Abstract: Aspects of the present invention include methods of synthesizing phosphocholine analogues and the phosphocholine conjugates formed therefrom and their use in preventing infections caused by microorganisms.

Abstract: Intermediates and methods for forming passivated surfaces on oxide layers and articles produced thereby are described. Hydroxyl or hydroxide groups on the oxide surfaces are reacted with a metal reagent of the formula Y(L-Pol)m, where Y is a transition metal, magnesium or aluminum, L is oxygen, sulfur, selenium or an amine, and “Pol” represents a passivating agent such as a polyethylene glycol, a hydrocarbon, or a fluorocarbon. The resulting modified surface can be further reacted with a passivating agent having a phosphate functional group or a polyvalent reagent comprising a passivating moiety and a plurality of functional groups that are reactive with or that form complexes with Y. The passivating agent can also include a functional group such as biotin to provide surfaces with a desired functionality. The passivated surfaces exhibit minimal binding to bio-molecules and can be used in single-molecule detection schemes.

Abstract: This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally.

Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Abstract: A dispersant comprising a polyester chain obtainable by polymerising a hydroxy carboxylic acid or lactone thereof such as ?-caprolactone with a cyclic alkylene carbonate such as 5,5-dimethyltrimethylene carbonate. The dispersant may be in the form of a phosphate ester where the polyester chain is reacted with a phosphating agent such as polyphosphoric acid or the polyester chain may be attached to a polyamine or polyimine such as polyethyleneimine.

Abstract: Disclosed is an organic thin film transistor including a phosphate-based self-assembled monolayer and a method of manufacturing the same. Example embodiments relate to an organic thin film transistor, which may include a single bond type phosphate-based self-assembled monolayer without intermolecular cross-linking, between source/drain electrodes and an organic semiconductor layer, thus exhibiting improved electrical properties, e.g., increased charge mobility, and to a method of manufacturing the organic thin film transistor.

Abstract: The invention provides a compound of formula I: wherein R1, Ra, Rb, Rc, and Rd have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds or salts. The compounds are useful for treating cancer in animals.

Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: An insecticide of formula 1 and the agriculturally acceptable salts thereof, wherein: R1 is selected from the group consisting of: the group OR5 wherein R5 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclic and substituted heterocyclic; the group —NR6OH wherein R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, carbocyclic and substituted carbocyclic; the group NR7R8 wherein R7 and R8 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl and carbocyclic; and the group wherein R1 is linked to R2 to form a diradical bridging group; R2 and R3 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, carbocyclic, substituted carbocyclic, aryl, substituted aryl, acyl and substituted acyl; and A is a diradical linking group which has a molecular weight of preferably

Abstract: A derivative of phosphoric acid ester salt or adduct or a mixture thereof is obtained from a reaction product, polycondensed with at least one aldehyde, of at least one polyol phosphoric acid ester with at least one organic nitrogen base. The derivative is advantageously used as a flame-inhibiting and/or intumescent treatment in plastic mouldings, on porous carriers or in paint or coating systems. The production of the derivative or a mixture thereof by reacting at least one polyol with phosphorus pentoxide and reacting the polyol phosphoric acid ester obtained in that way with at least one organic nitrogen base forming a phosphoric acid ester salt or adduct, is characterized in that the amount of phosphorus pentoxide required for the esterification operation is suspended in an amount of the ester or ester mixture to be produced, then at a temperature in the range of 20–180° C.

Abstract: Disclosed are compounds having non-steroidal anti-inflammatory drugs (NSAIDS) covalently linked to a phospholipid moiety via a bridging group. Also disclosed are a process for the synthesis of the compounds, pharmaceutical compositions comprising the compounds and the use thereof for the treatment of diseases and disorders related to inflammatory conditions, such as the treatment of ischemia.

Abstract: Neopentyl glycol bis(diphenyl phosphate) liquid compositions are described that comprise from about 75% to about 90%, by weight, of neopentyl glycol bis(diphenyl phosphate), less than about 5% by weight of cyclic product, less than about 8% by weight of triphenyl phosphate, and with a P3 content of no less than about 1%, by weight. These compositions are made by continuously adding neopentyl glycol to a diaryl chlorophosphate mixture at elevated temperature, under vacuum, and in the presence of a catalyst.

