Abstract: The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R.sub.2 and R.sub.3, each independently, represent hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or the two groups R.sub.2 and R.sub.3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C.sub.1 -C.sub.4 alkyl, preferably a methyl group;R.sub.

Abstract: Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. represent one of the following groups ##STR2## R.sup.1 is a partially unsaturated lower hydrocarbon group which is optionally substituted with hydroxy, oxo, aryl or the group --OR, --SR or --OCOR or a lower alkyl group which is substituted with aryl or the group --OR', --SR' or --OCOR'. R and R' each represents aryl or a saturated or partially unsaturated C.sub.1-18 -hydrocarbon group which is optionally substituted with aryl or lower alkoxy, R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together represent dimethylene or trimethylene and R.sup.4 and R.sup.5 each is hydrogen, halogen, trifluoromethyl, cyano, nitro or lower alkyl, the group --OR' being different from lower alkoxy and the compounds of formula I having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the R.sub.1 s are the same and are alkyl of 1 to 3 carbon atoms or together are alkylene of 2 to 5 carbon atoms, X, Y and W are individually --O-- or --S--, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, --OH, alkyl and alkoxy of 1 to 3 carbon atoms and --CF.sub.3 with the proviso that when R.sub.1 and R.sub.2 are alkyl, X and Y are the same and their non-toxic, pharmaceutically acceptable acid addition salts having benzodiazepine inverse agonist properties.

Abstract: A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4 H-i midazo[1,5a][1,4]benzodiazepine is a 1,2-dihydroxy derivative of the isopropyl moiety and is itself an anxiolytic agent of greater activity than its substrate.

Abstract: Novel tricyclic fused pyrimidine derivatives represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently C.sub.1-8 alkyl or C.sub.2-8 alkenyl;R.sup.3 is hydrogen, C.sub.1-3 alkyl, C.sub.2-3 alkenyl, C.sub.1-6 alkyl-CO-, optionally substituted benzoyl, C.sub.1-4 alkyl-O-CO-, carbamoyl or formyl; andA is C.sub.2-4 alkylene or C.sub.2-4 alkenylene which may be substituted with C.sub.1-3 alkyl, halogen, nitro, amino, oxo, or phenyl optionally substituted with 1 to 2 members selected from the class consisting of amino, nitro, hydroxy, methoxy and methyl, and a salt thereofare useful for antiinflammatory, analgesic, antipyretic, anti-allergic anti-psoriatic and liver-protecting agent.

Abstract: A compound selected from the group consisting a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl, cycloalkyl of 4 to 6 carbon atoms and ##STR2## R.sub.4 and R.sub.5 are individually hydrogen or alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, amido and mono- and dialkylamido of 1 to 5 alkyl carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and cycloalkyl of 3 to 5 carbon atoms or taken together form alkylene of 3 to 5 carbon atoms, X and Y are individually selected form the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, --CF.sub.

Abstract: A compound for treating disorders of the central nervous system, which is of the formulawherein A taken together with the two carbon atoms denoted by .alpha. and .beta. is one of the following groups: ##STR1## R.sup.1 is one of the following groups:--CH.dbd.CH--R.sup.6 (d)and--C.tbd.C--R.sup.6, (e)R.sup.2 is hydrogen, R.sup.3 is lower alkyl, or R.sup.2 and R.sup.3 together are dimethylene or trimethylene, R.sup.4 and R.sup.5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R.sup.6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C.sub.3 -C.sub.7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R.sup.6 is different from hydrogen.

Abstract: There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) and (4) and wherein R.sup.1 signifies a 5- or 6-membered aromatic heterocyclic group or the group --C(R.sup.6).dbd.NOR.sup.7 (B), R.sup.2 signifies hydrogen and R.sup.3 signifies hydrogen or lower alkyl or R.sup.2 and R.sup.3 together signify dimethylene, trimethylene or propenylene, R.sup.4 and R.sup.5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl, R.sup.6 signifies hydrogen or lower alkyl and R.sup.7 signifies lower alkyl, the compound of formula I having the (S) or (R,S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.

Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 -cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: The application discloses novel benzodiazepine agonist compounds, namely, compounds having the formula ##STR1## wherein X is F, CF.sub.3, CH.sub.3, or CN, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for their production are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, nitro, amino, cyano, methylsulfonamido, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio or (alkanoyl of 2 to 4 carbon atoms)amino;R.sub.3 is hydrogen, fluorine, chlorine, bromine or alkyl of 1 to 3 carbon atoms;R.sub.

Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: The application discloses a novel benzodiazepine agonist compound, namely, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-6-oxo-4H-imida zo [1,5-a][1,4]benzodiazepine, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for its production are also disclosed.

Abstract: The application discloses novel benzodiazepine agonist compounds, namely, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-6-oxo-7-halo-4 H-imidazo [1,5-a][1,4]benzodiazepines, pharmaceutical compositions thereof, and a method of ameliorating central nervous system ailments therewith, especially convulsions and anxiolytic states. A novel intermediate and process for their production are also disclosed.