Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and diethyl(2-cyanoethyl)phosphonate, or a pharmaceutically acceptable salt thereof. The present invention is directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering diethyl(2-cyanoethyl)phosphonate, or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.

Abstract: The invention relates to derivatives of (1-cyanocyclopropyl)phenylphosphinic acid of the formula (I) and to salts thereof, of the formula (II), for enhancing stress tolerance in plants to abiotic stress, preferably to drought stress, especially for enhancing plant growth and/or for increasing plant yield.

Abstract: The present invention relates to boosting the action of crop protection compositions comprising in particular spiroheterocyclically substituted tetramic acid derivatives of the formula (I) by addition of ammonium or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted vegetation.

Abstract: The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.

Abstract: Aromatic and alkyl thiocarbonates with and without a neighboring group that participates in the hydrolysis of a thiocarbonate are described. The aromatic or alkyl thiocarbonates can be used for the protection of sulfur during oligonucleotide synthesis. Their facile processes of manufacture and methods of using the same are provided.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: The present invention provides a concentrate for dilution with water in the preparation of an agricultural composition for application to crops, soil or animals. The concentrate is recommended for use with agricultural chemicals whose agricultural activity varies with the pH of the water. It comprises an active ingredient and a combination of pH indicators for coloring the water, the pH indicators being selected so as to indicate different colors of spray water at different pH levels. The proportions of active ingredient and pH indicators are selected so that when the concentrate is added to water, the pH indicators indicate visually upper and lower pH limits for optimum activity of the agricultural chemical.

Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: An external preparation for skin has a pH value of 2.0-5.0 and comprises: (a) 1.0-7.0 mass % of at least one of the members selected from ?-hydroxy acids, (b) 0.1-3.0 mass % of a crosslinked type N,N-dimethylacrylamide-2-acrylamido-2-methylpropanesulfonic acid sodium salt copolymer, and (c) 0.1-3.0 mass % of an associating thickener constituted of a compound of the formula (1): R1—{(O—R2)k—OCONH—R3[—NHCOO—(R4—O)n—R5]h}m (1) wherein R1 represents a hydrocarbon group, R2 and R4 represent alkylene groups having 2-4 carbon atoms, which may be identical or different, or a phenylethylene group, R3 represents a hydrocarbon group, which may have a urethane bond, R5 represents a branched chain or secondary hydrocarbon group, m is a number of at least 2, h is a number of at least 1, k is a number within the range of 1-500, and n is a number within the range of 1-200.

Abstract: The present invention relates to methods and compositions for the protection of skin and mucous membranes from undesirable side effects of ionizing radiation in a patient undergoing ionizing radiation therapy. In particular, the application describes compositions and methods comprising the topical use of Nrf2 inducers.

Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.

Abstract: The invention relates to derivatives of (1-cyanocyclopropyl)phenylphosphinic acid of the formula (I) and to salts thereof, of the formula (II), for enhancing stress tolerance in plants to abiotic stress, preferably to drought stress, especially for enhancing plant growth and/or for increasing plant yield.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.

Abstract: The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.

Abstract: An amino or thiol linker building block for the synthesis of amino or thiol functionalized amino acids and generally of the following structure: is provided. Such building block may be introduced in the 5? end position of an amino acid under standard coupling conditions. Such building block allows in-line coupling control, “trityl-on” purification, and solid support functionalization/derivatization. Such building block is a stable, solid compound and can therefore be easily handled. With the building block of the present invention, deprotection may be carried out under standard detritylation conditions.

Abstract: The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.

Abstract: The present invention relates to compounds of the formula (I) or a tautomer or prodrug thereof, or a pharmaceutically acceptable salt of said compound, tautomer or prodrug, wherein: R1, R2, R3, R4 and R5 are each independently selected from H, halo, CN, CF3 and CONH2; compositions containing such compounds and the uses of such compounds as antiparasitic agents.

Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.

Abstract: A method of causing a patient to reduce or cease tobacco use that involves the administration of a cholinesterase inhibitor.

Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.

Abstract: According to the present invention, there is provided a fluorescent nucleotide represented by the formula: A-B-C, wherein A represents a residue of natural or synthetic nucleotide, oligonucleotide, polynucleotide, or derivative thereof, and binds to B at a base moiety in said residue; B represents a divalent linking group or a single bond; and C represents a monovalent group derived from a fluorescent dye having 0 or 1 sulfonic acid group or phosphoric acid group in a molecule. The present invention provides useful fluorescent nucleotides for labeling nucleic acids, specifically, fluorescent nucleotides of which uptake ratio is high in synthetic reaction of nucleic acids.

Abstract: An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H2O2 and as-used concentrations contain about 0.5% wt./wt. % H2O2. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier and/or hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt, an alkyl aryl polyoxyethylene surfactant, and/or a polyoxyethylene surfactant.

Abstract: Compounds, compositions, and methods for labeling membranes are disclosed. Compounds of formula G-L-E are described wherein G is a lipophilic group, L is a cleavable linkage and E is an electrophoretic group. The compounds become associated with membranes, and can be cleaved with a cleavage-inducing moiety thereby releasing the detectable electrophoretic group.

Abstract: An adhesive composition is provided which is suitable for the bonding of polymeric materials, in whole or in part, such as composite resins, or methacrylate-containing glass-ionomer filling materials, to tooth enamel, or tooth dentin, or to other hand tissues of the human body, such as bone. The composition comprises an unsaturated carboxylic acid ester, an unsaturated phosphate ester and other crosslinking agents. The especially preferred phosphates (which are provided as new compounds) are those of formula (I) in which: R1 is a hydrogen atom, alkyl C1-C4, or CN; R is an aliphatic, cycloaliphatic or aryl radical containing from 1 to 10 carbon atoms and having a valence of n+1; n is an integer from 1 to 5, preferably from 3 to 5.

Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.

Abstract: An adhesive composition is provided which is suitable for the bonding of polymeric materials, in whole or in part, such as composite resins, or methacrylate-containing glass-ionomer filling materials, to tooth enamel, or tooth dentin, or to other hand tissues of the human body, such as bone. The composition comprises an unsaturated carboxylic acid ester, an unsaturated phosphate ester and other crosslinking agents. The especially preferred phosphates (which are provided as new compounds) are those of formula (I) in which: R1 is a hydrogen atom, alkyl C1-C4, or CN; R is an aliphatic, cycloaliphatic or aryl radical containing from 1 to 10 carbon atoms and having a valence of n+1; n is an integer from 1 to 5, preferably from 3 to 5.

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

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: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.

Abstract: A fluorescent cyanine dye of the following general formula is disclosed: wherein: X1 and X2 are independently selected from the group consisting of —O—, —S—, —C(CH3)2 or —C═CH2; Y1 and Y2 are nonmetal atoms required to form a benzo-condensed or naphtho-condensed ring; Q is a conjugated moiety that increases the fluorescent quantum yield and the stability of the compound; R1 and R2 are independently selected from the group consisting of H, C1-C4, alkyl, alkylensulfonic group or alkylensulfonate group wherein the alkylene group has from 1 to 4 carbon atoms; R3, R4 and R5 are independently selected from the group consisting of H, a sulfonic group, a sulfonate group, alkylensulfonic, alkylensulfonate and —SO2NH(CH2)m—W—(CH2)nZ, wherein alkylene has 1 to 4 carbon atoms, with the proviso that at least one of R1 to R5 contains a sulfonic or sulfonate group; W is absent or is a group selected from —SO2NH, —O—, —COO

Abstract: Compositions and methods for killing dust mites and cleaning carpets and other textile fabrics are disclosed. A miticide composition concentrate for mixing with water and optionally with a carpet or fabric cleaning solution consists essentially of a solution of benzyl benzoate and a water soluble organic solvent for the benzyl benzoate such as benzyl alcohol, a surfactant and water. The amounts of the solvent, surfactant and water are selected to maintain a stable dispersion of benzyl benzoate and benzyl alcohol in the aqueous mixture. Also disclosed are aqueous carpet cleaning miticide composition comprising benzyl benzoate, at least one organic solvent which has an affinity for benzyl benzoate and water, at least one surfactant, an anti-resoiling agent, optionally, a fragrance, optionally, a chellating agent and water.

Abstract: 4,4-Diarylbutadienes of the formula I, 1

Abstract: An iron-dextran compound for parenteral treatment of iron-deficiency anemia comprises hydrogenated dextran having a weight average molecular weight (Mw) between 700 and 1,400 Daltons, preferably approximately 1,000 Daltons, a number average molecular weight (Mn) of 400 to 1,400 Daltons and wherein 90% by weight of the dextran has molecular weights less than 2,700 Daltons and the Mw of the 10% by weight fraction of the dextran having the highest molecular weights is below 3,200 Daltons, said hydrogenated dextran having been subjected to purification by membrane processes having a cut-off value between 340 and 800 Daltons, in stable association with ferric oxyhydroxide.

Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: A Human amine transporter polypeptide and DNA (RNA) encoding such polypeptide and a procedure for producing such polypeptide by recombinant techniques is disclosed. Also provided are methods for detecting agonists and antagonists to such polypeptide and the use of agonists and antagonists for treating diseases related to the underexpression and over-expression of the Human amine transporter of the present invention. Also disclosed are methods for detecting mutations in the nucleic acid sequence encoding the polypeptide and for detecting altered levels of the soluble form of the polypeptide.

Abstract: The invention relates to a method of treating the navicular disease in horses, which comprises treating the navicular disease in horses with an effective amount of at least one compound of formula (I), ##STR1## wherein R.sub.1 is hydrogen, hydroxy, amino or halogen, and R.sub.2 is hydrogen, halogen or a radical which is bound through C, N, S or O, or of a C.sub.1 -C.sub.4 tetraalkyl ester thereof, each in the free form or in the form of the salt and/or in the hydrate form; to a compound of formula (I) for use in a method of treating the navicular disease, to a composition for use in a method of treating the navicular disease, which comprises one or more than one compound of formula (I), as well as to the use of a compound of formula (I) for the preparation of a veterinary composition for treating the navicular disease.

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: A pesticidal composition to noxious organisms which comprises a diarylalkane and an active component effective for killing or repelling noxious organisms and the diarylalkane is at least one member selected from the group consisting of butyl diphenylmethane, butyl-1,1-diphenylethane and butyl-1,2-diphenylethane. The used diarylalkane has a high dissolving power to the effective component, a high boiling point and a high flash point with low unpleasant smell and does not deteriorate the effective component in the pesticidal composition.

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: 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: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.

Abstract: An insecticidal, acaricidal or nematocidal composition which comprises an organophosphorus compound represented by formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represents C.sub.1 to C.sub.4 alkyl; A represents H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkylthio or N(R.sup.4)R.sup.5 ; Z represents C(CN)R.sup.4 or N-R.sup.7 and an inert carrier show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating odor and exhibit very low toxicity to warm-blooded animals. R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are defined in the specification.