Abstract: Methods and compositions are provided for assays involving members of a specific binding pair ("sbp members") and members of a signal producing system ("sps members"). The signal producing system is capable of producing a detectible signal in relation to the presence or amount of an analyte in a sample suspected of containing the analyte. Exemplary of sps members are enzymes and enzyme substrates, which react with each other to produce a signal. The improvement of the present invention comprises temporarily delaying the production of the signal without subsequent reagent addition. The delay can be achieved by employing an inhibitor which can be an alternate substrate for the enzyme or a compound which reacts with the product of the enzyme and its substrate in an effective amount.

Abstract: 2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1,7-dicarboxylates of the formula, ##STR1## in which each R is independently H or lower alkyl, are prepared from di(lower alkyl) 1,3-acetone-dicarboxylates.

Abstract: An assembly is described for accurately and precisely controlling the position of a plunger in a syringe to deliver precise fluid volumes. The assembly includes a motor coupled to a lead screw that drives a bearing block along a linear guide rod to move the plunger of the syringe in a linear fashion. The position of the plunger is accurately controlled by attaching a digital encoder to the rotating motor shaft. The encoder and associated electronics output to a controlling processor that generates a series of regular pulses, typically 300 to 500 responsive to each motor revolution. Utilizing appropriate gear ratios of the motor and the lead screw, the number of pulses per full syringe stroke in typical applications can be on the order of one hundred thousand. The final position and the motion of the plunger (velocity and acceleration) can be controlled to within a few encoder pulses, thus precisely controlling the rate of delivery of the fluid and the volume of the fluid actually delivered by the syringe.

Abstract: 3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkanoyl]-pyrroles and their de-oxy analogs, for example, 3-(3,5-di-t-butyl-4-hydroxybenzyl)pyrrole, 2-chloro-4-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole, 3-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole and 3-[2-(3,5-di-t-butyl-4-hydroxyphenyl)-1-oxoethyl]pyrrole, have high pharmacological potency as anti-inflammatory, analgesic and antipyretic agents.

Abstract: Squaraine dyes and compositions of matter containing such dyes are disclosed. The squaraine dyes have an absorption maximum greater than 600 nanometers and are particulary useful in conjunction with a helium/neon (He/Ne) laser. Some of the squaraine dyes are hydrophilic and are therefore water soluble or water compatible and others of the squaraine dyes are lipophilic.

Abstract: Novel .delta.-caprolactam derivatives of formula I have anti-tumor, antibiotic and anthelmintic activity: ##STR1## wherein: R is H, lower alkyl, or lower acyl;R.sub.1, R.sub.2, and R.sub.3 are each independently H or lower acyl;R.sub.4 is H or acyl of 1 to 22 carbon atoms;R.sub.5 is H or lower acyl;R.sub.6 and R.sub.7 are each H or OH, or R.sub.6 and R.sub.7 together form an epoxide or a double bond;and the pharmaceutically acceptable salts thereof.

Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two,provided that when R.sup.3 is hydroxy, n is one or two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.

Abstract: Novel formulations are provided containing conjugated or unconjugated aminoglycosides, particularly labeled glycosides, a small amount of a polyamine, and additional additives, such as buffer, salt, and inert protein. The level of immunologic activity of the aminoglycoside is retained for long periods of time when stored in glass containers.

Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and propionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.

Abstract: Compounds and methods are disclosed for reversibly aggregating particles suspended in a liquid medium. The method comprises combining the liquid medium containing the particles with a polyionic polymer capable of aggregating the particles under conditions suitable for such aggregation. Thereafter, the particles are contacted with a chemical reagent capable of cleaving the polyionic polymer under conditions sufficient to reverse the aggregation. Optionally, magnetic particles are added to the liquid medium in the present method under conditions for non-specific binding and the medium including the aggregates is subjected to a magnetic field gradient to separate the aggregates from the medium. The compounds of the present invention are polyions. The aggregation of the particles is reversible upon contact with chemical agents which cleave at least some of the bonds within the polyionic polymer.

Abstract: New compounds of formulas I and II ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamino, n-lower alkylamino and ##STR2## wherein Ar is optionally substituted phenyl; Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or nothing;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB;R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy;R.sub.4 is lower alkyl; andR.sub.5 is hydrogen or lower alkyl,are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold. They are also vasodilators.

Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.

Abstract: Novel assays for ligands and receptors employing novel compounds that are conjugates of squarates dyes and members of a specific binding pair (sbp) are disclosed. The sbp members are selected from the group consisting of ligand and its complementary receptor. The sbp member is covalently or non-covalently bound to the squarate dye, which usually has an absorption maximum greater than 600 nanometers. The novel conjugates are employed in assays for determining the presence or amount of an sbp member analyte in a sample suspected of containing such analyte. Kits comprising such novel conjugates are also disclosed.

Abstract: This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.

Abstract: 4-Monosubstituted and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.

Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof whereinR.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 and R.sup.9 and R.sup.

Abstract: A controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet comprising a homogeneous matrix comprising about 4-9 weight percent of hydroxypropyl methylcellulose having a number average molecular weight in the range of from about 80,000 to about 130,000, about 81-96 weight percent naproxen or naproxen sodium, and 0.1 to about 2 weight percent of a pharmaceutically acceptable lubricating agent, and optionally including a pharmaceutically acceptable coating.

Abstract: Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.

Abstract: A method is disclosed for preparing a sample suspected of containing digoxin for determination of digoxin in the sample during an assay. The method comprises contacting the sample with .beta.-cyclodextrin in an amount and under conditions sufficient to allow a substantial portion of digoxin in the sample to bind to the .beta.-cyclodextrin. The .beta.-cyclodextrin with bound digoxin is separated from at least one other component of the medium. Next, the digoxin is released from the .beta.-cyclodextrin to provide a sample containing digoxin which may be analyzed by any of a number of assay techniques.