Abstract: An improved process for the reduction of 2-(2-nitrovinyl)thiophene to form 2-(2-thienyl)ethylamine employs a boron-containing reducing agent, preferably diborane. The 2-(2-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.

Abstract: Combinations of 9-[[2-hydroxy-1-(hydroxymethyl)-ethoxy]methyl]guanine and at least one other antivirally active drug such as phosphonoacetic acid and its salts, phosphonoformic acid and its salts, acycloguanosine, or a 5-(2-halogenovinyl)-2'-deoxyuridine show synergy in their activity against various herpes virus infections including HSV-1 and HSV-2.

Abstract: This invention relates to compounds of the formula ##STR1## or 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: Assay methods are provided for determining an analyte in a sample suspected of containing the analyte. The method is carried out using a composition that includes a conjugate of a first sbp member with a particle. A luminescer is reversibly associated with a nonaqueous phase of the particle. Where the first sbp member is not complementary to the analyte, a second sbp member that is capable of binding to the first sbp member is employed. Unbound conjugate is separated from conjugate that is bound to the analyte or to the second sbp member. A reagent for enhancing the detectability of the luminescer is added and the light emission of the luminescer acted on by the reagent is measured.

Abstract: Novel arylsulfonyl-dihydropyridine derivatives which are useful as calcium entry-blocker cardiovascular agents have the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, lower alkyl, or lower alkoxyalkyl;R.sup.2 is hydrogen or chloro; andR.sup.3 is hydrogen, lower alkyl, or lower alkoxyethyl.A novel process using chiral sulfoxide reagents efficiently produces single isomers of these and other sulfonyl dihydropyridines.

Abstract: Novel 13,14-dihydroprostaglandin derivatives of the formula ##STR1## wherein: m is 1 or 3;R.sub.1 is hydrogen or alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 and R.sub.4 are independently hydrogen or methyl;R.sub.5 is alkyl, CF.sub.3 (CH.sub.2).sub.n -- in which n is an integer of 3-5, cycloalkyl, or optionally substituted phenyl, benzyl or phenoxy; orR.sub.4 and R.sub.5 taken together with the carbon to which they are attached is cycloalkyl of 4-8 carbon atoms;X is cis --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 -- when m is 3, orX is --CH.sub.2 CH.dbd.C.dbd.CH-- when m is 1;and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.;or a pharmaceutically acceptable salt thereof,have been prepared. They are useful in particular for their antihypertensive and anti-ulcerogenic properties.

Abstract: Compounds of the formula (1): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2, wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen; or a pharmaceutically acceptable salt thereof, are useful as selective .alpha..sub.2 -blockers.

Abstract: A device and a method for producing the device for use in a chromatographic system wherein a component of a mixture is partitioned is comprised of a chromatographic material. In the chromatographic system the component traverses at least a portion of the chromatographic material. The device generally has at least one longitudinal edge substantially corresponding to the direction of traverse of the component. The longitudinal edge is modified to control the shape of the fron t of the traversing component by introducing along the edge either a plurality of indentations or a chemical substance.

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: 2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds of the formula, ##STR1## in which Y is OH;O.sup.- M.sup.+, wherein M is an alkali metal; orNRR', wherein R is lower alkyl and R' is lower alkyl or aryl, or NRR' is the residue of a saturated cyclic amine,are prepared from pyrrole.

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-acetonedicarboxylates.

Abstract: 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-halopyrroles. Hydrolysis and .beta.-decarboxylation of these compounds affords ketorolac and related compounds.

Abstract: A method for determining the presence of a polynucleotide analyte in a sample suspected of containing the analyte is disclosed. The method comprises combining in an assay medium the sample and first and second polynucleotide reagents complementary to the analyte. Each of the first and second reagents hybridize with a different region of the analyte. The first reagent contains means for rendering the first reagent non-covalently polymerizable. The second reagent contains means for rendering the second reagent detectable. The sample and the first and second reagents are combined in the assay medium under conditions for polymerizing the first reagent wherein the second reagent becomes bound to the polymerized first reagent only when the analyte is present in the sample. A determination is then made as to whether the second reagent has become bound to the polymerized first reagent.

Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.

Abstract: Nucleoside analogues having a ring-open structure, of general formula: ##STR1## where R and R' may be hydrogen, silyl groups, substituted alkyl groups, benzyl groups and the like, and X is an optionally substituted base such as guanine or adenine, have been shown to exhibit anti-viral and other biological acivities at non-toxic levels.

Abstract: Sixteen carbon atom carboxylic acids having 16-phenoxy or 16-phenylthio substituents, and 0, 1, or 4 triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors.

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: The present invention relates to novel synthetic antigens, conjugates and antibodies based upon specific peptide sequences and the production thereof. More particularly, the invention relates to a polypeptide which is a determinant site of a protein, the polypeptide having from 8 to 20 amino acid residues, having an amino-terminal amino acid and a carboxyl-terminal amino acid, wherein the polypeptide includes:(a) a four amino acid sequence which corresponds to the four amino acid sequence of a .beta.-turn of the protein;(b) a sequence of two to eight amino acid residues attached to the amino terminal (H.sub.2 N--) of the four amino acid sequence; and(c) a sequence of two to eight amino acid residues attached to the carboxyl terminal (--COOH) of the four amino acid sequence,wherein the amino acid residues of subparts (b) and (c) correspond to those attached to the amino terminal and the carboxyl terminal, respectively of the .beta.

Abstract: Novel fluorogenic peroxidase substrates are provided employing novel water soluble activated capped aromatic fluorescent compounds for use as peroxidase substrates. The novel compounds can be used in a wide variety of ways for determination of peroxides, peroxidase, and in assays for analytes employing peroxidase as a label on a member of a specific binding pair.

Abstract: Combinations of 9-(1,3-dihydroxy-2-propoxymethyl) guanine or a pharmaceutically acceptable salt thereof, with .beta.-interferon show a surprisingly high degree of synergism in their activity against viral infections.