Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.

Abstract: The present invention relates to an agent for the expression of long-term potentiation of synaptic transmission, which contains a compound having a brain somatostatin activation property as an active ingredient and to a screening method of an agent for the expression of long-term potentiation of synaptic transmission, which uses a soniatostatin releasing property as an index. The present invention is useful for the prophylaxis and/or treatment of cerebral diseases of dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease and the like.

Abstract: The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective amount of a mitochondrial electron transport inhibitor or a pyrimidine compound of formula I.

Abstract: Composition of matter for application to a body surface or membrane to administer asimadoline by permeation through the body surface or membrane, the composition comprising asimadoline to be administered, at a therapeutically effective rate, alone or in combination with a permeation enhancer or mixture. Also disclosed are drug delivery devices and methods for the transdermal administration of asimadoline.

Abstract: The present invention is drawn to a therapeutic drug for micturition disorders and diseases of the lower urinary tract system, containing an organic acid salt of [2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]ethyl]-dimethylsulfonium. The invention enables treatment of diseases of the lower urinary tract system which cause urinary disorders, such as interstitial cystitis and prostatitis, which arise from unelucidated causes and thus are regarded intractable diseases.

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Abstract: The S-isomer of a compound represented by the following formula: and pharmaceutically acceptable salts thereof is disclosed as being useful for treating urinary disorders, including urinary incontinence, and gastrointestinal disorders, including gastrointestinal hyperativity.

Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.

Abstract: Use of a compound of formula (I) wherein R1 is an optionally substituted straight- or branched carbon chain having 12 to 22 carbon atoms which may be optionally interrupted by an optionally substituted phenylene, and each of R2, R3, R4 and R5, independently, is H or lower alkyl, in free form or in pharmaceutically acceptable salt form, in the prevention or treatment of chronic rejection in a recipient of organ or tissue allo- or xenotransplant, or of acute rejection in a xenograft transplant recipient.

Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.

Abstract: This invention relates to a single phase emulsifiable concentrate composition comprising (a) between about 0.05 and about 25 wt. % of a biologically, fungicidally and/or herbicidally active aza compound; (b) between about 2 and about 40 wt. % of a lactam selected from the group of N-methyl pyrrolidone, N-methyl caprolactam, a C8 to C18 alkyl pyrrolidone, a C8 to C18 caprolactam and a mixture thereof; (c) between about 2 and about 20 wt. % of a moisture scavenging agent selected from the group consisting of a liquid molecularly hindered carbodiimide, a molecular sieve or a mixture thereof and (d) between about 10 and about 80 wt. % of a mixture of at least two non-ionic surfactants having an overall hydrophilic/lipophilic balance (HLB) above 7. The invention also relates to the stable oil-in-water (o/w) miniemulsions prepared from the above by dilution to between about 40 and about 99.99 wt. % water for a “pour on”, dip or spray solution useful in the treatment of animals or plants.

Abstract: Composition and methods of alleviating impaired mental function and memory loss in mammals and reducing the recovery time from anaesthesia in age mammals, comprising treating the mammal with a non-toxic, enhancing effective amount of a cell membrane permeant calcium buffer. The buffer is preferably a calcium ion chelating agent having a KD selected from the range 1×10−4 to 1×10−8 Molar and being essentially calcium ion-selective over other metal ions. A most preferred buffer is BAPTA-AM.

Abstract: An anti-inflammatory analgesic patch containing loxoprofen, crotamiton, solvent, skin permeation accelerator, water-soluble polymers and moisturizers. The patch allows for the loxoprofen to penetrate the skin.

Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.

Abstract: Methods and compositions, useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's Disease (AD). These methods involve administering to a subject a pharmaceutical composition including one or more agents which modulate APP catabolism and amyloid deposition. Accordingly, the methods and compositions are useful for inhibiting amyloidosis in disorders in which amyloid deposition occurs. The methods are based, at least in part, on modulating catabolism of APP in APP-containing cells through the use of a mobile ionophore, such as carbonyl cyanide p-(trifluoromethoxy)phenylhydrazone, which does not substantially alter the viability of those cells.

Abstract: The present invention relates to non-secosteroidal compounds which activate and modulate the vitamin D receptor (VDR). Because compounds of the present invention display many of the beneficial properties of 1,25(OH)2D3, but with reduced calcium mobilization effects, they may be used advantageously to treat and prevent conditions that show vitamin D sensitivity. Such disease states typically show abnormal calcium regulatory, abnormal immune responsive, hyperproliferative, and/or neurodegenerative characteristics.

Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.

Abstract: The invention relates to compounds of formula (I) ##STR1## wherein R.sub.1 is an electronegative substituent, preferably nitro, cyano, formyl or carboxy, R.sub.2 is --A--R.sub.4, wherein A is a branched or straight chain C.sub.1-9 alkylene and R.sub.4 is carboxy or 5-tetrazolyl; R.sub.3 is an electronegative substituent, preferably nitro, cyano, halogen, formyl, carboxy, C.sub.1-5 alkyl carbonyl, aryl carbonyl or SO.sub.2 R.sub.6, wherein R.sub.6 is a branched or straight chain C.sub.1-5 alkyl, aryl alkyl, aryl or NR.sub.7 R.sub.8, wherein R.sub.7 and R.sub.8 are independently hydrogen, a branched or straight chain C.sub.1-5 alkyl or together form a C.sub.3-6 ring; or a pharmaceutically acceptable ester or salt thereof. The compounds are peripheral, long acting COMT (catechol-O-methyl transferase) inhibitors and are useful, e.g., in the treatment of Parkinson's disease and hypertension.

Abstract: The present invention relates to heavy metal chelate compositions, which are used as fungicides and bactericides, and methods of using the compositions. In particular, the present invention relates to a chelate, that is an EDDHA (copper-ethylenediamine-di-o-hydroxyphenylacetic acid), combined with a heavy metal, including iron, tin, zinc, manganese, copper, and combinations thereof.

Abstract: Compounds of general formula (I) ##STR1## wherein X ia a --CO.sub.2 H, --NH(OH)CHO or --CONHOH group; R.sub.1 is a cylcoalkyl, cycloalkenyl or non-aromatic heterocyclic ring containing up to 3 heteroatoms, any of which may be (i) substituted by one ore more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, halo, cyano (--CN), --CO.sub.2 H, --CO.sub.2 R, --CONH.sub.2, --CONHR, --CON(R).sub.2, --OH, --OR, oxo-, --SH, --SR, --NHCOR, and --NHCO.sub.2 R wherein R is C.sub.1 -C.sub.6 alkyl or benzyl and/or (ii) fused to a cycloalky or heterocyclic ring; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in specification are matrix metalloproteinase inhibitors.

Abstract: An environmentally safe method of killing insects and arachnids is disclosed herein. Insects and arachnids can be killed by the direct application of a solution of surfactant comprising between 0.01% and 10% of an alkali metal or ammonium salt of C.sub.6 to C.sub.14 dialkyl sulfosuccinate. The alkali metal or ammonium salt of C.sub.6 to C.sub.14 dialkyl sulfosuccinate can be applied with attractants to surfaces near or at surfaces where the elimination of arachnids or insects is needed.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: The present invention relates to phenylethanolamine compounds represented by general formula [I]: ##STR1## (where R.sub.1 represents hydrogen or halogen; R.sub.2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted with lower alkylaminocarbonyl which may be substituted with lower alkoxy, lower alkoxy substituted with cyclic aminocarbonyl of 4 to 6 carbon atoms, lower alkoxycarbonyl or carboxy; R.sub.3 represents hydrogen, hydroxy, lower alkoxy or lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups; R.sub.2 and R.sub.3 may be bonded to each other to form methylenedioxy substituted with carboxy or lower alkoxycarbonyl; and m and n are 0 or 1), and their pharmacologically acceptable salts, which have a potent .beta.3 adrenergic stimulating effect and high .beta.3 adrenergic receptor selectivity, as well as to processes for their production and intermediates in their production.

Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention provides a method and composition for controlling the growth of microorganisms in aqueous systems, such as industrial process waters. The method includes the steps of adding a synergistically effective amount of a biocide, 2-bromo-2-nitrostyrene ("BNS"), and an oxidant, peracetic acid, to industrial process waters to control microorganism growth. The composition of the present invention comprises a synergistically effective amount of a biocide, 2-bromo-2-nitrostyrene, and an oxidant, peracetic acid, to control microorganism growth. The method and composition of the present invention are particularly effective in the treatment of pulp and paper water processing systems.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.7)--, where R.sup.7 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an alkyl, --CO.sub.2 R.sup.8 (where R.sup.8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), --CONR.sup.9 R.sup.10 (where R.sup.9 and R.sup.10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), --CSNR.sup.9 R.sup.10, --CN, --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- (where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.

Abstract: Disclosed are drink mix compositions comprising a therapeutically effective dose of an anion exchange resin, and xanthan gum. These compositions may also contain one or more carriers wherein the compositions are in a form mixable with a liquid to form a suspension of the anion exchange resin and xanthan gum.

Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.

Abstract: Disclosed are methods and compositions for reducing coronary artery stenosis, restoring blood flow to infarcted myocardium, improving myocardial perfusion, reducing heart attacks or other adverse cardiovascular events, or treating symptoms of inadequate myocardial function in a mammal involving administering to the mammal (a) a compound that includes eicosapentaeneoic acid or docosahexaeneoic acid and (b) a cholesterol-lowering therapeutic, combined with dietary restrictions (resulting in aggressive loading of marine lipids), whereby a serum LDL concentration of less than 75 mg/dl (and preferably less than 55 mg/dl) is achieved. One particular method involves administering to the mammal a combination that includes (a) a compound that includes an eicosapentaeneoic or docosahexaeneoic acid (for example, a marine lipid) and (b) a cholesterol synthesis or transfer inhibitor, and which may also optionally include aspirin and/or niacin.

Abstract: Disclosed is a method of inhibiting the growth of marine organisms on a marine structure, by applying onto or into the marine structure a phenylamide compound. These compounds may be directly incorporated into the marine structure during manufacture, directly applied to the structure, or applied to the structure by means of a coating.

Abstract: Bi-aromatic compounds are provided along with methods for their preparation and use.

Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth are disclosed. The method comprises administering a nitroso or nitrone spin trap such as N-t-butyl-.alpha.-phenylnitrone (PBN) to the affected tissue.

Abstract: A phytosanitary composition, characterized in that it contains a combination of an oxynil and at least one substance selected from the group consisting of herbicides, insecticides, fungicides, growth regulators and/or pesticides, this substance which is liquid at ambient temperature being intended to keep the oxynil in the liquid state at the application site, if necessary after it has been brought into the liquid state.

Abstract: Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.

Abstract: Chlorothalonil compositions which are useful in formulating aqueous pesticidal sprays in which zinc oxide is present as a micronutrient; the compositions are particularly useful for application to potatoes.

Abstract: The use of novel compositions for preserving aqueous systems normally subject to spoilage is disclosed. The compositions incorporate an antimicrobial agent into an inert and biodegradable carrier. The resulting compositions are stable, active, non-toxic, non-corrosive, biodegradable, compatible with ecosystems while having a flash point above 200.degree. F. and a pleasant odor.

Abstract: A percutaneous absorption preparation comprising a support and, formed on one side thereof, a plaster layer comprising a pressure-sensitive adhesive and tulobuterol in an amount not lower than its saturation solubility in the pressure-sensitive adhesive, the tulobuterol contained in the plaster layer consisting of dissolved tulobuterol and crystalline tulobuterol with the ratio of the content of the crystalline tulobuterol to that of the dissolved tulobuterol being from 0.1 to 10.

Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.

Abstract: A method is provided for preventing or reducing the risk of hypertension in normotensive patients having insulin resistance by administering a cholesterol lowering drug, such as pravastatin, alone or in combination with an ACE inhibitor, especially one containing a mercapto moiety, such as captopril or zofenopril.

Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as etridiazole, potassium bicarbonate, sodium carbonate, potassium oleate, potassium caprylate and xanthan gum. The combination of potassium oleate, potassium caprylate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.

Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as pentachloronitrobenzene, sodium bicarbonate, sodium carbonate, potassium oleate, potassium octanoate and xanthan gum. The combination of potassium oleate, potassium octanoate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.

Abstract: A microbial inhibiting composition and method is disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and B-bromo-B-nitrostyrene. The method comprises administering an amount of this combined treatment to the particular water containing system for which treatment is desired.

Abstract: An aromatic compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.3 -C.sub.8 alkyl group, a C.sub.3 -C.sub.8 alkoxy group, an alkoxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkenyloxy group, an alkenyloxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 haloalkyl group, a C.sub.3 -C.sub.8 alkoxy group, a haloalkoxyalkyl group having 3 to 8 carbon atoms, a C.sub.3 -C.sub.8 haloalkenyl group, a C.sub.3 -C.sub.8 haloalkenyloxy group, a haloalkenyloxyalkyl group having 3 to 8 carbon atoms or a C.sub.3 -C.sub.8 alkynyloxy group; R.sup.2 is a halogen atom; R.sup.3 is, the same or different, a hydrogen atom, a halogen atom or a methyl group; R.sup.4 is a hydrogen atom or a methyl group R.sup.5 is, the same or different, a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 haloalkoxy group, a C.sub.1 -C.sub.4 alkylthio group, a C.sub.1 -C.sub.

Abstract: An antifungus composition in dry spray form contains in combination at least one antifungus agent of the family of allylamines, a noncyclized silicone polymer, a mineral or organic charge and a gas propellant. This composition is useful in the treatment of mycoses.

Abstract: Synergistic compositions for inhibiting microbial growth contain synergistic mixtures including 2-(2-bromo-2-nitroethenyl)furan ("BNEF") and a compound selected from the group consisting of beta-nitrostyrene ("NS"), beta-bromo-beta-nitrostyrene ("BNS"), methylchloro/isothiazolone ("IZN"), methylenebisthiocyanate ("MBT"), 2,2-dibromo-3-nitrilopropionamide ("DBNPA"), 2-bromo-2-bromomethyl-glutaronitrile ("BBMGN"), alkyldimethylbenzylammonium chloride ("ADBAC"), and beta-nitrovinyl furan ("NVF"). The synergistic compositions are effective against a wide spectrum of bacteria, algae and fungi. An antimicrobial composition comprising the synergistic mixture and a carrier is also disclosed.

Abstract: The invention concerns new diorganotin compounds derived from N-cyclohexyl-N'-hydroxy diazenium oxide, as well as bactericides and fungicides which are suitable as disinfectants, as preservatives for wood and other materials, for bactericidal and fungicidal finishing of textiles, plastics, building materials or as biocides for paint systems and which contain these diorganotin compounds as active ingredients.

Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a special protein tyrosine kinase inhibitor; and(ii) a cosmetically acceptable vehicle for the inhibitor.

Abstract: Disclosed are compositions and methods of treating oak wilt, decline, or other fungus-induced diseases of trees. A mixture is applied to the root system comprising sulfur and pentachloronitrobenzene or pentachlorophenol as its active ingredients, and optionally other ingredients such as a wetting agent, nitrogen, an insecticide, and a nutrient source. It is preferable to simultaneously treat the bark and crown of the tree with a composition which includes a fungicide and an insecticide. Other ingredients, such as a wetting agent or a fungicide/nutrient, can also be present in the Bark & Crown Composition.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.