Abstract: The sensitizing amines of the present invention, illustrated by the steroidal amines (I) ##STR1## the alkyl amines (II), bicyclic amines (III), bicyclic ethers (IV), tricyclic compounds (V), indoles (VI) and various species are useful in treating individuals who have cancer has become resistant to cancer chemotherapeutic agents and in preventing the resistance from developing or slowing the rate of resistance to the chemotherapeutic agents.

Abstract: Methanesulfonamides are structurally depicted by Formula I' ##STR1## or its pharmacologically acceptable salts where R.sub.3 is a C.sub.1-7 alkyl substituted with C.sub.3-7 cycloalkyl, or a C.sub.1-10 alkyl substituted with one to eight fluorine atoms, one to three hydroxy, one to three C.sub.1-5 acyloxy or one to three C.sub.1-4 alkoxy substituents. These compounds are useful as Class III antiarrhythmic agents and are stable against rapid metabolism. Methods for treating cardiac arrhythmias with the compounds of Formula I' as well as compositions thereof are also described.

Abstract: The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.

Abstract: 1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (III): ##STR1## wherein R is selected from the group consisting of hydroxy, esters thereof, and alkoxy, in which the alkyl group is of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino, and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.

Abstract: The present invention provides novel renin-inhibiting peptides and novel processes and intermediates for the preparation of both novel and known renin-inhibiting peptide analogs. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.

Abstract: Triazolo-benzodiazepine-1-ethanamines of the formulas ##STR1## where R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Ring A are as defined in the specification, e.g., 8-chloro-N,N-dimethyl-.beta.,6-diphenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benz odiazepine-1-ethanamine, and pharmacologically acceptable salts thereof, have been found to have substantial diuretic, natriuretic, but little, if any, kaliuretic activity, which can be used alone, or concomittently with other diuretic drugs such as furosemide or hydrochlorothiazide and/or with antihypertensive agents such as propranolol, captopril, minoxidil, prazosin, guanadrel sulfate, whose actions are supplemented by the action of a diuretic drug.

Abstract: 2,4-Dihydro-2-(omega-aminoalkyl)-1H-[1,2,4]triazolo[3,4-c][1,4]benzoxazin-1 -ones of the formula ##STR1## where n and -NRR are as defined in the specification, e.g., 2-[4-[4-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)piperadinyl]butyl]-2,4-dih ydro-1H-[1,2,4]triazolo[3,4-c][1,4]benzoxazin-1-one, are disclosed. They are useful for treating hypertension or allergy conditions in humans and valuable animals.

Abstract: Triazolo-benzodiazepine-1-ethanamines of the formulas ##STR1## where R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Ring A are as defined in the specification, e.g., 8-chloro-N,N-dimethyl-.beta.,6-diphenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benz odiazepine-1-ethanamine, and pharmacologically acceptable salts thereof, have been found to have substantial diuretic, natriuretic, but little, if any, kaliuretic activity, which can be used alone, or concomittently with other diuretic drugs such as furosemide or hydrochlorothiazide and/or with antihypertensive agents such as propranolo, captopril, minoxidil, prazosin, guanadrel sulfate, whose actions are supplemented by the action of a diuretic drug.

Abstract: Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-Chloro-1-hydroxymethyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula ##STR1## including the N-oxides, esters, and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.

Abstract: This specification concerns the use to treat hypertension in mammals of novel and known 4H-s-triazolo[4,3-a][1,4]benzodiazepines, known 4H-s-triazolo[4,3-a][1,3,4]benzotriazepines and 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-ones, and novel 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-thiones.

Abstract: Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-chloro-1-methanol-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]-benzodiaz epine compound of the formula: ##STR1## Including the N-oxides and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.

Abstract: Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 1-hydroxymethyl-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula: ##STR1## including the N-oxides esters and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.

Abstract: 6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety selected from the group consisting of pyrrolidino, piperidino, morpholino and 3,6-dihydro-1(2H)-pyridyl, and the pharmacologically acceptable salts thereof, are central nervous system depressant drugs which are useful in effective dosages in domestic and zoo animals for their calming and tranquilizing uses during shipment and to reduce aggressive behavior. In man these compounds are potentially useful for controlling anxiety and schizophrenia and for their sedative, muscle relaxant and anti-convulsant activity.

