Abstract: Compounds of the formula: ##STR1## wherein: X is O, NH or NR.sup.1 ; R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl or aryl (C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R.sup.3 is NH.sub.2, --NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.

Abstract: A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.

Abstract: The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds and the pharmaceutically acceptable salts or prodrugs thereof, depicted below, which are .beta.-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. More specifically, the compounds of the instant invention are selective agonists of .beta..sub.3 -adrenergic receptor. The invention also relates to methods of use for the compounds and to pharmaceutical compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving the lean meat to fat ratio in animals, e.g., ungulate animals, companion animals and poultry. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z are as defined in the specification.

Abstract: The invention provides novel compounds having the formula: ##STR1## wherein R when taken individually is H; R.sup.1 when taken individually is H or OH; R and R.sup.1 when taken together represent a double bond;R.sup.2 is an alpha-branched C.sub.3 -C.sub.8 alkyl, alkenyl, alkynyl, alkoxyalkyl or alkylthioalkyl group; a C.sub.3 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl or C.sub.5 -C.sub.8 cycloalkylalkyl group, any of which may be substituted by methylene or one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms;R.sup.3 is hydrogen or methyl;R.sup.4 is H or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy with the proviso that when R.sup.2 is alkyl it is not isopropyl or sec-butyl; when R.sup.4 is H, each of R and R.sup.1 is H, and R.sup.2 is not methyl or ethyl; and when R.sup.

Abstract: A method of treating tinnitus in a mammal in need of such treatment, in which the method comprises administering a therapeutically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 14 R.sup.4 are as defined herein.

Abstract: The present invention provides a vaccine to treat or prevent mastitis in a bovine species, comprising an immunologically effective amount of a plasminogen-activating streptokinase protein produced by Streptococcus uberis. The present invention further provides a method of treating or preventing mastitis in a bovine species comprising vaccinating a cow with an immunologically effective amount of a plasminogen-activating streptokinase protein produced by S. uberis. The present invention further provides an isolated plasminogen-activating streptokinase protein produced by S. uberis, or an immunogenic fragment thereof.

Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.

Abstract: Darifenacin, and its pharmaceutically acceptable salts, are useful in the treatment of cognitive impairment. The invention also discloses the use of combinations of darifenacin, or a pharmaceutically acceptable salt thereof, with an acetylcholinesterase inhibitor, in the treatment of cognitive impairment.

Abstract: A compound of the following formula: ##STR1## and its pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, phenyl or phenyl-C.sub.1-4 alkyl; or R.sup.1 and R.sup.2 are taken together with the nitrogen to which they are attached and form optionally substituted, saturated or unsaturated 3-, 4-, 5-, 6- or 7-membered heterocyclic cantaining one to two heteroatoms, provided that the heterocyclic is not pyrrolidinyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or a hydroxy protecting group;Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkyloxy, CF.sub.3 and carboxy-C.sub.1-4 alkyloxy; andX is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C.sub.

Abstract: Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl;X is --CONR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CH.sub.2 OR.sup.3, --CH.sub.2 NR.sup.3 R.sup.4 or --CONR.sup.3 OR.sup.4 ;R.sup.1, R.sup.3 and R.sup.4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.

Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.

Abstract: A fluid dispensing device for use with a fluid reservoir having a cup having a bottom wall and a top wall, the top wall including an orifice to permit removal of fluid from the cup and with the top wall having a threaded axial opening, the bottom wall being coupled to a conduit adapted for communication with fluid in a reservoir; and a column rotatably positioned in the axial opening and extending therefrom into and out of the cup, the column including an orifice positioned in the cup, the column including a threaded portion being cooperative with the threaded axial opening such that the position of the column orifice in the cup can be varied through a vertical range of movement by rotation of the column, and the column further including a tubular portion being in fluid communication with the column orifice and with the conduit and movable relative to the conduit while substantially maintaining a seal therebetween throughout the vertical range of movement of the orifice in the cup.

Abstract: This invention provides a compound of the following formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen, C.sub.1 -C.sub.5 alkyl or an O-protecting group; B is a dircet bond, C.sub.1 -C.sub.5 alkylene or C.sub.2 -C.sub.5 alkenylene; R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.3 alkyl; R.sup.2 is hydroxy or C.sub.1 -C.sub.5 alkoxy; R.sup.3 is hydrogen, hydroxy or C.sub.1 -C.sub.5 alkoxy; and R.sup.4 is hydrogen, phenyl or heteroaryl selected from furyl, thienyl and pyrrolyl, the phenyl and heteroaryl being optionally substituted by one to five substitutents selected from halo, hydroxy, C.sub.1 -C.sub.3 allyl, C.sub.1 -C.sub.3 alkoxy and C.sub.2 -C.sub.5 alkenyl.

Abstract: The present invention relates to a topical protein preparation to be used for the therapy of periodontitis and diseases of the teeth and of the tissues of the oral cavity, comprising a mixture of transferrin with at least one protein selected from albumins, lysozymes, protease inhibitors, and mixtures thereof.

Abstract: Use of droloxifene in the treatment of cardiovascular diseases.

Abstract: An osmotic device that, following the imbibement of water vapor, provides for the controlled release of a beneficial agent to an aqueous environment. The device comprises a hydrophilic formulation including a beneficial agent, and if needed, an osmagent, surrounded by a wall. The wall is formed at least in part of a semipermeable hydrophobic membrane having an average pore size between about 0.1 .mu.m and 30 .mu.m. The pores are substantially filled with a gas phase. The hydrophobic membrane is permeable to water in the vapor phase and the hydrophobic membrane is impermeable to an aqueous medium at a pressure less than about 100 Pa. The beneficial agent is released, for example, by osmotic pumping or osmotic bursting upon imbibement of sufficient water vapor into the device core.

Abstract: This invention relates to compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, this invention relates to synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.

Abstract: A child-resistant, elderly-accessible safety container designed for storage of potentially hazardous materials. The closure includes three major components: a rotatable member secured coaxially around the neck of the container and having at least one biasing member disposed along its upper surface, at least one resilient abutment member, extending outward from the neck and terminating in a tip end, and is capable of being distended or compressed by the biasing member, and a closure member having at least one closure member stop disposed along its inner surface. Turning the rotatable member in a predetermined direction causes the biasing member to contact and compress the abutment member tangentially in relation to the outer surface of the neck. Such compression interrupts contact of the tip end of the abutment member with the closure member stop allowing the closure member to be rotated in the opposite direction and removed from the container.

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.