Abstract: The novel imidazodiazepine derivatives of the formula: ##STR1## wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophrenic symptoms, hepatic encephalopathy and senile dementia, as well as, in the partial or complete antagonization of undesired side-effects of substances acting on benzodiazepine receptors after over-dosage or after their use in intensive medicine and in anesthesia.

Abstract: Benzamides of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is hydrogen, halogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, sulfamoyl, mono(lower alkyl)sulfamoyl or di(lower alkyl)sulfamoyl or R.sup.1 and R.sup.2 on adjacent carbon atoms together are a methylenedioxy group, with the proviso that R.sup.2 is different from hydrogen when R.sup.1 are bromine in the 3-position,and their pharmaceutically acceptable acid addition salts have monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and Parkinsonism.

Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups,enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.

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: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.

Abstract: Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl monohalophenyl, monolower-alkylphenyl, monolower-alkoxypheynl, monotrifluoromethylphenyl, monocyanophenyl or monoaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl, as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.

Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.

Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.

Abstract: Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.

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: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.

Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen,as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.

Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.

Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.

Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.

Abstract: 2-(2-Oxo-1-pyrrolidinyl)acetic acids of the formula ##STR1## wherein R.sup.2 is hydrogen or lower alkyl and R.sup.11 is hydrogen, lower alkanoyl or another group readily cleavable by means of ammonia, are described. The compounds of formula III of the invention are useful to prepare the compound of formula I of the invention which are useful as medicaments, for example, in the form of pharmaceutical preparations.

Abstract: Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 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.

Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions, such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.

Abstract: There are described novel pharmaceutically active substances which have a pronounced affinity to the central benzodiazepine receptors and which have only a low toxicity.These active substances, namely imidazobenzodiazepines of the formula ##STR1## wherein A is lower alkylene, n is zero or 1, R.sup.1 is lower alkynyl, lower alkenyl, aryl, (C.sub.3-8)-cycloalkyl optionally substituted by lower alkyl or (C.sub.5-8)-cycloalkenyl optionally substituted by lower alkyl, or a 5- or 6-membered saturated or unsaturated heterocycle which contains an oxygen or sulphur atom as a ring member and which is optionally substituted by lower alkyl, R.sup.4 and R.sup.5 each are hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene, the compounds of formula I in which R.sup.2 and R.sup.