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    IMIDAZODIAZEPINE DERIVATIVES
    18.
    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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