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    HYDROXYMETHYLIMIDAZODIAZEPINES AND THEIR ESTERS
    5.
    发明专利
    HYDROXYMETHYLIMIDAZODIAZEPINES AND THEIR ESTERS 未知

    公开(公告)号：CA2209424A1

    公开(公告)日：1996-07-11

    申请号：CA2209424

    申请日：1996-01-03

    Applicant: HOFFMANN LA ROCHE

    Inventor： BUETTELMANN BERND ,  GERECKE MAX ,  BORER RENE ,  SZENTE ANDRE

    IPC: A61K31/55 ,  A61P21/02 ,  A61P25/20 ,  C07D487/04 ,  C07D495/14

    Abstract: The invention pertains to hydroxymethylimidazodiazepines of general formula (I) and their esters. These compounds can be used as anxiolytic and/or anticonvulsive and/or muscle-relaxing and/or sedative hypnotic agents. In formula (I), A together with the two carbon atoms designated as .alpha. and .beta. is one of the radicals (A1), (A2) or (A3); R1 is hydrogen or lower alkanoyl; R2 is phenyl, o-halophenyl or 2-pyridyl; R3 is hydrogen, lower alkyl, methylaminomethyl, allylaminomethyl or diethylaminomethyl; R4 is halogen, CF3 or nitro; R5 is hydrogen or halogen.

    Imidazodiazepines
    6.
    发明专利
    Imidazodiazepines 未知

    公开(公告)号：AU655472B2

    公开(公告)日：1994-12-22

    申请号：AU1823492

    申请日：1992-06-12

    Applicant: HOFFMANN LA ROCHE

    Inventor： BORER RENE ,  GASSNER WALTER ,  GERECKE MAX ,  KYBURZ EMILIO

    IPC: A61K31/55 ,  A61K20060101 ,  A61K31/33 ,  A61K31/38 ,  A61K31/395 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  C07D20060101 ,  C07D487/04 ,  C07D487/12 ,  C07D487/14 ,  C07D495/14 ,  C07D495/22

    Abstract: The novel imidazodiazepine derivatives of the general formula in which A, together with the two carbon atoms marked by alpha and beta , denotes one of the groups B denotes one of the radicals Q denotes one of the groups R denotes a lower alkyl group which is optionally substituted by hydroxyl, lower alkoxy, aryl, C3-6-cycloalkyl, aroyl, aryloxy, heteroaroyloxy, acyloxy, aryl-(lower) alkoxy, halogen, the group -NR R or a five-membered heterocycle bonded via a carbon or a nitrogen atom, or denotes a lower alkenyl or alkynyl group, an aroyl group, a five-membered heterocycle bonded via a carbon atom or C3-6-cycloalkyl which is optionally substituted by acyl or lower alkyl, R and R each denote hydrogen, halogen or lower alkyl, R denotes hydrogen or lower alkyl, R denotes hydrogen, aryl, acyl, C3-6-cycloalkyl, aralkoxycarbonyl or lower alkyl which is optionally substituted by aryl, morpholino, lower alkoxy, hydroxyl, 2,2-dimethyl-1,3-dioxolan-4-yl, alkoxycarbonyl, carbamoyl, alkoxycarbonylamino, aralkoxycarbonyl or amino or R and R , together with the nitrogen atom, either denote phthalimido or a six-membered saturated heterocycle, can be used for the control or prevention of diseases. They are particularly suitable for the control or prevention of epileptic attacks, anxiety, tension and excitation states, sleep disorders, schizophrenia symptoms, hepatic encephalopathy and senile dementia, and also partially or completely to antagonise undesired side effects of substances acting on the benzodiazepine receptor after overdosage or after use thereof in intensive medicine and in anaesthesia.

    PROCESS FOR THE PRODUCTION OF IMIDAZO-DIAZEPINES
    10.
    发明专利
    PROCESS FOR THE PRODUCTION OF IMIDAZO-DIAZEPINES 未知

    公开(公告)号：HU9201929D0

    公开(公告)日：1992-08-28

    申请号：HU9201929

    申请日：1992-06-10

    Applicant: HOFFMANN LA ROCHE

    Inventor： BORER RENE ,  GASSNER WALTER ,  GERECKE MAX ,  KYBURZ EMILIO

    IPC: A61K31/55 ,  A61K20060101 ,  A61K31/33 ,  A61K31/38 ,  A61K31/395 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  C07D20060101 ,  C07D487/04 ,  C07D487/12 ,  C07D487/14 ,  C07D495/14 ,  C07D495/22

    Abstract: The novel imidazodiazepine derivatives of the general formula in which A, together with the two carbon atoms marked by alpha and beta , denotes one of the groups B denotes one of the radicals Q denotes one of the groups R denotes a lower alkyl group which is optionally substituted by hydroxyl, lower alkoxy, aryl, C3-6-cycloalkyl, aroyl, aryloxy, heteroaroyloxy, acyloxy, aryl-(lower) alkoxy, halogen, the group -NR R or a five-membered heterocycle bonded via a carbon or a nitrogen atom, or denotes a lower alkenyl or alkynyl group, an aroyl group, a five-membered heterocycle bonded via a carbon atom or C3-6-cycloalkyl which is optionally substituted by acyl or lower alkyl, R and R each denote hydrogen, halogen or lower alkyl, R denotes hydrogen or lower alkyl, R denotes hydrogen, aryl, acyl, C3-6-cycloalkyl, aralkoxycarbonyl or lower alkyl which is optionally substituted by aryl, morpholino, lower alkoxy, hydroxyl, 2,2-dimethyl-1,3-dioxolan-4-yl, alkoxycarbonyl, carbamoyl, alkoxycarbonylamino, aralkoxycarbonyl or amino or R and R , together with the nitrogen atom, either denote phthalimido or a six-membered saturated heterocycle, can be used for the control or prevention of diseases. They are particularly suitable for the control or prevention of epileptic attacks, anxiety, tension and excitation states, sleep disorders, schizophrenia symptoms, hepatic encephalopathy and senile dementia, and also partially or completely to antagonise undesired side effects of substances acting on the benzodiazepine receptor after overdosage or after use thereof in intensive medicine and in anaesthesia.

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