Abstract: There is disclosed the use of a compound containing a high density negatively charged domain of vicinally oriented radicals for the preparing of a medicament for preventing, alleviating or combating restenosis in mammals including man.

Abstract: A method for producing the health-benefits of exercise including (but not limited to) the treatment and prevention of cachexia, other wasting disorders, cancer, atherosclerosis, heart disease, acute or chronic autoimmune disease, chronic inflammatory disease, alcoholic hepatitis, non-alcoholic hepatitis, rheumatoid arthritis, osteoarthritis, type II diabetes, insulin insensitivity, Parkinson's disease, Alzheimer's disease, and any other condition caused or mediated by chronic oxygen radical damage or by chronic chemical toxicities using diacylglycerol or any of its' derivatives or analogues; phospholipids, including but not limited to phosphatidylinositol or any of its' derivatives or analogues; hydrogen peroxide; any lipid peroxide or lipid-soluble peroxide (including but not limited to short-, medium-, or long-chain fatty acid peroxides); any water soluble peroxide derivative which retains any of the reactive properties of the original peroxide; oxygen radical generating system capable of generating superox

Abstract: The present invention relates to methods for regulating the release of TGF-&bgr; from living cells in vitro or in vivo, comprising bringing the cells into contact with an effective amount of a NAALADase inhibitor. Such methods are believed to be useful for affecting neuroregeneration, cell proliferation, cell differentiation, extracellular matrix formation, myelination, inflammation, immune function, liver function, pancreatic function, angiogenesis, or wound healing; and/or for preventing or treating diabetes.

Abstract: This invention is directed to pharmaceutical compositions and methods for treating demyelinating disorders based upon inhibitors of the interaction of glutamate with the AMPA and of the interaction of glutamate with the kainate receptor complex.

Abstract: A method and device are disclosed which prevent the intrusion of insects onto wood structures by using a barrier capable of retaining pesticide. In the disclosed method, the barrier maintains a minimal effective level of insecticide for a predetermined period of time.

Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.

Abstract: The present invention relates to pharmaceutical compositions and methods for treating opioid tolerance using NAALADase inhibitors.

Abstract: Chemically stable, insecticidally active pellets having a low moisture content and at least about 95% active ingredient are described, as well as a method for manufacturing them. The active ingredient is selected from a class of N-hydrocarboyl phosphoroamidothioate and phosphoroamidodithioate compounds as described in the specification. The pellets generally have a moisture content of about 0.5% by weight or less, preferably less than about 0.3% by weight. The pellets can be produced by one of two types of processes as described in detail, including a high pressure axial extrusion process and a low pressure basket extrusion process.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.

Abstract: A method for treating or preventing chronic obstructive pulmonary disease (COPD) by using as active agent a non-glucorticoid steroid, analogue thereof, such as dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEA-S), or their salts, in an amount effective for preventing or treating COPD.

Abstract: Method for controlling harmful organisms in genetically modified vegetable plants containing a gene derived from Bacillus thuringiensis, said gene encoding and expressing a protein with an insecticidal action, wherein an insecticidally active quantity of one or more compounds from the following groups (a) to (f) is applied to the plants, their seeds or propagation material and/or the area in which they are cultivated:

Abstract: A food additive useful for lowering serum cholesterol in humans contains a sterol or stanol ester of a fatty acid or a dicarboxylic acid ester of a sterol or stanol made by reacting a sterol, stanol and a carboxylic acid in the presence of an effective amount of a catalyst selected from the group consisting of calcium oxide, calcium hydroxide, a calcium salt of a carboxylic acid, magnesium hydroxide and combinations thereof described herein below.

Abstract: The invention provides methods of inhibiting cerebral amyloid angiopathy. The invention further provides methods of treating a disease state characterized by cerebral amyloid angiopathy in a subject with an A&bgr;40 inhibitor having the structure: Q-[—SO3−X+]n or Q-[—OSO3−X+]n wherein Q is a carrier group; X+ is a cationic group; and n is one.

Abstract: This invention concerns the compounds of formula 1

Abstract: A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.

Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: 1

Abstract: A chemical agent of the diterpene family obtained from a member of the Euphorbiaceae family of plants for use in the treatment of prophylaxis of prostate cancer or a related cancer or condition.

Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.

Abstract: Compounds of the general class of substituted pentanedioic acids, where the substituted moiety might be (subclass 1) a sulfanyl alkyl group; (subclass 2) an halogenated benzyl and a phosphinyl group; (subclass 3) a phosphonomethyl group, may be used for prevention, management and/or treatment of hyperaggressive behavior arising from environmental or social conditions, injury or disease, as may [2-(pentafluorophenylmethyl) hydroxyphosphinyl]methyl-pentanedioic acid, and/or other related substituted pentanedioic acids that inhibit NAALADase or mimic NAAG, and/or 2-(phosphonomethyl)-pentanedioic acid (2-PMPA) and/or beta-N-acetyl-aspartyl-glutamate (NAAG) and/or alpha N-acetyl-aspartyl-glutamate.

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 &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: 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: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)methylphosphinic acid; ii) (S)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iii) (R)-(3-amino-2-hydroxypropyl)methylphosphinic acid; iv) (3-amino-2-hydroxypropyl)difluoromethylphosphinic acid; and v) (3-amino-2-oxopropyl)methylphosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

Abstract: The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.

Abstract: Disclosed and claimed are prodrugs activated by catalytic proteins, such as enzymes and catalytic antibodies. The invention comprehends such prodrugs, as well as haptens, to elicit catalytic antibodies to activate the prodrugs. The prodrugs are useful as cytotoxic chemotherapeutic agents; e.g., as antitumor agents.

Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.

Abstract: In various aspects, the invention provides compounds that bind to one or more RANTES receptors for the treatment of chemokine mediated disease states, such as compounds of formula (I): 1

Abstract: The present invention provides a hair-growing agent comprising, as an active ingredient, a phosphatidic acid represented by formula (I): (wherein R1 represents alkyl, alkenyl, alkanoyl or alkenoyl; and when R1 represents alkyl or alkenyl, R2 represents alkyl, alkenyl, alkanoyl or alkenoyl, and when R1 represents alkanoyl or alkenoyl, R2 represents alkyl or alkenyl).

Abstract: The present invention provides a hair-growing agent comprising, as an active ingredient, a phosphatidic acid represented by formula (I): (wherein R1 represents straight-chain alkyl having an odd number of carbon atoms, straight-chain alkenyl having an odd number of carbon atoms, or straight-chain alkynyl having an odd number of carbon atoms).

Abstract: The invention provides a compound of formula (I): 1

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: The invention concerns compounds derived from (&agr;-aminophosphino) peptides, of general formula (I), in which R1 and R2 each represents a hydrogen atom or taken together form an imine with the adjacent nitrogen atom; R3 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl group, a cycloalkylmethyl group or finally, a methyl group substituted by a heterocyclic, aromatic or saturated group; R4 represents a phenyl group, a benzyl group, these groups capable of being substituted or not, a hydrogen atom, an alkyl group, analkenyl group or a cycloalkyl group; R5 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl, cycloalkylmethyl group or finally a methyl group substituted by a heterocyclic, aromatic or saturated group; R6, R7 and R8 can in particular represent a hydrogen atom, an alkyl group, a phe

Abstract: The present invention relates to pharmaceutical compositions and methods of using NAALADase inhibitors for treating glutamate-mediated diseases, disorders and conditions selected from the group consisting of anxiety, anxiety disorders and memory impairment.

Abstract: An oxidizing species is described herein as a reaction product through an in situ preparation combining a protonizable phosphorus or sulfur compound, and a halide source at controlled proportions in an aqueous, non-aqueous, gel, aerosol, solid-phase or powdered media. The oxidizing species can be used to reduce microbial and viral populations on a surface or object or in a body or stream of water. The invention thus finds applications as a bleach, sanitizer, oxidant, or in any other application in which an oxidizing agent can be beneficially used alone or in a formulation.

Abstract: The present invention provides therapeutic compositions containing lysophosphotidic acids, methods for making the compositions, and methods of using the compositions in the preservation and treatment of organs.

