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|Title:||Thieno-1,4-diazepin-5-ones and benzo-1,4-diazepin-5-ones|
|Abstract:||Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonizing the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have transquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. 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. Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.|
|Inventor(s):||Gerecke; Max (Reinach, CH), Haefely; Willy (Reinach, CH), Hunkeler; Walter (Magden, CH), Kyburz; Emilio (Reinach, CH), Mohler; Hanns (Inzlingen, CH), Pieri; Lorenzo (Riehen, CH), Polc; Petar (Binningen, CH)|
|Assignee:||Hoffmann-La Roche Inc. (Nutley, NJ)|
|Filing Date:||Nov 16, 1981|
|Claims:||1. A compound of the formula ##STR31## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR32## the dotted line represents the double bond present in groups (a) and (b), X is halogen, alkylthio, aralkylthio, N-nitrosoalkylamino, alkoxy, mercapto, ##STR33## wherein R.sup.4 represents lower alkyl or ##STR34## wherein R.sup.5 and R.sup.6 each represent lower alkyl, allyl or phenyl or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent morpholino and either R.sup.21 is hydrogen and R.sup.31 is lower alkyl or R.sup.21 and R.sup.31 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration.|
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