Abstract: RAN 4008/306K Imidazodiazepine derivatives of the general formula I wherein A together with the two carbon atoms denoted as .alpha. and .beta. represents one of the groups and (a) (b) (c) and the dotted line represents the double bond present in groups (a) and (b), D represents ?C=0 or ?C=S, R1 represents cyano, lower alkanoyl or a group of the formula -COOR4, R4 represents methyl, ethyl, isopropyl or 2-hydroxyethyl, R5 represents hydrogen, trifluoromethyl or halogen and R6 represents hydrogen, trifluoromethyl, halogen or lower alkyl and either R2 represents hydrogen and R3 represents hydrogen or lower alkyl or R2 and R3 together represent trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are novel and are suitable for antagonising the central -depressant, muscle relaxant, ataxic, blood pressure -lowering and respiratory-depressant properties of 1,4 -benzodiazepines which have tranquillising activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzo-diazepines which have tranquillising activity participates, for shortening an anaesthesia induced by such 1,4-benzodiazepines etc. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7- -nitro-2H-1,4-benzodiazepin-2-one. The present imidazodiazepine derivatives can be manufactured according to various methods starting from partially novel starting materials and can be formulated into galenical administration forms.

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