Abstract: Disclosed are compounds of the class of 1-alkyl-4-phenyl and 4-(2-thienyl)-6,7-methylenedioxy-2(1H)-quinazolinones and quinazolinthiones, including the 3,4-dihydro derivatives thereof, useful as pharmaceutical agents, e.g. as anti-inflammatory agents. Such compounds, e.g. 1-isopropyl-4-phenyl-6,7-methylenedioxy-2(1H)-quinazolinones and 1-isopropyl-4-phenyl-6,7-methylenedioxy-2(1H)-quinazolinthiones, may be prepared by reacting the corresponding N-alkyl-N-(3,4-methylenedioxyphenyl)urea or thiourea with an aromatic aldehyde, e.g. benzaldehyde, in the presence of an acid at elevated temperatures to obtain the 3,4-dihydro-2(1H)-quinazolinones or 3,4-dihydro-2(1H)-quinazolinthiones which may then be oxidized to the corresponding 3,4-unsaturated compounds.
Abstract: The invention discloses optionally substituted 3-methylsulfinyl indazoles having pharmacological activity in animals and useful as sleep-inducing agents. The compounds may be prepared by diazotization of an optionally substituted .alpha.-methylsulfinyl-o-toluidine.
Abstract: Acyl substituted phenyl alkanoic acids, e.g. p-pivaloyl phenyl acetic acid, are prepared by hydrolyzing p-pivaloyl phenyl acetonitriles and are useful as hypolipidemic agents.
Abstract: Compounds of the formula I: ##SPC1##whereinR.degree. is lower alkyl,n is 0, 1 or 2,R is lower alkyl,R' is a radical of the formula ##SPC2##In which Y and Y' are the same or different and represent hydrogen, lower alkyl, lower alkoxy, halo of atomic weight of 19 to 36 or one of Y and Y' is trifluoromethyl while the other is hydrogen, or a radical of the formula ##SPC3##In which Y" is hydrogen, fluorine, chlorine or alkyl of 1 to 3 carbon atoms,Are prepared by cyclizing a compound of formula II ##SPC4##in which R, R', R.degree. and n are as defined above, with phosgene, or,Where R is not a tertiary alkyl group in which the tertiary carbon atom is directly attached to the ring nitrogen atom, with a C.sub.1 -C.sub.2 alkyl chlorocarbonate or 1,1'carbonyldiimidazole. The compounds of formula I possess pharmaceutical activity in animals.
Abstract: Benzocycloheptaoxazolones are prepared by a multi-step process starting with a lower alkyl ester of a 3-oxo-5-phenylvaleric acid. The compounds are useful as anti-inflammatories and as intermediates in the preparation of pharmaceutically useful compounds.
Abstract: 10-(2-substituted-aminoethyl)-10,11-dihydro-5-methylene-2 or 3 7 or 8-substituted or unsubstituted-5H-dibenzo[a,d]cycloheptenes e.g., 10-(2-dimethylaminoethyl)-10,11-dihydro-5-methylene-5H-dibenzo[a,d]cyclohe ptane, prepared by various methods including acid dehydration of the corresponding dibenzo[a,d]cycloheptene-5-ols. The compounds are useful as anti-depressants.
Abstract: The invention discloses compounds of the class of 5-substituted-5H-dibenzo[a,d]cycloheptenes which are 5-hydrazinoalkyl- or 5-aminoalkyl-5H-dibenzo[a,d]cyclohepten-5-ols, or their 10,11-dihydro derivatives. The compounds are pharmaceutically active and useful, for example, as anti-convulsants and tranquilizers. A key intermediate are compounds which are a spiro[5H-dibenzo[a,d]cyclohepten-5-oxazolin-2-one] which are subjected to alkaline hydrolysis to obtain the compounds of the invention.
Abstract: Anti-inflammatory and analgesic agents of the formula I: ##SPC1##whereinR.degree. is lower alkyl,N IS 0, 1 OR 2,R is lower alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or phenyl,R' is a radical of the formula ##SPC2##In which Y and Y' are the same or different and represent hydrogen, lower alkyl, lower alkoxy, halo of atomic weight of 19 to 36 or one of Y and Y' is trifluoromethyl while the other is hydrogen, or a radical of the formula ##SPC3##In which Y" is hydrogen, fluorine, chlorine or alkyl of 1 to 3 carbon atoms,Are prepared by cyclizing a compound of formula II: ##SPC4##in which R, R', R" and n are as defined above, with, for example, phosgene.
