Abstract: 2-Oxy-4H-3,1-benzoxazin-4-ones, useful as serine protease inhibitors, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:a is an integer of 1 to 4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of hydroxy, benzyloxy, lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms, lower alkylthio or halo-lower alkyl having one to six carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, --NR.sup.1 CO.sub.2 R.

Abstract: Novel compounds and assay methods are provided for determining the presence of lithium in serum, plasma, urine or other sample without deproteinization. The novel compounds are water soluble derivatives of TMC-crownformazans and provide signal enhancement by increased absorbance of the dye-lithium complex over the dye anion.

Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte is disclosed. The method involves contacting a test solution containing the sample and a first member of a specific binding pair with an end portion of a strip of bibulous material capable of being traversed by the test solution through capillary action. The first member of a specific binding pair is capable of binding the analyte. The strip contains a second member of a specific binding pair integral therewith for concentrating and non-diffusively binding the first sbp member at a small situs on the strip separated from the end portion of the strip. The detectible signal is produced in relation to the presence of the analyte in the test solution. The test solution passes through the situs as the test solution traverses the bibulous material.

Abstract: A method and apparatus for determining the presence of particles in a fluorescent dispersion which exceed either a predetermined fluorescence intensity or size are disclosed. The method and apparatus involve the irradiation of the dispersion with excitation light, the examination of the fluorescent light entering an optical fiber from a portion of the excited region small enough to permit only a low probability that more than one particle of interest is present in the volume during a predetermined period of time, and the measurement of the emitted fluorescence entering the fiber, substantially free of excitation light, to the extent that the fluorescence differs in intensity from that of the dispersion in the absence of the particle.

Abstract: Compounds are disclosed according to the formula ##STR1## or an optical isomer thereof. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.

Abstract: A method for assaying for a ligand analyte which is a member of a specific binding pair ("sbp member") consisting of ligand and its complementary receptor is disclosed. The ligand analyte has a binding site in common with an interfering substance present in a sample suspected of containing the analyte. The interfering substance has at least two binding sites. The method comprises combining in an assay medium without intervening separation (1) the sample, (2) a blocking receptor which does not bind to the ligand and does bind to the interfering substance, thereby blocking the binding of a common receptor to the interfering substance, and (3) a common receptor which binds to the common binding site. Any additional members of a signal producing system capable of producing a detectable signal in relation to the amount of analyte in the sample are added to the assay medium. Next, the assay medium is examined for the presence of a detectable signal.

Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CHCH.sub.2 --;X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);is an integer of 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.

Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.

Abstract: Methods are provided for modulating Ligand-Receptor interactions by binding of molecules at two epitopes of a receptor, where the epitopes are in relatively close special relationship. By providing for inhibition of changes in conformation of the receptor, where the inhibition is due to steric interactions or molecular bridging between the two epitopic sites, Ligand-Receptor interactions may be modulated. The modulation of Ligand-Receptor interactions has application to diagnostic assays, modulation of cellular activity, and modulation of the physiological activity of macromolecular compounds.

Abstract: A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, sulfonylamino, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.

Abstract: Methods are provided for rapidly determining a number of parameters in a few determinations. Particularly, the method is applicable to blood typing, determining the blood type as to the ABO and Rh type, as well as the determination of isoantibodies to the antigens. The method employs fluorescent particles having a plurality of fluorescers, where the presence or absence of light emission of a particular wavelength can be determined.

Abstract: Compounds having the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the definitions given herein, are useful as antiarrhythmic agents.

Abstract: 4-Monosubstitued 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 depicted in the formula: ##STR1## wherein: X is oxygen or NH, Y is hydrogen, iodo, fluoro, methyl or trifluoromethyl, Z is hydrogen or fluoro and Z' is fluoro; and the wavy line indicates that the group may be above or below the plane of the ring; and the pharmaceutically acceptable acid addition salts thereof.

Abstract: .alpha.-amino acids having a substituted .omega.-guanidino group are disclosed herein.

Abstract: Compounds according to the formula ##STR1## , its optical isomers, or a pharmaceutically acceptable salt thereof wherein:m and n are integers of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or .alpha.-amino acid side chains;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.6, halo, --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COO(R.sub.6) group wherein R.sub.

Abstract: Synthetic nonapeptide and decapeptide LHRH antagonist analogues having a halo lower alkyl guanadino-substituted amino acyl residue at position six are disclosed herein.

Abstract: Improved sensitive immunoassays are provided involving channeling involving one, usually two enzymes, where the enzymes are related by the product of one enzyme being the substrate of the other enzyme. A dispersed aggregation is formed in the assay medium of (1) the analyte, (2) one of the enzymes bound to a second binding member ("SBM") (enzyme - SBM conjugate) which conjugate is non-covalently bound to a first binding member ("FBM"), and (3) a multiplied amount of the other enzyme bound in the complex. The large amount of enzyme or reactant in the complex is achieved by having a multiplicity of linkages binding the enzyme or reactant directly or indirectly to FBMs. The enzyme channeling provides for a detectable signal which can be related to the amount of analyte in the medium.

Abstract: Compounds useful for treating inflammatory diseases, in particular rheumatoid arthritis, represented by the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:R.sub.1 is H or lower alkyl having 1 to 6 carbon atoms;R.sub.2 is H, lower alkyl having 1 to 6 carbon atoms or ##STR2## in which R.sub.3 is H, lower alkyl having 1 to 6 carbon atoms or a pharmaceutically acceptable cation;R.sub.4 and R.sub.5 are each independently H or lower alkyl having 1 to 6 carbon atoms;X and Y are each independently O or S; andn is an integer of 1-6.