Abstract: Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, methyl or ethyl, and R.sub.3 is hydrogen, fluorine, chlorine, bromine, --CN, --NO.sub.2, --CF.sub.3, or alkylthio in which the alkyl is from one to three carbon atoms, inclusive; including the pharmacologically acceptable acid addition salts or H-oxides thereof, in association with a pharmaceutical carrier. The process is the administration of the above compositions to humans at a dose of from about 0.1 mg./kg./day to about 1 mg./kg./day for anti-depressant and anti-anxiety effects.

Abstract: 1-(Aminoalkyl) substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, methyl, or ethyl; wherein R' and R" are selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl as defined above; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl as defined above, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, and alkylsulfonyl, in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are prepared by reacting a compound of the formula: ##STR2## wherein X is chlorine or bromine and wherein R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are defined as above with an amine of the formula: ##STR3## wherein R' and R" are defined as above.

Abstract: The compound of the formula ##STR1## wherein R' and R" are alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2 is phenyl, o-chlorophenyl, o-fluorophenyl, or 2,6-difluorophenyl, is prepared by reacting a 1-halomethyl-6-phenyl-4H-s-triazo[4,3-a][1,4]-benzodiazepine with N,N-dimethylhydroxylamine and a strong base. The compound II and its pharmacologically acceptable acid addition salts have sedative and tranquilizing activity.

Abstract: 6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety selected from the group consisting of pyrrolidino, piperidino, morpholino and 3,6-dihydro-1(2H)-pyridyl, and the pharmacologically acceptable salts thereof, are central nervous system depressant drugs which are useful in effective dosages in domestic and zoo animals for their calming and tranquilizing uses during shipment and to reduce aggressive behavior. In man these compounds are potentially useful for controlling anxiety and schizophrenia and for their sedative, muscle relaxant and anti-convulsant activity.

Abstract: 1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, methyl, ethyl, fluorine, chlorine, and bromine, and X is selected from fluorine, chlorine, and bromine; wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms inclusive; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl, as defined above, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, and alkylsulfonyl, in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are prepared by reacting a compound of the formula: ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 R.sub.4, and R.sub.5 are defined as above, with an haloacyl chloride or haloacyl bromide of the formula ##STR3## wherein R.sub.o and X are defined as above and X' is chlorine or bromine.

Abstract: This invention relates to novel benzodiazepinium compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, hydroxy, mercapto, amino, monoalkylamino of 1 through 3 carbon atoms, arylamino wherein the aryl moiety is selected from the group consisting of unsubstituted and monosubstituted phenyl and naphthyl, alkanoylamino of 1 through 4 carbon atoms, aroylamino wherein the aroyl moiety is selected from the group consisting of unsubstituted and monosubstituted benzoyl and naphthoyl, alkanesulfonamido of 1 through 3 carbon atoms, and arylsulfonamido wherein the aryl moiety is selected from the group consisting of unsubstituted and monosubstituted phenyl and naphthyl; R.sub.1 is lower alkyl of 1 through 3 carbon atoms; R.sub.2 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sub.3, R.sub.4, R.sub.5 and R.sub.

Abstract: Compounds of the formula: ##STR1## wherein R'.sub.o and R".sub.o are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; R.sub.2 is phenyl, o-chlorophenyl, o-fluorophenyl, 2,6-difluorophenyl and 2-pyridyl are prepared by multistep reactions from compounds of formula I: ##STR2## wherein R.sub.1 and R.sub.2 are defined as above and X is chlorine or bromine.Compounds of formula III, intermediates in the preparation thereof, Schiff's bases of compounds IIIA (III in which R'.sub.o and R".sub.o are hydrogen), and the pharmacologically acceptable acid addition salts are useful in birds and mammals, including man, as sedatives, antianxiety, antidepressant, anticonvulsive, and muscular relaxing agents.