Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with a more desirable protecting group.

Abstract: 4-Hydroxypyrrolo[2,3-d]pyrimidines are regiospecifically halogenated at the C-5 position by silylation in the presence of an inert organic solvent and iodination, bromination or chlorination.

Abstract: This invention provides certain N-phenyl-N'-substitutedphenylsulfonylureas compounds, formulations, and a method for treating susceptible neoplasms in mammals using the sulfonylurea compounds.

Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.

Abstract: An assay method for the rapid determination of hydrolytic enzyme activity in large numbers of samples is provided which comprises bonding a resin-binding compound, such as biotin, to one side of the scissile bond of the substrate and a reporter molecule, such as a fluorescence marker, to the opposite side of the scissile bond, incubating the modified substrate and the enzyme in multiple well plates, e.g. 96-well plates, optionally in the presence if a test inhibitor or activator compound transferring the incubation solutions to a second multiple well plate having upper and lower chambers separated by a porous membrane the upper chamber of which contains resin beads capable of binding with the resin-binding compound, filtering and washing the wells of the second plate and reading the emission from the plates. The invention also provides protease substrates for HIV-1 protease, vertebrate stromelysin and derivatives thereof which are useful in the assay method.

Abstract: Newly-discovered antibiotic A10255 factors B, C, E, F, G, H, and J are produced by submerged aerobic fermentation of Streptomyces gardneri NRRL 15537 and NRRL 18260 or an A10255-producing variant or mutant thereof. The antibiotics are active against a wide variety of pathogenic bacteria, and also enhance feed-utilization efficiency in chickens, weanling pigs, cattle and sheep. The antibiotics can also be used to detect the thiostrepton-resistance gene in Streptomyces species.

Abstract: The present invention provides 4-amino-6-substituted-hexahydrobenz[cd]indoles which are useful in treating disease states which can be benefited by an alteration of 5-HT.sub.1A receptors.

Abstract: 2-Methyl-10-(4-methyl-1-piperazinyl)-4H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.

Abstract: The present invention involves certain 4-amino-6-substituted-tetrahydrobenz[cd]indoles and their use in treating disorders which can be benefited by modifying 5-HT A receptor function.

Abstract: An improved drug delivery system comprising a gun style injection device used for holding and administering a disposable pre-filled drug cartridge, a holster device used for receiving an end of the gun style injection device and thereafter severing cannula from cartridge and disposing of spent cannulas and cartridges, and an improvement to the drug cartridge is disclosed. The gun style injection device comprises a barrel, a handle, a hinged and spring loaded squeeze lever, and a safety trigger. The holster device comprises a leg protection panel to which a housing is coupled for disposing of spent cartridges. The holster housing is adapted for receiving the barrel of the gun style injection device. The holster housing provides a means for severing the cannula from a used cartridge and disposing of both the cannula and cartridge in separate containers. The cartridge design itself is improved in order to increase the performance of the gun style injection device and the holster cannula severing mechanism.

Abstract: The present invention relates to a hypodermic syringe having the same general appearance as a pen which is specifically adapted to provide for multiple measured injections of materials such as insulin or human growth hormone.

Abstract: Two embodiments of a multi-dose syringe both include structure for indicating the selected amount of liquid to be injected. A first element and a second element coupled respectively to the syringe housing and the plunger rod are adapted for calibrated movement with respect to each other, one of the first and second elements includes an outer portion having dose-indicating scale thereon, and another of the first and second elements surrounding said outer portion includes a window through which only a segment of the dose-indicating scale on said portion is visible, the visible portion indicating the amount of liquid selected for injection.

Abstract: A method of preparing an optical fiber for user in an interferometric system includes introducing a portion of a single-mode, polarization preserving fiber having an asymmetric cladding into a medium capable of etching away the cladding and withdrawing the portion from the medium after sensing an optical intraction between light introduced into the optical fiber and the medium.

Abstract: Disclosed is a process using hydrolysis and hydrogenation for converting enamino .beta.-lactams to their saturated alkyl ester acid salts, key intermediates to 1-carbacephalosporins. Also disclosed are intermediates resulting from the process.

Abstract: 2-amino-4-hydroxypyrido[2,3-d]pyrimidines, having a 6-substituted ethyl or ethenyl group, are useful antineoplastic agents.

Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.

Abstract: Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.

Abstract: An optical fiber interferometric system includes a pair of single-mode, polarization-preserving fibers having distal and proximal ends. The cladding of a selected portion of one of the fibers having been removed to allow an evanescent portion of a light wave traveling within the fiber to interact with any medium surrounding the selected portion of the fiber. A light source for producing a light of known character is coupled to the proximal ends of the pair of optical fibers for introducing a source signal to the pair of fibers. A reflector at the distal ends of the optical fibers reflects the light from the distal ends back toward the light source. The return signals are used to construct an interferogram which is observed to detect any modulation in the phase of the light signals. The modulation is examined ratiometrically to derive a change in the index of refraction of the medium surrounding the selected portion substantially free of any environmentally induced phase noise.

Abstract: Administration of a folate binding protein binding agent in conjunction with use of an antitumor agent which is an inhibitor of glycinamide ribonucleotide transformylase or other antifolate reduces the toxic effects of such agent and provides an enhanced therapeutic index.

Abstract: The present invention is directed to a class of novel C-25-monohydrazine derivatives, and C-25, C-26-bishydrazine derivatives, of the polyether monensin. The derivatives are useful in animal husbandry.