Abstract: The present invention relates to phosphoric acid derivatives represented by general formula (I), wherein each symbol is as defined in the description and nontoxic salts thereof. Because of having a TNF&agr; production inhibitory effect, the compounds represented by general formula (I) are useful as preventives and/or remedies for rheumatoid arthritis, ulcerative colitis, Crohn's disease, hepatitis, sepsis, hemorrhagic shock, multiple sclerosis, cerebral infarction, diabetes, interstitial pneumonia, uveitis, pain, glomerulonephritis, HIV-associated diseases, cachexia, myocardial infarction, chronic heart failure, oral aphtha, Hansen's disease, infection, etc.

Abstract: The invention provides a compound of formula (I): 1

Abstract: A method for therapeutic or prophylactic control of Acquired Immunodeficiency Syndrome (AIDS) in which an effective dose of phosphonoformic acid or a therapeutically-acceptable salt thereof is administered to a patent.

Abstract: The present invention relates to a male contaceptive composition suitable for oral administration, wherein the composition comprises a pharmaceutically acceptable, non-toxic cationic salt of an alkyl sulfate.

Abstract: The present invention relates to a method of inhibiting the activity of the HIV virus in a human comprising administering to the human an effective dose of phosphonoformic acid or a therapeutically effective salt thereof.

Abstract: The present invention relates to methods of using NAALADase inhibitors to regulate TGF-&bgr; and to treat neurodegenerative disorders, extracellular matrix formation disorders, cell-growth related diseases, infectious diseases, immune related diseases, epithelial tissue scarring, collagen vascular diseases, fibroproliferative disorders, connective tissue disorders, inflammatory diseases, respiratory distress syndrome and infertility.

Abstract: Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable salt or ester thereof. In preferred embodiments, an interaction between an amyloidogenic protein and a basement membrane constituent is modulated.

Abstract: Pesticidal formulations of cadusafos are provided. An aqueous capsule suspension is provided, containing from about 150 to about 360 grams of cadusafos per liter of formulation and having lower mammalian toxicity than aqueous cadusafos microemulsion formulations is prepared by interfacial polymerization of a first polyfunctional compound, such as a polymethylene polyphenyl isocyanate, with a second polyfunctional compound, such as a polyfunctional amine or mixtures of polyfunctional amines, in an aqueous phase optionally containing from about 0.05 to about 0.50 xanthan gum viscosity modifier/stabilizer. A granular form of the microencapsulated cadusafos is also provided. Several such formulations and the method of their preparation are described.

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 phosphatidic 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: Compounds of formula (I) 1

Abstract: A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.

Abstract: The present invention relates to pharmaceutical compositions and methods of using NAALADase inhibitors for treating glutamate-mediated diseases, disorders and conditions selected from the group consisting of anxiety, anxiety disorders and memory impairment.

Abstract: The present invention is, generally, directed to the use of betulinic acid and derivatives thereof for the treatment of neuroectodermal tumors. The present invention is based on the discovery that betulinic acid and its derivatives are potent anti-neuroectodermal agents. As disclosed herein, betulinic acid and its derivatives are useful for the treatment of neuroectodermal tumors, including, due to its distinct mechanism of action, neuroectodermal tumors that are resistant to conventional chemotherapeutical agents. In addition to the new use of known compounds, the invention discloses novel compounds and pharmaceutical compositions for the treatment of neuroectodermal tumors.

Abstract: A lipid preparation comprising at least about 10% phosphatidic acid (PA) is used to treat human conditions or disease. Examples of such conditions or disease are withdrawal syndromes or cancer.

Abstract: Phospholipid-HETE derivatives, compositions and methods of use are disclosed. The compounds are particularly useful for treating dry eye.

Abstract: Chemically stable, insecticidally active pellets having a low moisture content and at least about 95% active ingredient are described, as well as a method for manufacturing them. The active ingredient is selected from a class of N-hydrocarboyl phosphoroamidothioate and phosphoroamidodithioate compounds as described in the specification. The pellets generally have a moisture content of about 0.5% by weight or less, preferably less than about 0.3% by weight. The pellets can be produced by one of two types of processes as described in detail, including a high pressure axial extrusion process and a low pressure basket extrusion process.