Abstract: Compounds having the structure ##STR1## where (Z--COO is the residue of an iodinated aromatic acid;R.sup.1 and R.sup.2 are independently alkyl, fluoroalkyl, cycloalkyl, aryl or aralkyl; andR.sup.3 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, cyano, sulfonate, carboxamido, sulfonamido, CO.sub.2 -alkyl, CO.sub.2 -aryl or CO.sub.2 -aralkyl;are useful as contrast agents in x-ray imaging compositions and methods.

Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 0 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently a substituent as defined for R.sup.1 and R.sup.2 above, halogen, hydroxy or acylamino;and R.sup.5 and R.sup.6 are independently H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, alkoxyalkyl, or acetamidoalkyl;or R.sup.5 and R.sup.6, taken together with the nitrogen atom to which they are attached, represent a 4 to 7-membered nitrogen containing ring, are useful as contrast agents in x-ray imaging compositions and methods.

Abstract: Disclosed are aqueous compositions containing a contrast agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract, wherein R is a substituted or unsubstituted alkyl group containing from 2 to 8 carbon atoms, wherein said substituents are selected from the group consisting of C.sub.1 -C.sub.6 alkyl, hydroxy and alkoxy; and n is 1 to 5.

Abstract: Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.

Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.

Abstract: Disclosed is a pre-filled plastic syringe containing a liquid product for terminal sterilization comprising: a syringe barrel equipped with a one-way valve and a slidable plunger to equalize pressure differentials; a filter engaging the one way valve to prevent backward migration of viruses and bacteria; an end cap covering the open end of the barrel to maintain sterility; and an end cap restraining device to prevent plunger blow-out.

Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.

Abstract: Compounds of the formula ##STR1## wherein: Y is a bond, or C.sub.1 -C.sub.6 alkylene;R.sub.1 is hydrogen or C.sub.1 -C.sub.3 lower-alkyl;R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.3 lower-alkyl or halogen;R.sub.4 is hydrogen or C.sub.1 -C.sub.3 lower-alkyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents, particularly against picornaviruses.

Abstract: Novel substituted 2-azabicyclo[2.2.2]octane derivatives, pharmaceutical compositions containing them, methods for treating central nervous system disorders utilizing them, and processes for synthesizing them.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower-alkanoyl or hydrogen;R.sub.2 and R.sub.3 are the same or different lower-alkyl; or pharmaceutically acceptable acid-addition salts thereof are useful in the treatment of disorders of the central nervous system.

Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.

Abstract: Stable particles comprising a core consisting of a water-insoluble ester or amide of 3,5-diacetamido-2,4,6-triiodobenzoic acid encapsulated with methyl cellulose, such particles having an average particle size of less than about 10 .mu.m, dispersions containing such particles, and methods for the preparation thereof are disclosed. The particles are particularly useful as contrast agents for use in x-ray and ultrasound diagnostic imaging compositions and methods.

Abstract: An elastomeric stopper for a fluid-containing bottle to hermetically seal the content therein and to provide access thereto by the insertion of an infusion device through the stopper, the stopper comprising an annular protuberance which forms a second seal with the shaft of the infusion device to prevent leakage, blow-out and introduction of particulate matter into the bottle.

Abstract: The present invention is directed to a syringe assembly (48), particularly useful for use with conventional prefilled pharmaceutical cartridge-needle units (46), including a hollow body (4) housing the cartridge-needle unit or other syringe structure. The substantially hollow body and the syringe structure include mating slits (28, 29, 30) and a ring (26) so that the needle (60) can be exposed for I.M. injection use and then withdrawn into the body for safety. The body is configured so that when the user diametrically squeezes the body adjacent the slit(s), the ring disengages the slit(s) due to the deformation of the body which permits the needle tip (62) to be positioned inside, for safety, or outside, for use, of the body. The internal position is also useful for safely injecting a pharmaceutical into an IV port (88).

Abstract: Disclosed is a stopper for a medical vial suitable for piercings by a spike without producing unacceptable amounts of particulate matter, comprising: a stopper body of an elastomeric material; and an abrasion resistant coating covering the top, central, piercable surface of the stopper.

Abstract: A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.

Abstract: Disclosed is a method for terminal steam sterilization of a pre-filled plastic syringe or a pre-filled plastic cartridge, said method comprising the steps of: maintaining a head space in the syringe or cartridge of less than about 10%--of the fill--volume; providing at least a 10% leeway for the plunger therein to slide in response to pressure differential; and sterilizing the syringe or cartridge at an autoclave pressure that is less than the internal pressure of the syringe or cartridge.

Abstract: Particles having an average diameter of less than about 12 microns comprising fatty acid cores encapsulated with human serum albumin and methods for their preparation are disclosed. These materials are useful as contrast agents in ultrasonic imaging, having scattering intensities that are equivalent to or greater than those obtain from dispersed microbubbles but being much more stable, both in storage and when used in vivo, than are contrast agents based on dispersed microbubbles.

Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl, 4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.