Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof therefor.

Abstract: Compounds having the structural formula ##STR1## wherein L is O;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.3 is from one to three of a variety of substituents at any or all of the 5-, 6- and 7-positions;or a pharmaceutically acceptable acid addition salt thereof if the compound has a basic functional group or a pharmaceutically acceptable acid addition salt thereof if the compound has an acidic functional group,which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.

Abstract: Compounds of formula I; ##STR1## wherein R.sup.1 is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis;R.sup.2 is hydrogen, nitro, lower alkyl amino, diloweralkyl amino or methyl;R.sup.3 is hydrogen or --P(R.sup.4)OR.sup.5 ;R.sup.4 is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-;R.sup.5 is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl;n is from 0 to 2X is oxygen, sulfur, or --NR.sup.6 ;R.sup.6 is hydrogen or lower alkyl;Q is chosen from the group consisting of ##STR2## R.sup.7 is lower-alkyl or loweralkyloxy methylene; and R.sup.8 is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyland its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula I are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.

Abstract: This invention relates to a holder for use in combination with a pre-filled cartridge-needle unit, the holder comprising a hollow body sized for housing the cartridge-needle unit therein, and means for permitting the body to move axially relative to the cartridge-needle unit. In one preferred embodiment, the distal end of the body is elliptical in cross section and the proximal end of the body is circular in cross section. In another preferred embodiment, the body comprises a pair of cam slots at the distal end and a pair or retaining slots at the proximal end, the slots being sized to accept a circumferential ring on the cartridge-needle unit and positioned to hold the cartridge-needle units in use and safe positions. The holder is easier to use and manufacture and reduces the susceptibility of health care workers to accidental needle strikes.

Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: The invention pertains to heterocycle substituted phenoxyalkylheterocycles of the formula ##STR1## wherein Thi, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, or a pharmaceutically acceptable salt thereof which are effective antipicornaviral agents.

Abstract: A compound of the formula ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.

Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: Compounds of the formula ##STR1## wherein Azo is alkyltetrazolyl, oxadiazolyl, imidazolyl, pyrazolyl, triazolyl, oxazolyl, triazinyl, thiazolyl, isothiazolyl;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or substituted phenyl or substituted heterocyclyl is an effective antipicornaviral agents.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a barium salt in a pharmaceutically acceptable carrier comprising a cellulose derivative; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Abstract: A solid effervescent antacid formulation comprising as primary ingredients from about 35 to about 53 percent by weight of calcium carbonate, from about 0 to about 14 percent by weight of magnesium carbonate, from about 3.5 to about 7 percent by weight of a bicarbonate salt, from about 3.5 to about 7 percent by weight of malic acid and from about 21 to about 35 percent by weight of a bulking agent.

Abstract: Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclyl-carboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.

Abstract: Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.

Abstract: A plastic syringe adapted for use with power injector systems comprises a cylindrical barrel for receiving a liquid, a plunger axially reciprocable within the barrel for discharging the liquid therefrom, a discharge extension at the distal end of the barrel terminating in a discharge outlet, at least one radially outwardly extending mounting lug located at or near the outer proximal end of the barrel, the lug having a distal surface having first and second ends defining a constrained portion of the barrel, and the lug being crown shaped such that the center of the distal surface of the lug is distally offset from the ends of the lug. In another embodiment, the syringe comprises a cylindrical collar adapted to fit over and attach to the proximal end of the cylindrical barrel, and the crowned lug is located at or near the outer proximal end of the collar.

Abstract: Novel 2H-[1]benzothiopyrano[4,3,2-cd]indazoles are disclosed as antitumor agents. Compositions containing the benzothiopyranoindazoles and methods of treating tumors and cancer in mammals with benzothiopyranoindazoles are also disclosed.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkanes and iodophenyl ethers as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.