Abstract: Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.

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

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or (C.sub.1 -C.sub.6)alkyl; R.sup.2 is phenyl, pyridyl, thienyl or furyl, and R.sup.2 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo, and trifluoromethyl; R.sup.3 is phenyl, naphthyl, pyridyl, thienyl or furyl, and R.sup.3 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo and trifluoromethyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: An oral drug delivery system having delayed gastrointestinal transit comprising a non-continuous compressible element and an attached controlled release device and which in the expanded form resists gastrointestinal transit; and a modular system for use therein comprising a non-continuous compressible element and an attached receptacle means for receiving and holding a drug-containing orally administrable controlled release device and which in the expanded form resists gastric transit.

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## with a compound of the formula ##STR3## wherein A is MgCl, MgBr or Li.

Abstract: Compounds of the formula ##STR1## which are intermediates in the preparation of 4,5-difluoroanthranilic acid, an intermediate itself in the synthesis of quinolone antibacterials, and methods of preparing these intermediates.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, C.sub.1 to C.sub.4 alkoxy, C.sub.1 to C.sub.4 alkylthio or C.sub.1 to C.sub.6 alkyl and R.sup.2 is a group of the formula ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sup.4 is --CH.dbd.C.sub.2, --CH.sub.2 --YR.sup.5, or --COR.sup.6, R.sup.5 is hydrogen or an acid labile alcohol protecting group, Y is oxygen or sulfur, and R.sup.6 is --NR.sup.7 R.sup.8 or --OR.sup.9 wherein R.sup.7, R.sup.8 and R.sup.9 are independently selected from hydrogen or C.sub.1 to C.sub.6 alkyl, or an alkaline or alkaline earth metal salt thereof, which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.

Abstract: The use of rapamycin prodrugs of formula I as immunosuppressant agents, intermediates formed in the preparation of its prodrugs as well as the prodrugs themselves.

Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.

Abstract: Compounds of the formula ##STR1## which are useful in treating migraine and other disorders, and intermediates used in the preparation of said compounds.

Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2, and the pharmaceutically acceptable salts thereof. The compounds are useful in treating inflammation or other prostaglandin or leukotriene mediated diseases.

Abstract: MUSCARINIC RECEPTOR ANTAGONISTS OF THE FOLLOWING FORMULAE: ##STR1## Muscarinic receptor antagonists, useful especially in the treatment of irritable bowel syndrome, of formula (IA) or (IB) or a pharmaceutically acceptable salt thereof, where R.sup.2 and R.sup.3 are each independently H, halo or C.sub.1 -C.sub.4 alkyl; m is 0, 1 or 2; n is 1, 2 or 3; Y is a direct link, O or S; with the proviso that when n is 1, Y is a direct link; Het is a group of formula (A) or (B), where p is 0, 1 or 2, q is 1, 2 or 3, and r is 0, 1, 2 or 3, with the proviso that the sum of p, q and r is at least 3, the N atom of "Het" being attached to the group (CH.sub.2).sub.n in formula (IA) and to the H atom in formula (IB); and R.sup.1 is a group of formula (a), (b) or Het.sup.1, where R.sup.4 and R.sup.5 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.t OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.t NR.sup.6 R.sup.7, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.

Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and X are as defined below. Such compounds are useful as oncogene inhibitors and antitumor agents.

Abstract: An automatic motorless label applying system includes a supply reel having a continuous carrier strip with a plurality of labels detachably mounted thereon. The strip is directed through an air actuated linear indexing mechanism which includes an upstream solenoid and a downstream solenoid. The upstream solenoid has clamp members which clamp the strip and then move it in a down-stream direction by the upstream solenoid itself moving laterally. The downstream solenoid clamps the strip when the upstream solenoid returns towards its original position. The labels are sequentially detached from the strip and each label is applied to a respective container.

Abstract: An automatic filling system which inserts objects into containers includes a feed hopper. A conveyor conveys a plurality of the objects into the feed hopper. The feed hopper has a discharge station. A collection station is located at the discharge station for disposing the containers in a position for receiving the objects fed from the discharge station. The feed hopper includes a flat inclined disc which receives the objects from the conveyor. The disc is rotated at a sufficiently high speed to cause the objects to move under centrifugal force toward the periphery of the disc. The feed hopper further includes a cylindrical member having an annular wall disposed around the disc and having an upper edge located generally at the same elevation as the upper end of the disc so that objects moving toward the periphery of the disc are moved to the upper edge of the cylindrical member and are conveyed on the upper edge away from the upper end of the disc.

Abstract: An automatic blister system includes an inspection station into which blisters are delivered in seriatim. After inspection the blisters are removed from the inspection station. A transport assembly conveys the blister through the inspection station. A sensor or detector is mounted in the inspection station directed at the path of travel of the blisters. In addition, a high speed camera is in the inspection station which is actuated by the sensor for capturing a picture of the blister. The characteristics of the blister in the picture are then monitored.

Abstract: Improved means for constraining a rumen drug delivery device in a rolled configuration, said means comprising a laminate, which may be perforated, comprising a water-permeable material having a low friction surface in the presence of water, said material being bonded by means of a water-dispersible pressure sensitive adhesive to a repulpable tape, said tape having said water-dispersible pressure sensitive adhesive on both its surfaces; a laminate comprising a flexible, water-permeable polymeric material bonded between the low friction surface material and the repulpable tape; and devices constrained by said means.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein the broken line represents a saturated or an olefinic bond, R.sup.1 and R.sup.4 are each hydrogen or C.sub.1 to C.sub.6 alkyl, and R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 to C.sub.6 alkyl, halogen, C.sub.1 to C.sub.6 alkoxy or C.sub.1 to C.sub.6 alkylthio, and pharmaceutically acceptable salts thereof, pharmaceutical compounds containing the same, methods of preparing the foregoing compounds, and to novel intermediates in the preparation of the foregoing compounds. These compounds are useful as agents in the prevention of neuronal damage in the brain following cerebral ischemia and during the progression of Alzheimer's disease and also as anticonvulsants.

Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.