Abstract: The invention concerns the use of certain compounds related to fatty acids to control nematodes that infest plants or the situs of plants. Nematodes that parasitize animals can also be controlled using the methods and composition of this invention. Certain of the useful compounds are fatty acid esters that are predicted inhibitors of nematode delta-12 fatty acid desaturases and can be, for example, from C16 to C20 in length.

Abstract: The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor

Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.

Abstract: The selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A response to serotonin (5-HT) is achieved using analogs of oleamide. Selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A leads to a modulation of serotonergic signal transduction of cells having various receptor subtypes. A subset of analogs is identified that inhibits rather than potentiates the 5-HT2A, but not the 5-HT1A, receptor response. These analogs enable the selective modulation of serotonin receptor subtypes and even have opposing effects on the different subtypes. An analysis of the activity of the oleamide analogs discloses that the structural features required for activity are highly selective. In particular, the presence, position, and stereochemistry of the 9-cis double bond is required and even subtle structural variations reduce or eliminate activity.

Abstract: A method of inhibiting the release of a proinflammatory cytokine in a cell is disclosed. The method comprises treating the cell with a cholinergic agonist. The method is useful in patients at risk for, or suffering from, a condition mediated by an inflammatory cytokine cascade, for example endotoxic shock. The cholinergic agonist treatment can be effected by stimulation of an efferent vagus nerve fiber, or the entire vagus nerve.

Abstract: The present invention ralates to compounds of formula (I): wherein R is hydrogen (H) or C1-6 alkyl; and X is defined such that —NH—(X)—COOH is the residue of an amino acid, which amino acid may itself optionally be substituted at any pendant amino group thereof by a residue of a carboxylic acid or a derivative thereof; or a salt thereof. The use of these compounds, in particular as potential anti-inflammatory and immunomodulatory drugs, and their preparation are described.

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: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteasome inhibitors.

Abstract: Use of nordihydroguaiaretic derivatives to suppress CDC-2 and survivin, stimulate apoptosis, and treat tumors.

Abstract: Compounds of general formula (I), wherein: n represents an integer from 1 to 10; R1 and R6, independently of each other, represent a hydrogen atom, a group useful for protecting nitrogen atoms in peptide synthesis or a group of formula COR or —CH2COR, wherein R represents a hydrogen atom, an alkyl group of 1 to 10 carbon atoms, a —COORa group wherein Ra represents H or an alkyl group, a primary —NH2 amino group or a secondary or tertiary amine, an alkoxy group, a phenyl group or a pyridinium group; R2, R3, R4 and R5, independently of one another, represent a hydrogen atom, an alkyl group of 1 to 10 carbon atoms; Y represents CH2 and Z represents CO, or Y represents CO and Z represents CH2, for preparing a medicine for treating tumoral pathologies or neurodegenerative diseases such as Alzheimer's or Lehn's disease.

Abstract: The present invention relates to a composition, which contains L-carnitine or alkanoyl-L-carnitine, and a glucosaminoglycan or a constituent thereof, suitable for the prevention of articular disorders and for the therapeutic treatment of articular diseases.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The invention relates to a novel composition with antimicrobial activity. It is in the food industry a well-known method to use the product L-arginine, Na-lauroyl-ethylester monohydrochloride (LAE). This product is well tolerated and suitable for use in the preservation of all perishable food products. The action of LAE can be further improved by combining the product with a second component selected from the group consisting of potassium sorbate, sodium sorbate and sorbic acid. The weight ratio of LAE to the second component is preferably in the range of 1:50 to 50:1. The combination of the two products leads to a synergistic combined activity against such microorganisms as Bacillus subtilis, Staphylococcus aureus, Bacillus megaterium, Citrobacter intermedium, Enterobacter aerogenes, Escherichia coli, Candida albicans, Penicillium camemberti and Cladosporium cladosporioides.

Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1

Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.

Abstract: Novel synergistic fungicidal compositions used for protecting seeds, plants and other vegetative material against fungi contain a mixture of one or more compounds selected from group A and one or more compounds selected from group B. Compounds from group A are selected from &bgr;-Amino butyric acid and its N-benzoyl-octyl ester derivatives. Compounds from group B are selected from the group of fosetyl aluminum, dimethomorph, a mixture of folpet and ofurace (45:5), folpet, fencaramid (Bayer SZX), mancozeb, cymoxanil, methalaxyl, the single optical isomer of metalaxyl, a mixture of cymoxanil and mancozeb (4:1), copper sulfate, copper hydroxide, copper sulfate hydrate, azoxystrobin, and acibenzolar-s-methyl.

Abstract: the present invention provides novel compounds represented by formula I: 1

Abstract: The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: The present invention describes a method for providing creatine to an animal which includes receiving a creatine ester by the animal. The creatine ester is suitable for being modified by the animal to form creatine.

Abstract: The present invention provides a creatine ester anti-inflammatory compound which may be received by animals and then metabolized into a biologically active form of creatine. The biologically active creatine inhibits the production of chemical mediators, released during an inflammatory response, which are important components in the inflammatory response and the inflammation and pain resulting from physical or chemical trauma to cells and tissue.

Abstract: The present invention relates to insect repellant compositions containing, based upon the total weight of the composition, from about 6 to about 30 percent by weight of insect repellant active material having functionality selected from ester, amide, urethane or combinations thereof; from about 5 to about 30 percent by weight of alcohol, and from about 1 to about 10 percent by weight of nonionic surfactant. The compositions of the invention exhibit reduced rates of degradation of the active material in solution and are less drying and irritating to sensitive skin.

Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: There is provided a topical composition that comprises (a) a substantially anhydrous insect repellent selected from the group consisting of ethyl 3-(N-butylacetylamino) propionate or a derivative thereof, p-menthane-3,8-diol, hydroxyethyl isobutyl piperidine carboxylate (1-piperidine carboxylic acid), and mixtures thereof, and (b) a non-volatile solvent. A second embodiment of the present composition includes the same insect repellent, and a volatile solvent, and, optionally, a film former. A third embodiment includes the same insect repellent, a non-volatile solvent, a volatile solvent, and, optionally, a film former.

Abstract: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: Use of nordihydroguaiaretic derivatives to suppress CDC-2 and survivin, stimulate apoptosis, and treat tumors.

Abstract: The invention concerns the use of certain compounds related to fatty acids to control nematodes that infest plants or the situs of plants. Nematodes parasitizing animals can also be controlled using the methods and composition of this invention. The useful compounds are inhibitors of nematode delta-12 fatty acid desaturases and can be, for example, from C16 to C20 in length. A feature of these compounds is that their inhibitory effect on the activity of a nematode delta-12 desaturase, or on the viability or fecundity of a nematode, is smaller in the presence of the product of a delta-12 fatty acid desaturase (e.g., linoleate) than in the presence of the substrate of the enzyme (e.g., oleate).

Abstract: A method of inhibiting the release of a proinflammatory cytokine in a cell is disclosed. The method comprises treating the cell with a cholinergic agonist. The method is useful in patients at risk for, or suffering from, a condition mediated by an inflammatory cytokine cascade, for example endotoxic shock. The cholinergic agonist treatment can be effected by stimulation of an efferent vagus nerve fiber, or the entire vagus nerve.

Abstract: Use of nordihydroguaiaretic derivatives to suppress CDC-2 and survivin, stimulate apoptosis, and treat tumors.

Abstract: We have discovered that the topical application of the amino acid lysine and the 6-methyl derivative of lysine to Herpes simplex virus Type II is therapeutically beneficial and relieves the discomfort and symptoms of HSV infections and prevents or reduces the number of severity of HSV infections. We have also discovered that derivatives of lysine, in addition to 6-methyl lysine and derivatives of arginine have an inhibitory effect upon HSV replication. These compounds are useful in the prevention and treatment of HSV lesions.

Abstract: A process for the production of dihomo-&ggr;-linolenic acid comprising the steps of culturing a microorganism having an ability to produce araquidonic acid and having a reduced or lost &Dgr;5 desaturase activity to produce dihomo-&ggr;-linolenic acid or a lipid containing dihomo-&ggr;-linolenic acid, and recovering the dihomo-&ggr;-linolenic acid.

Abstract: A composition is disclosed which is suitable for the prevention and/or treatment of cell and tissue abnormalities of exogenous, toxic or metabolic origin and suitable for reducing the toxic effects of cyclosporin-A and other immunosuppressive agents, which may take the form of a food supplement or of an actual medicine, containing as its active ingredients in combination or separately packaged: (a) propionyl L-carnitine or one of its pharmacologically acceptable salts, and (b) an amino acid selected from the group consisting of glycine, serine, alanine and arginine, or mixtures thereof.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Abstract: Therapeutic methods for the prevention and treatment of neurodegenerative conditions are described, the methods including administering to a subject in need thereof a neuroprotective effective amount of a selective inhibitor of inducible nitric oxide synthase.

Abstract: A novel solid, crystalline and non-hygroscopic substance consisting of acetyl L-carnitine acid fumarate and a process for preparing same are disclosed.

Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells in bone marrow which are capable of undergoing normal hematopoiesis and differentiation, wherein the bone marrow is contacted with an inhibitor of NO, such as an inhibitor of nitric oxide synthase (NOS), thereby producing bone marrow having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis and differentiation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor of NO, such as an inhibitor of NOS. The invention also pertains to a method of regenerating tissue in an adult mammal comprising contacting a selected tissue (e.g.

Abstract: The present invention relates to novel carbamates, ureas, and pharmaceutically acceptable salts thereof, compositions comprising the carbamate, urea, or a pharmaceutically acceptable salt thereof, and methods for treating or preventing cancer, inflammation, or a viral infection comprising administering to a patient in need of such treatment or prevention a therapeutically effective amount of the carbamate, urea, or pharmaceutically acceptable salt thereof.

Abstract: Novel synergistic fungicidal compositions used for protecting seeds, plants and other vegetative material against fungi contain a mixture of one or more compounds selected from group A and one or more compounds selected from group B. Compounds from group A are selected from &bgr;-Amino butyric acid and its N-benzoyl-octyl ester derivatives. Compounds from group B are selected from the group of fosetyl aluminum, dimethomorph, a mixture of folpet and ofurace (45:5), folpet, fencaramid (Bayer SZX), mancozeb, cymoxanil, methalaxyl, the single optical isomer of metalaxyl, a mixture of cymoxanil and mancozeb (4:1), copper sulfate, copper hydroxide, copper sulfate hydrate, azoxystrobin, and acibenzolar-s-methyl.

Abstract: Novel synergistic fungicidal compositions used for protecting seeds, plants and other vegetative material against fungi contain a mixture of one or more compounds selected from group A and one or more compounds selected from group B. Compounds from group A are selected from &bgr;-Amino butyric acid and its N-benzoyl-octyl ester derivatives. Compounds from group B are selected from the group of fosetyl aluminum, dimethomorph, a mixture of folpet and ofurace (45:5), folpet, fencaramid (Bayer SZX), mancozeb, cymoxanil, methalaxyl, the single optical isomer of metalaxyl, a mixture of cymoxamil and mancozeb (4:1), copper sulfate, copper hydroxide, copper sulfate hydrate, azoxystrobin, and acibenzolar-s-methyl.

Abstract: A health food/dietary supplement is disclosed, endowed with a protective action on liver function against exogenous and endogenous hepatoxic agents, the characterizing components of which are isovaleryl L-carnitine and/or propionyl L-carnitine and an extract of Silybum marianum (milk thistle) standardized to a least 70 percent by weight of silymarin.

Abstract: This invention provides methods and chemical agents for enhancing transient expression in eukaryotic cells.

Abstract: The present invention relates to cleaning compositions which comprise the insect repellent ethyl 3-(N-butylacetamino)propionate and the use of this insect repellent in all types of cleaning compositions for repelling insects. This invention furthermore relates to a method for cleaning and for simultaneously repelling insects in which cleaning compositions comprising ethyl 3-(N-butylacetamino)propionate are used.

Abstract: A composition of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of the compound, and a diagnostically acceptable carrier. A method for detecting malignant tumors, by administering a tumor detecting effective amount to a host in need of tumor detection of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of said compound and detecting the malignant tumors using NMR.

Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula I wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.

Abstract: Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Abstract: Therapeutic methods of treatment, compositions and foodstuffs are described which contain isoflavone compounds described by general formula (1), in which Z is H, R1 is H, or RACO where RA is C1-10alkyl or an amino acid, R2 is H, OH, or ORB where RB is an amino acid, or CORA where RA is as previously defined, W is H, A is H or OH, and B is selected from (a), (b), (c), or W is H, and A and B taken together form a six-membered ring selected from (d), or W, A and B taken with the groups with which they are associated comprise (e), or W and A taken together with the groups with which they are associated comprise (f) and B is (g) wherein R3 is H, CORA where RA is as previously defined, CO2Rc where RC is C1-10alkyl, or CORB where RB is as previously defined, R4 is H, CORD where RD is H, OH, C1-10alkyl or an amino acid, CO2RC where RC is as previously defined, CORE where RE is H, C1-10alkyl or an amino acid, COOH, CORC where RC is as previously defined, or CONHRE where RE is as previously defined, R5 is H, CORC where