Abstract: Substituted isoxazolyl benzamides, e.g., o-(3-trifluoromethyl-5-isoxazolyl)-N-methylbenzamide, are prepared by cyclizing a corresponding 1-hydroxy-1-[(2-hydroxyimino)-3-trifluoropropyl]-2-alkyl phthalimidine with a strong acid and are useful as minor tranquilizers and sleep inducers.
Abstract: 2-amino-5-(substituted or unsubstituted phenylalkyl)-thiadiazoles, e.g., 2-amino-5-(4-[phenylbutyl])-thiadiazole, prepared, e.g., by ring closure, of corresponding 1-(substituted or unsubstituted phenylalkanoyl)-thiosemicarbazide in a strong acid medium. The compounds are useful as minor tranquilizers and sedative hypnotics.
Abstract: Disclosed herein is a patient ventilator apparatus having a pneumatic control system operable in three different modes wherein the apparatus assists the breathing of the patient, controls the patient's breathing in a timed manner, or operates in a combination assist/control mode according to certain predetermined conditions. Fluidic circuitry controls a valved bellows apparatus, which in turn supplies air to a patient subject to limitations of time, volume, and pressure, wherein the gas supplied to the bellows comprises an adjustable oxygen/air mixture. Fluidic timers are provided for use in the control mode of the circuitry, and identical fluidic circuitry combinations are provided for use in the assist mode to automatically trigger the ventilator apparatus into an inspiratory state according to the patient's breathing requirements and to trigger such apparatus into an exhalation state when a predetermined inspiratory pressure is attained.
Abstract: Substituted 1,2-dihydrobenz[f]isoquinolines, e.g., 4-(p-chlorophenyl)-1,2-dihydrobenz[f]isoquinoline, are prepared by cyclizing N-substituted-.alpha.-naphthylethylamines and are useful as non-estrogenic antifertility agents.
Abstract: 10-(2-substituted-aminoethyl)-10,11-dihydro-5-methyl-2 or 3, 7 or 8-substituted or unsubstituted-5H-dibenzo[a,d]cycloheptenes, e.g., 10-(2-dimethylaminoethyl)-10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepte ne, are prepared by hydrogenating a corresponding 10-(2-dimethyl-aminoethyl)-10,11-dihydro-5-methylene-2 or 3, 7 or 8-substituted or unsubstituted-5H-dibenzo[a,d]cycloheptenes and are useful as anti-depressants.
Abstract: 3-Substituted-4-aryl isoquinolines, e.g. 3-tertiary butyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline, prepared from corresponding isoquinoline intermediates, are useful as anti-diabetic agents.
Abstract: Substituted or unsubstituted isoxazolyl benzamides, e.g., o-(3-phenylisoxazol-5-yl)-N-methylbenzamide, are prepared by cyclizing a corresponding 1-hydroxy-1-[substituted or unsubstituted-.beta.-(hydroxyimino)phenethyl]-2-alkyl phthalimidine with a strong acid and are useful as minor tranquilizers, muscle relaxants, and sleep inducers.
Abstract: 2,6-halo and trifluoromethyl-substituted-benzoic acids, e.g., 2,3,4,6-tetrafluorobenzoic acid or 2-chloro-6-trifluoromethylbenzoic acid, are prepared from substituted 2,4-halo and trifluoromethyl-substituted benzene compounds and are useful as plant growth regulators.
Abstract: Substituted 7,12-methano-dibenzazocines, e.g., 7,13-dihydro-6,12-dimethyl-7,12-methano-6H-dibenz[c,f]azocine, are prepared by cyclizing 3-benzylamino-alkyl-indan-1-ols and are useful as anti-inflammatory agents.
Abstract: The compounds are alkyl-substituted-tricyclic quinazolinones of the class of imidazo[2,1-b]quinazolin-5-ones and pyrimido[2,1-b]quinazolin-6-one, e.g., 2-methyl-2,3-dihydro-10-(4'-fluorobenzyl)-imidazo[2,1-b]quinazolin-5(10H)- one, useful, for example, as bronchodilator agents. Processes for preparation of said compounds include the reaction of a N-carboxy anthranilic anhydride (an isatoic anhydride) with an alkyl substituted cyclic pseudothiourea such as a 2-organomercapto-4,5-dihydroimidazole or a 2-organomercapto-3,4,5,6-tetrahydropyrimidine and the cyclization of a 2-(.omega.-hydroxy(branched)alkylamino)-4-quinazolone.