Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: The present invention relates to novel acyclic ethylenediamine derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as in the specification. It also relates to novel intermediates used in the synthesis of such derivatives.Compounds of the formula I and their pharmaceutically acceptable salts are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.

Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.

Abstract: The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of azabiaglo and related compounds.

Abstract: This invention relates to devices useful for the controlled delivery of one or more beneficial agents to an environment of use. More specifically, this invention concerns such devices which are powered by hydrogel. This invention also relates to the controlled delivery of one or more beneficial agents to an aqueous environment of use through the use of such hydrogel powered dispensing devices. Also disclosed are methods for the controlled delivery of one or more beneficial agents to an aqueous environment of use which comprises administering to or otherwise placing the devices of this invention in the environment of use.

Abstract: High strength, high porosity delivery devices have a shaped surface and disintegrate quickly in an aqueous medium. The devices can be prepared by disposing a formulation in a die to form a frozen predevice. A second die is contacted with the frozen formulation surface at a pressure and temperature for a time sufficient to locally momentarily liquify and shape the device surface. The shaping is followed by lyophilization.

Abstract: An improved device for repairing fractured bones is provided, the device comprising a specially designed connector, which is especially useful in combination with a plate having a tab cut out, a stop, a flat portion and a bore portion and with a compression screw and a lag screw.

Abstract: A process for the stereoselective preparation of intermediates in the preparation of potent, chiral thiazolidine-2,4-dione hypoglycemics.

Abstract: PDGF-B analogues are prepared in which an amino acid residue at a protease site is replaced with the corresponding amino acid residue from PDGF-A. The polypeptide is obtained at yields which are five to ten times greater than that for naturally occurring PDGF-B and retains the biological activity of the natural polypeptide.

Abstract: The present invention relates to certain antibiotic compounds, designated N787-182 compounds herein and derivatives thereof, which are antiparasitic agents, active against insect pest, acari, free-living nematodes and endo- and ectoparasites. This invention also relates to pharmaceutical and other compositions comprising such compounds, methods of using such compounds, the microorganism Streptomyces hygroscopicus ATCC 53718 and mutants or genetically transformed or recombinant form thereof, and processes for producing such compounds.

Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof; wherein X.sub.1, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock etc.

Abstract: Macrolides of the FK-506 type and methods of treatment of resistance to transplantation, fungal infections, and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides.

Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined hereinbelow that exhibit activity as immunostimulants.

Abstract: 7.beta.- 2-(aminothiazolyl and thiadiazolyl)-2-oxyiminoacetamido!cephalosporin derivatives having a 3- N-(optionally substituted) aminopyridiniumthiomethyl! substituent have antibacterial activity and are of use in antibacterial therapy. Processes for the preparation of such cephalosporins plus intermediates for use in the preparation thereof, including N-(optionally substituted)amino-thiopyridones, are also described.

Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.

Abstract: The present invention relates to novel substituted oxindoles of the formula I as defined below and related compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as inhibitors of phosphodiesterase ("PDE") type IV. The compounds of this invention are useful in the treatment of AIDS, asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, atopic, dermatitis, shock, other inflammatory diseases, and other conditions where the action of phosphodiesterase type IV is implicated.

Abstract: The present invention provides compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Compounds of the formulae ##STR1## where R is cycloalkyl or aryl; R.sub.1 is alkyl, X is O or C.dbd.O; A is O or S; and B is N or CH are useful as hypoglycemic agents.

Abstract: A compound of the formulaR.sup.1 -A.sup.2 -A.sup.1 -Asp-p-nitroanilidewherein:A.sup.1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid;A.sup.2 is a residue of a lipophilic .alpha.-amino acid;R.sup.1 is alkylcarbonyl, phenalkylcarbonyl, alkoxycarbonyl, phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbonyl or R.sup.2 -A.sup.3 whereinA.sup.3 is a residue of a lipophilic .alpha.-amino acid; andR.sup.2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, and a method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta..