Abstract: The present invention relates to compositions containing at least one metal chelate, at least one phosphonate salt, and at least one phosphate salt, which are used as fungicides and bactericides, and methods of using the compositions.

Abstract: Antimicrobial formulations, which may be essentially free of an antimicrobial active, comprising one or more proton donating agents and an alkyl phosphate anionic surfactant comprising a mono alkyl phosphate having the chemical structure: 1

Abstract: Bile-acid conjugates useful for sustained release of L-DOPA, inhibitors of catechol O-methyl transferase and/or inhibitors of L-aromatic amino acid decarboxylase are provided.

Abstract: The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.

Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: Methods of synthesizing a phosphate ester of combretastat-in A-4 and trans-isomers thereof in which combretastatin A-4 is reacted with dibenzylphosphite in the presence of carbon tetrabromide, or with 2,2,2-trichloroethyl phosphorodichloridate, to form a phosphate ester of combretastatin A-4 with protecting groups thereon.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: An anti-depressant, mental & emotional stress suppressor and mood improver having a prominent action for decreasing blood cortisol level and serotonin reuptake and has an effect of alleviating symptoms associated with depression and mental & emotional stress of a subject administered with the improver. The improver contains as the effective ingredient a combination of phosphatidy-L-serine and phosphadtidic acid, or the salts thereof, comprising at least 20% (w/w) phosphatidy-L-serine and typically within the range of about 20%-40% of phosphatidy-L-serine, out of the total phospholipid content of the composition and at least 3% (w/w) of phosphatidic acid, preferably above about 10% and typically within the range of about 20%-40% of phosphatidic acid, out of the total phospholipid content of the composition.

Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treatment or prophylaxis of undesired thrombosis.

Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of ore or more aquatic organisms in a column of water. The complexes comprise a least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: Applicant has probed the Edg2 lysophosphatidic acid (LPA) receptor with a series of LPA analogs to determine receptor activation. The present invention is drawn to a series of LPA analogs which function as Edg2 receptor agonists, and methods of using such compounds to activate the Edg2 receptor of the surface of a cell. The compounds of the invention comprise a glycerol backbone with an Sn1 ester-linked saturated or unsaturated alkyl group, substitutions of the hydroxyl group (—OH) at carbon two of the glycerol backbone, and optional replacement of the phosphate di-anion with either a hydroxyl group or a dimethylated phosphate. These LPA analogs may find uses in cancer and neurological disorders.

Abstract: A fungicidal composition for plants containing phosphonate (PO3) and phosphate (PO4) salts, and derivatives thereof is disclosed. The composition provides a single product which may be employed to control a Phytophthora infestans infection in plants.

Abstract: The present application relates to the use of compounds that influence the sex hormone system for the treatment of wounds and/or fibrotic disorders. Preferred compounds for use in such treatments are steroid hormones and especially the oestrogens.

Abstract: The enzyme Lp-PLA2 in purified form, an isolated nucleic acid molecule incoding Lp-PLA2, the use of an inhibitor of the enzyme Lp-PLA2 in therapy and a method of screening compounds to identify those compounds which inhibit the enzyme.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: 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 possess a &bgr;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &bgr;-lactamase inhibitors and as antibiotics.

Abstract: A fungicidal composition for plants containing phosphonate (PO3) and phosphate (PO4) salts, and derivatives thereof is disclosed. The composition provides a single product which may be employed to control a Phytophthora infestans infection in plants.

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

Abstract: Disclosed is a method of inhibiting or preventing a condition associated with undesired secretion of a macrophage inflammatory protein using inhibitors of ATP-sensitive K+-channels, inhibitors of the Na+/H+ antiporter, inosine, or inosine analogs.

Abstract: The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.

Abstract: 1

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: This invention relates to a method of treating patients afflicted with acute renal failure. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: A pharmaceutical formulation for stimulating growth of Gram-positive Bacilli and increasing the acidity in vagina comprises sucrose and/or maltose, optionally with other sugars, viscous base, and anti-fungal and/or anti-bacterial agents.

Abstract: Disclosed is a polycarbonate resin composition comprising an aromatic polycarbonate (PC), a high-impact polystyrene resin (HIPS) and a non-halogen phosphate, and also talc and/or polytetrafluoroethylene (PTFE). Optionally, the composition may contain a core/shell-type, grafted, rubber-like elastic material. The composition has good flame retardancy and has good physical properties such as stiffness, impact resistance, outward appearance and flowability.

Abstract: A stabilized two-part disinfecting system comprising a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition. The first part contains a non-esterifying acid and an alcohol-containing humectant or antifreeze, while the second part contains a salt of an organic acid and an optional metal chlorite. Methods for making a disinfecting composition by mixing the two-part disinfecting system, as well as for disinfecting substrates by contact therewith, are also disclosed.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: This invention relates to a method of treating patients afflicted with hangover. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: A fertilizer composition for plants containing phosphonate and phosphate slats, and derivatives thereof is disclosed. The composition provides a single product which may be employed to stimulate the growth response in plants.

Abstract: The present invention relates to a pharmaceutical composition and a method for treating a compulsive disorder using a NAALADase inhibitor.

Abstract: Polyribosylribitol phosphate oligosaccharides are produced in a multistep process. The compound of the formula: ##STR1## wherein R.sub.1 is a first protecting group and R.sub.2 is a second protecting group, is coupled to a solid polyethylene glycol monomethyl ether (PEG) support. Following removal of the first protecting group, the resulting compound is coupled with a repeating unit for chain elongation of the formula: ##STR2## The protecting group is removed from the phosphorus atom and the steps of removing the first protecting group, coupling with the repeating unit is repeated until the desired number of repeating units in the oligomer has been terminated. The oligomer then is terminated with a chain terminating molecule of the formula: ##STR3## wherein m is an integer and R.sub.3 is a third protecting group.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: A fungicidal composition for plants containing phosphonate and phosphate salts, and derivatives thereof is disclosed. The composition provides a single product which may be employed to control a parasitic fungi in plants through mitigation of pathological acerbation of certain fungi.

Abstract: This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: ##STR1## or pharmaceutically acceptable salts thereof wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or ##STR2## and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources;R.sub.3 is hydrogen or lower alkyl andR.sub.

Abstract: Phosphopeptides which significantly reduce bone loss or weakening are provided by the invention. Also provided is a method for treating or preventing any condition associated with bone loss or weakening by administering the phosphopeptides by oral or injectable means.

Abstract: Acyloxyalkyl esters of phosphate-containing second messengers which are capable of permeating cell membranes. Once inside the cell, the ester derivatives undergo enzymatic conversion to the biologically active form of the second messenger. The acyloxyalkyl esters have the formula: ##STR1## wherein A.sub.1 to A.sub.6 is H, OH, F or ##STR2## wherein R is an alkyl group having from 2 to 6 carbon atoms and R' is H or CH.sub.3 or R is CH.sub.3 and R' is CH.sub.3 and wherein at least one of A.sub.1 to A.sub.6 is a phosphoester having the formula set forth above.

Abstract: Chronic HIV infection is treated by administering to a subject an organic thiophosphate alone or in combination with another anti-HIV or anti-AIDS drug. The organic thiophosphate is preferably WR 151327, a compound with antioxidant and free radical scavenging activities, or a functional derivative or analogue thereof. WR 151327 suppresses induction of HIV expression in chronically infected cells mediated by cytokines such as TNF.alpha. and GM-CSF. Pharmaceutical compositions comprising at least one organic thiophosphate in combination with one or more anti-HIV or anti-AIDS drugs are also disclosed.

Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.

Abstract: Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.

Abstract: The invention relates to an inositol phosphate containing pharmaceutical composition which comprises an aliphatic ester or ether for improvement of the bioavailability of the inositol phosphate in mammals including man at non-parenteral administration. The invention also covers the use of at least one aliphatic ester or ether compound for the preparing of an inositol phosphate containing medicament with improved bioavailability of inositol phosphate in mammals including man at non-parenteral administration.

Abstract: The present invention is directed to plasmalogens and pharmaceutical compositions thereof which are useful for treating neurodegenerative diseases. Carbons 1 and 2 of the phosphoglyceryl backbone of the plasmaolgens have from 10-24 carbon atoms containing from 1 to 6 double bonds. The phosphoryl group is bonded to choline, ethanolamine, serine or inositol.

Abstract: The present invention relates to liquid formulations of endosulfan in the form of suspension concentrates which comprise a surfactant combination of a phosphoric ester based on an ethoxylated alkylphenol and an ethoxylated alkylaryl- and alcohol phosphate ester, to processes for their preparation, and to their use in crop protection.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: The present invention comprises dipropylene glycol dibenzoate and diethylene glycol dibenzoate, the improvement comprising the addition of dipropylene glycol monobenzoate or diethylene glycol monobenzoate, whereby the plasticizer is resistant to fungal growth.