Abstract: This invention provides a method for treating sleep apnea, hyponea and snoring in a human patient by administering to said patient a pilocarpine compound that results in an exposure of the tissues of the naso-pharyngeal and oro-pharyngeal region to pilocarpine levels in an amount effective to reduce or eliminate such sleep apnea, hyponea and snoring condition in such patient during the treatment interval.Pilocarpine hydrochloride or nitrate solutions may be applied nasally in drop form for convenience.

Abstract: This invention provides a method for treating sleep apnea, hypopnea and/or snoring in a human patient by administering to said patient a compound that results in the release of pilocarpine to the nasopharnyx and hypopharnyx tissues an amount effective to reduce or eliminate such sleep apnea, hypopnea and snoring condition in such patient.Pilocarpine hydrochloride and pilocarpine nitrate in sustained release ocular compositions are preferred for convenience but other forms such as eye-drop solutions or aqueous gel forms may also be used. Pro-drug or targeted drug forms of pilocarpine that result in more effective tissue absorption and subsequent release of the pharmacologically active pilocarpine may also be utilized.

Abstract: This invention provides an automatically controllable water reuse system having, in combination, a) a reservoir for water to be reused, b) a switch for controlling the level of water in said reservoir, c) an electrically powered timing mechanism which controls in a timed relationship filtering and pumping apparatus which can be turned "on" by a water level switch in the reservoir. The timer, pumping, filtering, and valve control combination is timed to provide at least four modes of operation including first and second modes to clean moveable solids from first and second filters, a third mode to pump filtered water for reuse to end points of use, e.g. to a toilet water storage tank or to garden irrigation end points and a fourth mode providing either a rest period before beginning the water pumping, filtering, distribution cycle again or for manual operation of the apparatus to direct the water for reuse to a desired reuse endpoint.

Abstract: 1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a -tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl] carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.

Abstract: 1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a-tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)ami no)-1H-indol-2-yl]carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.

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: Zinc ceftiofur complexes, e.g., zinc ceftiofur hydrochloride and zinc ceftiofur sodium complexes, have been found to provide the good antibiotic activity of ceftiofur while providing low dissolution rate and long half-life properties enabling the formulation of improved long term therapy forms of ceftiofur, useful in antibiotic therapy of valuable warm-blooded animals. Pharmaceutical compositions of such zinc ceftiofur complexes and a method of using such zinc ceftiofur complexes in veterinary antibiotic applications are also provided.

Abstract: The combination of clindamycin and primaquine or pharmaceutical salts thereof is effective in treating patients with Pneumocystis carinii pneumonia.

Abstract: Certain cis-N-(2-amino-cycloalophatic)benzamides of the formula ##STR1## where m is 0, n is 2, r is alkyl, R.sub.1 and R.sub.2 are taken together with the nitrogen denote a pyrrolidine ring, X and Y are hydrogen or a halogen having an atomic number of from 9 to 35, e.g., cis-3,4-dichloro-N-methyl-n[2-(1-pyrrolidinyl)cyclohexyl]benzamide, and salts thereof, have been found to have CNS seizure blocking or preventing drug action, e.g., anti-convulsant drug properties with little or no analgesic properties.

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: The trans(+)-2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]a cetamide enantiomer, and salts thereof, have been found to be useful as Central Nervous System anti-seizure drugs, at reasonable dosages in warm-blooded animal patients, including humans, as determined in a standard anti-convulsant laboratory animal tests.

Abstract: 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.

Abstract: OMEGA-(Hydroxy, ether and ester) alkyl-2-Amino-Cycloalkenyl and -cycloalkyl amide compounds of the formula: ##STR1## where the wavy line bonds, m, n, p, A, R, R.sub.1, R.sub.2, X, Y and Z are as defined in the specification, e.g., 3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-3-(3-acetyloxypropyl)cyclohexe nyl]benzamide, and pharmacologically acceptable salts thereof, are useful as analgesic drug compounds having low physical dependence liability, compared to morphine and methadone. Pharmaceutical compositions and methods for using these compounds and compositions as analgesics are disclosed. Processes for preparing this class of compounds are also disclosed.

