Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.

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: Maleimide derivatives, i.e., the compounds of Formula I: ##STR1## wherein: R.sup.1 is H, halo, alkyl, OH, alkoxy, haloalkyl, NO.sub.2, or NR.sup.5 R.sup.6 ;R.sup.2 is H or CN;R.sup.3 is aryl or heteroaryl, provided that R.sup.3 is heteroaryl when R.sup.2 is H and R.sup.4 is NR.sup.5 R.sup.6 ; andR.sup.4 is NR.sup.5 R.sup.6 or isothiourea,where R.sup.5 and R.sup.6 are independently H or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use as chemotherapeutic agents.

Abstract: 2-methyl-4-hexene- and 3-methyl-5-heptene-l,2-diol derivatives are disclosed together with methods for preparing such derivatives. Where the derivative is a 2-methyl-4-nexene- or 3-methyl-5-heptene-l,2-diol conjugated to a label, the conjugates are useful in immunoassays. Where the 2-methyl-4-hexene or 3-methyl-5-heptene-l,2-diol is conjugated to an immunogenic carrier, the conjugates may be employed as an immunogen for use in the preparation of antibodies. The label conjugate and the antibodies can be utilized in an immunoassay for the determination or detection of cyclosporin in a sample suspected of containing cyclosporin.

Abstract: A method is disclosed for producing multiple copies of a primary polynucleotide sequence located at the 3' terminus of a polynucleotide. The method comprises (a) forming in the presence of nucleoside triphosphates and template-dependent polynucleotide polymerase an extension of a primary polynucleotide sequence hybridized with a template sequence of a single stranded pattern polynucleotide comprising two or more template sequences each containing one or more site specific cleavage sequences, (b) cleaving into fragments said extension at cleavable polynucleotide sequences in the presence of means for specifically cleaving said cleavable polynucleotide sequences when said extension is hybridized with said site specific cleavage sequences, (c) dissociating said fragments, (d) hybridizing said fragments with single stranded pattern polynucleotide, and repeating steps (a)-(d). Steps (a)-(d) may be conducted simultaneously or wholly or partially sequentially.

Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.

Abstract: Compounds of the Formula (I), (II), or (III): ##STR1## wherein the variables are as defined in the specification and the pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, and are particularly useful as angiotensin II antagonists.

Abstract: Methods are disclosed for inactivating interfering binding proteins in a immunoassay for a member of a specific binding pair (sbp). The method comprises including in an assay medium containing a sample suspected of containing an sbp member and an interfering binding protein an effective amount of a water soluble compound having two substituted or unsubstituted phenyl groups linked to a common atom. When the sbp member or its sbp partner has two phenyl groups linked to a common atom, the compound has a number of groups other than hydrogen attached to the phenyl groups and the atom that differs by at least two from the number of such groups on the sbp member. When the sbp member or its sbp partner has two phenyl groups linked to a common atom and the binding protein is not an antibody, the compound has only one group other than hydrogen attached to a phenyl group or the common atom.

Abstract: This invention is directed to an adjuvant composition in the form of an emulsion which is comprised of an emulsion-forming amount of a non-toxic tetra-polyol or of a POP-POE block polymer and an immunopotentiating amount of a muramyldipeptide of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, where R and R.sub.1 are each independently H or acyl of 1 to 22 carbon atoms, R.sub.2 is optionally substituted alkyl or optionally substituted aryl, R.sub.3 is H, alkyl, or aryl, R.sub.4 is H or lower alkyl, X is L-alanyl, L-.alpha.-aminobutyryl, L-arginyl, L-asparginyl, L-aspartyl, L-cysteinyl, L-glutaminyl, L-glutamyl, glycyl, L-histidyl, L-hydroxyprolyl, L-isoleucyl, L-leucyl, L-lysyl, L-methionyl, L-ornithinyl, L-phenylalanyl, L-prolyl, L-seryl, L-threonyl, L-tyrosyl, L-tryptophanyl, or L-valyl, and Y is D-glutamine, D-isoglutamine or D-isoasparagine. This invention is also directed to a vaccine containing an antigen and an adjuvant composition of the invention.

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: This invention relates to compounds of the formulaor an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.

Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.

Abstract: Assay methods are provided for determining the presence of lithium in high sodium content liquids such as 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: Compounds of the formula: ##STR1## wherein: A is oxo or dioxo;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo;are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.

Abstract: Methods are disclosed for conducting assays. One such method comprises providing in combination a first bibulous member zone ("first zone") and a liquid medium containing a component. The first zone has non-diffusively bound thereto a reagent interreactive with the component. Conditions are selected wherein the liquid medium and at least a portion of the component contained therein traverse all of the first zone and migrate by capillary migration into a second bibulous member zone ("second zone"). The second zone is of a different composition than the first zone and is incapable of specifically binding the component except when an analyte is to be detected and the method further includes causing a reagent to become bound to the first bibulous member zone in relation to the amount of analyte present.

Abstract: Methods and compositions are disclosed for determining a peroxidatively active substance (PAS). The methods comprise the step of detecting a fluorescent signal produced upon cleavage of a compound of the formula F-L-Q, wherein F is a fluorester capable of producing the signal, Q is a quencher capable of quenching the signal when linked to F, and L is a bond, or a linking group having a bond, wherein the bond is capable of being cleaved by a reaction of the PAS with a substrate of the PAS and a hydrogen donor wherein the cleavage of the bond substantially reduces the quenching. The methods have application in a wide variety of systems including assays and improved assays for analytes. Also disclosed are kits for conducting the methods and improvements in accordance with the present invention.

Abstract: The instant invention is directed toward an immunoassay which can determine the presence of amphetamines in a sample suspected of containing amphetamine and/or methamphetamine by employing at least two conjugates, each comprised of a functionally similar label bound to an amphetamine analog and a methamphetamine analog respectively and an antibody to amphetamine and an antibody to methamphetamine wherein at least one of the antibodies is a monoclonal antibody.

Abstract: Novel squaraine dyes and compositions of matter containing such dyes are disclosed . The novel squaraine dyes have an absorption maximum greater than 600 nanometers and are particularly 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: This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, --SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W whereW is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl;or a pharmaceutically acceptable salt thereof.

Abstract: Novel squaraine dyes and compositions of matter containing such dyes are disclosed. The novel squaraine dyes have an absorption maximum greater than 600 nanometers and are particularly 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.