Abstract: Abstract Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.

Abstract: A stent for placement within a body lumen and comprising a wall structure wherein at least a portion thereof is a hollow wall. The hollow wall has disposed therein a hydrophilic material which can be in the form of a gel, for example, which swells upon introduction of a liquid into the hollow wall to thereby achieve inflation thereof. The hollow wall is fabricated of a semi-permeable membrane whereby fluid from tissues surrounding the stent at the site of placement can pass through the membrane and swell the hydrophilic material to thereby inflate the hollow wall. A drug can be disposed with the hydrophilic material for release through the membrane at the site of stent placement. The entire wall structure of the stent can be a hollow wall, or the wall structure can incorporate both hollow and non-hollow wall portions such as hollow and solid fibers which are braided, woven or wound together.

Abstract: The following 3-carboxaldehyde quinolines and naphthyridines have antibacterial activity ##STR1## wherein A, Y, R, and R.sub.2 are as defined herein. These compounds are particularly suitable for administration by injection. A specific example of such compound is 1-cyclopropyl-6-fluoro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-y l]-4-oxo-1,4-dihydroquinoline-3-carboxaldehyde.

Abstract: Streptomyces avermitilis lacking branched-chain 2-oxo acid dehydrogenase activity and avermectin B O-methyltransferase activity, method for preparation thereof, and use thereof to produce natural and non-natural B avermectins useful as parasiticides.

Abstract: A method of using certain 3-aryl-2-hydroxypropionic acid derivatives and analogs in the treatment of hypertension.

Abstract: The present invention relates to novel 3-aminopiperidine derivatives and related 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, R.sup.6, R.sup.7, R.sup.8, Y and m are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.

Abstract: This invention relates to a novel process for preparing novel N-cyclopropyl intermediates useful for preparing certain of the 1,7-disubstituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acid derivatives of this invention which contain a cyclopropyl substituent at the 1 position as well as other 1,4-dihydroquinol-4-one-3-carboxylic acid derivatives so substituted with cyclopropyl.

Abstract: Compounds of the formula ##STR1## wherein R, Y and R.sup.1 are as defined in the specification. These compounds are muscarinic receptor antagonists which are selective for smooth muscle muscarinic sites over cardiac muscarinic sites, and are useful in the treatment of diseases associated with altered motility on tone of smooth muscle, including irritable bowel syndrome, diverticular disease, urinary incontinence, oesophageal achalasia and chronic obstructive airways disease.

Abstract: A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.

Abstract: Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.

Abstract: A form of calcium carbonate having a blocky rhombohedral crystal structure and properties including a surface area of from about 3 to about 15 m.sup.2 /g, an average discrete particle size of from about 0.2 to about 0.9 micron, wherein the discrete particles have an aspect ratio less than about 2:1, and a particle size distribution such that at least about 60 weight percent of the particles have a size within 50 percent of the equivalent discrete particle spherical diameter, suitable for use as a filler material in papermaking to improve the optical properties of the resulting paper, is disclosed. An accelerated heat-aging process, including embodiments thereof which utilize hydrothermal techniques, for rapidly producing this form of calcium carbonate, and a related form of calcium carbonate having a hexagonal prismatic crystal structure and the same properties, in large quantities to meet the demand of the papermaking industry, as well as a method for using these materials in papermaking, are also disclosed.

Abstract: This invention relates to certain polyamines and polypeptides found to be present in the venom of the Agelenopsis aperta spider. The polyamines of this invention and the salts thereof antagonize excitatory amino acid neurotransmitters, which neurotransmitters affect cells of various organisms and are useful in antagonizing said neurotransmitters, per se, in the treatment of excitatory amino acid neurotransmitter mediated diseases and conditions and in the control of invertebrate pests. The polypeptides of this invention and one of said polyamines and the salts thereof block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se, in the treatment of calcium channel mediated diseases and conditions and in the control of invertebrate pests. This invention also relates to compositions comprising said polyamines, polypeptides and salts thereof.

Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;A and B are each independently CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro;a pharmaceutically-acceptable cationic salt thereof; ora pharmaceutically-acceptable acid addition salt thereof.

Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.

Abstract: N-Alkenylbenzo[b]thieno[3,2-b]oxazin-2,4-diones, pro-drugs of cyclooxygenase and 5-lipoxygenase inhibitory N-alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives; pharmaceutical compositions comprising one or more of said pro-drugs and a pharmaceutical acceptable carrier; and the use of said pro-drugs to treat mammalian diseases arising from biological mediators formed in the mammalian body by cyclooxygenase and/or 5-lipoxygenase catalyzed reactions.

Abstract: An implant comprising a specially adapted bone screw having a threaded shank portion and a sleeve which mates with and operates in cooperation with the threaded shank portion is provided. Also provided is a driver specially adapted for inserting and removing the implant of the invention. A method of compressing a fracture in a bone is also provided. The implant generates bone compression by itself and can be used either alone or with plates and washers. It is easily inserted into a fracture and also is easily removed from the fracture. The driver which is specially adapted to be used in combination with the implant of the invention aids in the ease of insertion and removal of the implant.

Abstract: A form of calcium carbonate having a blocky rhombohedral crystal structure and properties including a surface area of from about 3 to about 15 m.sup.2 /g, an average discrete particle size of from about 0.2 to about 0.9 micron, wherein the discrete particles have an aspect ratio less than about 2:1, and a particle size distribution such that at least about 60 weight percent of the particles have a size within 50 percent of the equivalent discrete particle spherical diameter, suitable for use as a filler material in papermaking to improve the optical properties of the resulting paper, is disclosed. An accelerated heat-aging process, including embodiments thereof which utilize hydrothermal techniques, for rapidly producing this form of calcium carbonate, and a related form of calcium carbonate having a hexagonal prismatic crystal structure and the same properties, in large quantities to meet the demand of the papermaking industry, as well as a method for using these materials in papermaking, are also disclosed.

Abstract: Azabicyclo[2.2.2]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## ps with a compound of the formula wherein A is MgCl, MgBr or Li.

Abstract: The invention provides compounds of the formula: ##STR1## The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic conditions.