Abstract: Microbiological control in water systems is achieved with an amount,of 1,3-dibromo-5,5-dimethylhydantoin that is less than the amount of N,N′-bromochloro-5,5-dimethylhydantoin required to achieve the same degree of microbiological control. The methods of combating Escherichia coli and/or Enterococcus faecium in an aqueous medium, and biofilms such as formed by Pseudomonas aeruginosa on surfaces contacted by the aqueous medium, involve introducing into the medium a biocidally effective amount of 1,3-dibromo-5,5-dimethylhydantoin. A microbiological control agent for use in water in accordance with U.S. Environmental Protection Agency regulations is purveyed in containers of a water control agent comprising 1,3-dibromo-5,5-dimethylhydantoin, which containers bear a label having thereon dosage levels pursuant to requirements promulgated by the U.S. Environmental Protection Agency. The 1,3-dibromo-5,5-dimethylhydantoin is used or purveyed either as a product having a large average particle size (e.g.

Abstract: The present invention provides ester compounds, methods of controlling a pest and uses of the ester compounds. The ester compounds are encompassed by formula (1): wherein R represents a C1 to C3 alkyl group. The methods of controlling a pest entail applying the ester compound encompassed by formula (1) to a pest or to a habitat of the pest or both. The uses of the ester compounds encompassed by formula (1) are for controlling pests.

Abstract: A process for the roller compaction and manufacture of a pharmaceutical formulation comprises the steps of adding sodium phenytoin to a vessel of a blender and adding at least one excipient to the vessel. The mixture is blended and transferred to a roller compactor, where pressure is applied to the blend of sodium phenytoin and excipient. Next, the resultant compaction is milled to form a granulation, which is blended a second time and is suitable for further processing into a dosage form. Preferably, the excipients include magnesium stearate, sugar, lactose monohydrate, and talc. In an alternative embodiment, talc is added immediately prior to the granulation being blended for a second time.

Abstract: The present invention relates to novel imidazolidine derivatives of formula I, 1

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di-unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Abstract: Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.

Abstract: Among the enhanced properties of the 1,3-dibromo-5,5-dimethylhydantoins described are their larger average particle sizes, their compactibility even though devoid of a binder, their excellent free-flowing and low-dust properties, and their more appealing aesthetic qualities, as compared to previously known 1,3-dibromo-5,5-dimethylhydantoins. These novel 1,3-dibromo-5,5-dimethylhydantoins can be produced, for example, by concurrently feeding (i) an aqueous solution or slurry formed from an inorganic base and 5,5-dimethylhydantoin, and (ii) a brominating agent, in proportions such that each nitrogen atom is substituted by a bromine atom, thereby forming product which precipitates in an aqueous reaction mixture. The pH of the reaction mixture is maintained in the range of about 5.5 to about 8.5.

Abstract: A process for the dry granulation and manufacture of a pharmaceutical formulation comprises the steps of adding sodium phenytoin to a vessel of a mixer/granulator and adding at least one excipient to the vessel. Heat is then applied from the vessel to the sodium phenytoin and excipient to achieve the desired target temperature. Next, while the heat is applied from the vessel, the sodium phenytoin and excipient are mixed and chopped in the vessel to form a granulation suitable for encapsulating into a dosage form. Preferably, the excipients include magnesium stearate, sugar, lactose monohydrate, and talc. In an alternative embodiment, talc is added after chopping and blended into the formulation to form a blend suitable for encapsulating into a dosage form.

Abstract: The present invention relates to hydantoins of formula I, 1

Abstract: Pseudomonas aeruginosa biofilm on a surface is eradicated or at least reduced using a microbiocidally effective amount of at least one of the following bromine-based microbiocides:

Abstract: The present invention pertains to single morphic forms of a compound selected from 2S-[4-(2,5-dioxopyrrolidin-1-yl)-2S-mercaptobutyrylamino]4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide and 2S-[2S-mercapto-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butyrylamino]-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide, isolable as such.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The antimicrobial efficacy of N-chlorosulfamate solutions, namely buffered aqueous combinations of HClNSO3−(mono-N-chlorosulfamate) and Cl2NSO3 (di-N-chlorosulfamate), herein referred to as “stabilized hypochlorite”, can be markedly enhanced by the addition of certain organic dopants. The dopants themselves are select hypochlorite stabilizing agents, which are known to readily form stable organochloramides when reacted with “free” hypochlorite (HOCl or NaOCl). Highly effective antimicrobial enhancing dopants include 5,5-dialkyl hydantoins, arylsulfonamides, and succinimides. Examples of these include 5,5-dimethylhydantoin, benzenesulfonamide, and succinimide. Other, less effective dopants include glycolurils. Generally, the dopant is present in a minor mole fraction, relative to the molar amount of stabilized hypochlorite present in the enhanced antimicrobial solution.

Abstract: A highly safe and useful therapeutic agent for hypoalbuminaemia contains a hydantoin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof as an effective ingredient: 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to a novel class of N,N′-di substituted hydantoin hydroxamates capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.

Abstract: A highly safe and useful therapeutic agent for hypoalbuminaemia contains a hydantoin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof as an effective ingredient: wherein each of R1 and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. Administration of the compounds substantially increases the serum albumin value of patients suffering from hypoalbuminaemia from abnormal values, and significantly improves the condition of hypoalbuminaemia.

Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Microbiological control is achieved by continuously and inexpensively dosing water in contact with biofilm, or that comes into contact with biofilm, using a highly effective biocide that provides very effective microbiocidal control of planktonic microorganisms and of biofilm species, even where the biofilm infestations have been in existence for long periods of time and thus have encased themselves in a substantial quantity of slimy defensive polysaccharide layers or films. In addition, the biocide used makes possible significant reduction in copper and/or iron surfaces in contact with the water as compared to N,N′-bromochloro-5,5-dimethyl hydantoin. Still other advantages are made possible by the described technology.

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: The present invention relates to methods and compositions for treating selected conditions of the central and peripheral nervous systems employing non-synaptic mechanisms. More specifically, one aspect of the present invention relates to methods and materials for treating seizure and seizure disorders, epilepsy, status epilepticus, migraine, spreading depression, intracranial hypertension; for treating the pathophysiological effects of head trauma, stroke, ischemia and hypoxia; for treating or protecting from the pathophysiological effects of neurotoxic agents such as ethanol; and for treating neurophsyciatric disorders and central nervous system edema by administering agents that modulate ionic concentrations and/or ionic gradients in the brain, particularly ion-dependent or cation-chloride cotransporter antagonists. Electrolyte cotransport antagonists and combinations of such compositions with other agents for treating various conditions are disclosed.

Abstract: This invention relates to pharmaceutical compositions comprising combinations of a GABA agonist, a prodrug thereof or a pharmaceutically acceptable salt of said GABA agonist or said prodrug and an ARI, a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug, kits containing such combinations and methods of using such combinations to treat mammals, including humans, suffering from diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic retinopathy, diabetic microangiopathy, diabetic macroangiopathy, cataracts or foot ulcers.

Abstract: The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.

Abstract: The present invention relates to novel hydantoin compounds represented by formula (I) which shows an inhibitory activity against farnesyl transferase, and thus can be used as an anti-cancer agent, or pharmaceutically acceptable salts thereof, in which R1, R2, R3 and R4 are as defined in the present application. The present invention also relates to a process for preparation of the compound of formula (I), and to an anti-cancer composition comprising the compound of formula (I) as an active ingredient.

Abstract: Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or —Q—R4; R2 and R3 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, —COR8, —CO2R8, —CONR8R10, —OR9, —SO2NR9R10, or —S(O)4R8; R8 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 to C3 alkyl; R11 is hydrogen, —OR12, or —NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alk

Abstract: A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula —CO—, —CH(OH)—, or —NR3— (R3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R1, L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules.

Abstract: Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-dione; and, 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-cyanophenyl)-5-methylimidazoline-2,4-dione.

Abstract: This invention is directed to a stabilized biocidal composition which comprises a mixture of at least one halopropynyl compound, and particularly a halopropynyl carbamate fungicide such as IPBC, a UV absorber and an organic epoxide.

Abstract: Novel diphenylethylene compounds containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.

Abstract: Novel diphenylethylene compounds containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidine compounds, known to lower leptin levels, the present compound increase leptin levels and have no known liver toxicity.

Abstract: A method for the prophylaxis or treatment of conditions for which 5-HT1-like agonists are indicated comprising the administration of therapeutically-effective amount of compounds of formula (I) 1

Abstract: A method for preventing fungal diseases in crops which comprises the steps of: (a) applying to a crop an aqueous or a non-aqueous spray composition which includes a pesticide and a spray adjuvant including a solvent and an emulsifier, wherein the solvent is a mixture of aliphatic hydrocarbons having a distillation range of about 520 to 600° F. and an aromatic content of about 1% or less, or the solvent is a single or combination of C6-C18 fatty alcohol(s); and (b) applying chlorothalonil to the crop previously to, simultaneously with, or subsequently to the application of the aqueous spray composition, wherein phytotoxicity associated with the application of chlorothalonil is reduced or eliminated.

Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.

Abstract: Mammalian subjects may be phenotyped as poor or extensive metabolizers with respect to CYP2C19 by measuring the ratio of R and S mephenytoin or S-mephenytoin to S-4-hydroxymephenytoin produced from racemic mephenytoin in urine, saliva or plasma samples.

Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: Compounds of formula wherein W is —OH or —NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)m moiety by a ring nitrogen, —CONR2R3, —NR1COR2, —NR1SO2R2, —NR1CONR2R3, —NR1COOR4, heteroarylthio, alkylthio, arylalkylthio, heteroarylalkylthio, heterocycloalkylalkylthio, heterocycloalkylthio or arylthio; Y is carbon, nitrogen, oxygen or sulfur, provided that when Y is carbon, n is 2; Z is alkyl, aryl, alkoxy, aryloxy, aralkoxyaryl, aralkoxyheteroaryl, heteroaryl, heterocycloalkyl, heteroaryloxy, —CONR2R3, —NR1COR2, —NR1CONR2R3, —OCONR2R3, —NR1COOR4, or —SO2R2; R1 is hydrogen, alkyl, heterocycloalkylalkyl, aralkyl or heteroarylalkyl; R2 and R3 are independently R1, aryl or heteroaryl; or R2 and R3 taken together with the nitrogen atom to which they are attached form a 5- to 7-membered ring, which may optionally contain another heteroat

Abstract: Disclosed are biocidal compositions comprising mixtures of formaldehyde-releasing imidazolidines, such as 1,3-dimethylol-5,3-dimethylhydantoin, and 3-isothiazolones stabilized with low levels of copper salts.

Abstract: Provided are compositions typically including 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine and [2,5-dioxo-3-(2-propynyl)-1-imidazolidinyl]methyl chrysanthemate, as well as a method of controlling pests.

Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: Novel inhibitors of bone reabsorption and antagonists of vitronectin receptors The present invention relates to 5-membered ring heterocycles of the formula I, in which E, F, G, W, Y and Z have the meaning given in the patent claims, to their preparation and to their use as medicaments. The novel compounds are used as vitronectin receptor antagonists and as inhibitors of bone reabsorption.

Abstract: Hydantoin derivatives for eliminating free radicals and active oxygen which can be easily made into pharmaceutical preparations, show little, if any side effects, and are capable of being administered by the oral route. The pharmaceutical compositions for eliminating the active oxygen and the free radicals contain at least one hydantoin derivative represented by the following formula (I): wherein each of R1 and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. The hydantoin derivatives which have an action of eliminating the active oxygen and the free radicals are, accordingly, useful as pharmaceutical agents for treating a variety of diseases in which active oxygen and free radicals are involved or play a detrimental role.

Abstract: 5-Membered ring heterocycle of the formula I, in which D includes a COOR15, CON(CH3)R15 or CONHR15 radical and R15 includes a 6-24 member bicyclic or tricyclic radical, compositions, preparation and use as inhibitors of thrombocyte aggregation, metastasization of carcinoma cells, binding of osteoclasts to bone surfaces and for the treatment of tromboses.

Abstract: The present invention provides for the treatment of non-insulin dependent diabetes mellitus or obesity comprising the systemic administration of a compound having the formula or a pharmacologically acceptable salt thereof, wherein each R is H or NH2, and with the proviso that at least one R group must be NH2.

Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules.