Abstract: Benzodiazocines corresponding to the formula ##STR1## are converted to benzodiazepines corresponding to the formula ##STR2## of claim 1 by subjecting the benzodiazocine (a) if it is halogen-substituted in the 3-position to a thermal treatment which may also take place in the presence of a nucleophilic agent for the reaction or (b) if the 3-position is hydroxy substituted to treatment with a Lewis acid which is a chlorinating or brominating agent. Whenever the diazepine obtained as the final product has a 2-halogenomethyl group it may then be converted to benzodiazepine which is otherwise substituted in the 2-position.

Abstract: New quaternary derivatives of 10-bromoajmaline and 10-bromoisoajmaline are disclosed which exhibit antiarrhythmic and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup.- represents an acid anion as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.

Abstract: New N.sub.b -quaternary 10-bromosandwicine and 10-bromoisosandwicine derivatives are disclosed which exhibit antiarrhythmic properties and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup..crclbar. represents an acid anion, as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.

Abstract: Acidiferous salts of 17-.beta.-n-pentyl sparteine are crystallized out of a solution of 17-.beta.-n-pentyl sparteine and a dicarboxylic acid selected from the group consisting of tartaric acid, fumaric acid or mixtures thereof. The novel acidiferous pentyl sparteine salts are employed in pharmaceutical compositions for the treatment of cardiac disorders and in venous therapeutical applications, and process improved stability and pharmacological properties.

Abstract: 1,4-Benzodiazepin of the formula ##STR1## wherein R is a low molecular straight or branched alkyl and X is halogen or trifluoromethyl, and pharmaceutically acceptable acid addition salts of these benzodiazepins. The benzodiazepins are made by heating an acyldiamine in the presence of phosphorus oxychloride at the latter's boiling point followed by reacting the resulting mixture of 7-member and 8-member compounds with an alkali metal alkoxide.

Abstract: 1,2,3,4-Tetrahydro-1,5-benzodiazocines having the following formula ##STR1## in which R.sup.1 is a hydrogen, alkyl radical having at most 6 carbon atoms, methoxyethyl, or benzyl radical,R.sup.2 is a halo, hydroxyl, acetoxy or benzoxy radical,R.sup.3 is a phenyl, 2-methylphenyl, 2-chlorophenyl, 2-bromophenyl, 2-fluorophenyl, 2-nitrophenyl, 2-(trifluoromethyl)phenyl, 3-(trifluoromethyl)phenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,4-dimethoxyphenyl, or 3,4,5-trimethoxyphenyl radical,R.sup.4 is a hydrogen, chloro, fluoro, bromo, trifluoromethyl, methyl, methoxy, or methylthio radical, andR.sup.5 is a hydrogen or methoxy radical, or R.sup.4 and R.sup.5 together are an ethylendioxy radical, or an acid addition salt of the said benzodiazocine, and processes of making the same are described.

Abstract: A 1,3 diaminopropane derivative having the formula I ##STR1## in which R.sub.1 is hydrogen, methoxyethyl, benzyl or alkyl of at most 6 carbon atoms or is cycloalkyl of 3 to 6 carbon atoms,R is hydroxy, acetoxy or benzoxy, andA and B are phenyl or phenyl substituted with one to three identical or different members selected from the group consisting of halogen, alkyl, alkoxy, the alkyl or alkoxy moieties of the latter two groups having at most 4 carbon atoms, or phenyl substituted by nitro, trifluoromethyl, methylthio, or ethylenedioxy,or an acid addition salt of said diaminopropane derivative.

Abstract: New 1,4-benzodiazepine derivatives are disclosed which are substituted in 2-position by cyanomethylene or carbamoylmethylene and have the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, or nitro, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents phenyl which may be substituted by halogen or CF.sub.3, and R.sub.4 represents cyano or carbamoyl. The compounds exhibit tranquilizing activities. The cyanomethylene-compounds are prepared by oxidizing corresponding cyanomethyl compounds with Cr-VI-oxide in an acidic reaction medium. The cyanomethylene-group can subsequently be hydrolyzed into the carbamoylmethylene group.

Abstract: 1,4-benzodiazepin of the formula ##STR1## wherein R is a low molecular straight or branched alkyl and X is halogen or trifluoromethyl, and pharmaceutically acceptable acid addition salts of these benzodiazepins. The benzodiazepins are made by heating an acyldiamine in the presence of phosphorus oxychloride at the latter's boiling point followed by reacting the resulting mixture of 7-member and 8-member compounds with an alkali metal alkoxide.

Abstract: A benzodiazepine derivative of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl which may be a straight chain, branched chain or cyclic group and may also be substituted,R.sub.2 is halogen, free hydroxyl, esterified hydroxyl, etherified hydroxyl, nitrile, carboxyl or a derivative thereof or is thioalkyl, thioaryl or the group ##STR2## R.sub.3 and R.sub.4 in this group being the same or different and being hydrogen, acyl, aryl, alkyl, aralkyl, aryloxyalkyl which latter five groups may also be substituted, or wherein R.sub.3 and R.sub.4 are saturated or unsaturated, straight chain or branched alkyl and in which groups the several alkyl may be interconnected directly or through a hetero atom, which if the hetero atom is nitrogen may also be substituted, and in which formula I, A and B are phenyl or phenyl, substituted by nitro, trifluoromethyl, halogen, methylthio, alkyl or alkoxy; or a pharmaceutically acceptable acid addition salt of said benzodiazepine derivatives of formula I.

Abstract: A benzodiazepine derivative of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl which may be a straight chain, branched chain or cyclic group and may also be substituted,R.sub.2 is halogen, free hydroxyl, esterified hydroxyl, etherified hydroxyl, nitrile, carboxyl or a derivative thereof or is thioalkyl, thioaryl or the group ##STR2## R.sub.3 and R.sub.4 in this group being the same or different and being hydrogen, acyl, aryl, alkyl, aralkyl, aryloxyalkyl which latter five groups may also be substituted, or wherein R.sub.3 and R.sub.4 are saturated or unsaturated, straight chain or branched alkyl and in which groups the several alkyl may be interconnected directly or through a hetero atom, which if the hetero atom is nitrogen may also be substituted,And in which formula I, A and B are phenyl or phenyl substituted by nitro, trifluoromethyl, halogen, methylthio alkyl or alkoxy;Or a pharmaceutically acceptable acid addition salt of said benzodiazepine derivatives of formula I.