Abstract: In preparing arylalkanoic acids, e.g. ibuprofen or naproxen, via the conversion of the selected .alpha.-haloketal derivative of a 1-haloethyl aryl ketone to the haloalkyl ester of the arylalkanoic acid using a zinc salt catalyst the improvement comprising reacting a ring-substituted 6-membered ring ketal of the selected 1-haloethyl C.sub.6 -C.sub.12 -aryl ketone with a soluble zinc carboxylate salt to form the corresponding 3-haloalkyl arylalkanoic acid ester. The ester is converted to the alkali metal salt of the acid with base in an aqueous/water insoluble organic liquid mixture and the crude salt is converted to the corresponding acid in an aqueous/water insoluble solvent mixture for the acid, the organic solution of the acid is washed with a pH 7.0 to 8.

Abstract: A method for treating cerebral ischemia conditions by administering to the afflicted patient an effective amount of a compound of formula (I) ##STR1## where p, m, R, R.sub.1, R.sub.2, E, X, Y and Z are as defined in the specification, e.g., (5.alpha.,7.alpha.,8.beta.)-(-) or (.+-.)-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4.5]dec-8-yl ]benzeneacetamide, or ##STR2## where R, R.sub.1, R.sub.2, X and Y are as defined in the specification, e.g., (-) or (.+-.)-trans-2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)cyclohex yl]benzeneacetamide, or a pharmaceutically acceptable salt thereof.

Abstract: Dry granulate pharmaceutical compositions containing 85 to 99 percent by weight of ibuprofen and 1 to 15 percent, by weight of Croscarmellose sodium, types A and/or B (cross-linked sodium carboxymethylcellose) are useful for making ibuprofen compressed tablet and filled capsule formulations containing from about 100 to about 1200 mg. of ibuprofen per dosage unit. They are particularly helpful for making compressed tablets containing from 800 to 1200 mg. of ibuprofen per tablet, which have bioavailability rates similar to those of presently known lower dosage strength ibuprofen tablets.

Abstract: N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., (1.alpha.,2.beta.)-(.+-.)-3,4-dichloro-N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cy clohexyl]-N-methylbenzeneacetamide, and salts thereof, have useful analgesic activity, low abuse or physical dependence liability properties. Processes for their preparation are disclosed. Pharmaceutical compositions containing such compounds and methods for their use are also disclosed.

Abstract: An improved process for preparing sulfonylated indoline compounds of the formula ##STR1## via reduction of a nitrodiol of the formula ##STR2## where R.sub.1 and R.sub.3 are defined in the specification, to obtain the corresponding aminodiol ##STR3## and then the aminodiol (III) is sulfonylated and cyclized in situ to obtain the sulfonylated indoline compound (I). The substituted indoline compounds (I) are useful in overall processes for making 1,2,8,8a-cyclopropa[c]benzo[1,2-b:4,3-b']dipyrrol-4(5H)-ones which have useful light absorber, anti-bacterial and anti-tumor pharmaceutical use properties.

Abstract: Analgesic 2-oxa-spirocyclic compounds of the formula ##STR1## where the wavy line bonds, p, n, m, A, q, X, Y, R, R.sub.1, R.sub.2 and E are as defined in the specification, e.g., trans-4-bromo-N-methyl-N-[7-(1-pyrrolidinyl)-2-oxaspiro[4.5]dec-8-yl]benza mide, and trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-2-oxaspiro[4.5]dec-8-yl] benzeneacetamide, and acid addition salts thereof. Pharmaceutical compositions and methods of using these compounds as analgesics are disclosed. Processes for preparing the class of compounds are also disclosed.

Abstract: 3-(Activated ester)methyl-3-cephem-4-carboxylic acids are prepared by the direct reaction of a 3-hydroxymethyl-3-cephem-4-carboxylic acid with an activated-O-ester-methyl forming acylating agent in the presence of a 4-(tertiary amino)pyridine catalyst, and an acid absorbing base, in a non-polar liquid solvent at -78.degree. C. to +30.degree. C.