Abstract: A composition and a process for producing the composition are disclosed. The composition comprises an alkoxylated phosphite ester which has the formula of (HO[{CH(R)}mO]n)3P in which each R can be the same or different and can be independently hydrogen or an alkyl group, or combinations of two or more thereof and m is a number from 2 to about 20 and n is a number from 2 to about 20. The process comprises contacting a trialkyl phosphite with an alkylene glycol or polyalkylene glycol to produce a mixture followed by heating the mixture. Also disclosed in a process for using the composition, which comprises contacting a carbonyl compound, in the presence of the composition, with an alcohol.

Abstract: This invention relates to attachment chemistries for binding macromolecules to a substrate surface or to other conjugation targets. More particularly, this invention relates to attachment chemistries involving branched or linear structures having one or more hydrazide attachment moieties for binding the macromolecules to a substrate surface, or for other conjugation reactions. Novel modifying reagents are provided for the introduction of protected hydrazide attachment moieties or precursor forms of such hydrazides to the macromolecule, either as a single hydrazide or as multiple hydrazides.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: Hydrazino, oxyamino and carbonyl-based reagents and methods for incorporation into oligonucleotides during their solid phase synthesis are provided. Modified oligonucleotides are provided that incorporate the reagents provided here in. Immobilized oligonucleotides and oligonucleotide conjugates that contain covalent hydrazone or oxime linkages are provided. Methods for preparation of surface bound oligonucleotides are provided. Methods for the preparation of oligonucleotide conjugates are also provided.

Abstract: A pharmaceutically acceptable salt of 2-methyl-3-butenyl-l-pyrophosphoric acid; an agent for treating lymphocytes which comprises at least one of 2-methyl-3-butenyl-l-pyrophosphoric acid, a pharmaceutically acceptable salt thereof, and a hydrate thereof; V?2V?2 type T cells treated by the same; and a medicine containing the same specifically stimulate and proliferate the human V?2V?2 type T cells, and also induce and enhance an antitumor activity thereof.

Abstract: The present invention relates to catalysts comprising chiral monophosphorus compounds and their use, the chiral monophosphorus compounds themselves and also their precursors.

Abstract: The present invention relates to a new chemical compound known as hexa-citrated phytate and a method of production thereof. The new chemical compound has six citrate molecules attached at the hydroxyl group of a citric acid to phosphates of a phytate molecule. This new chemical compound is a very effective oral chelator maintaining metals and metalloids in the saline solution of blood. The new chemical compound is also very effective in dissolving artery plaque, as well as copper, zinc and iron.

Abstract: The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.

Abstract: A facile synthesis of symmetric esters of C1-C10 alkylenebisphopsphonic acids is disclosed in which a C1-C10 alkylenebis(phosphonic dichloride) is reacted with an alcohol in the presence of a catalytic amount of 1H-tetrazole and a base in an aprotic solvent to form a first reaction mixture. The first reaction mixture is maintained for a time period sufficient to form a C1-C10 alkylenebis(chloro ester phosphonate) that is reacted under basic conditions with an excess of a hydroxylated compound to form a second reaction mixture that is itself maintained for a time period sufficient to form a C1-C10 alkylenebis(ester phosphonate) partial ester, homoleptic tetraester or mixed tetraester. The material so formed can be recovered or used as is.

Abstract: An organic electroluminescent device includes an anode, a cathode, and an organic layer having a light-emitting area and arranged between the anode and the cathode.

Abstract: The phosphorus-containing compound of the present invention is represented by the following formula (I), (II) or (III): wherein Z1, Z2 and Z3 each represents a cycloalkane, a cycloalkene, a polycyclic aliphatic hydrocarbon or an aromatic hydrocarbon rings which may have a substituent; R represents a halogen atom, a hydroxyl, a carboxyl, a halocarboxyl(haloformyl), an alkyl, an alkoxy, an alkenyl or an aryl groups; A represents a polyvalent group corresponding to an alkane; Y1, Y2 and Y3 each represents —O—, —S— or —NR1—, wherein R1 represents a hydrogen atom or an alkyl group; k is an integer of 1 to 6; m is an integer of 0 to 2; n is an integer of not less than 1; q is an integer of 0 to 5; r is 0 or 1; and S is an integer of 1 to 4. The phosphorus-containing compound is excellent in heat resistance and is useful as flame retardants, plasticizers, or stabilizers.

Abstract: A novel antioxidant has the advantages of both the hindered phenols and the phosphite antioxidant is prepared from phosphorus trichloride and 2,5-di-tert-butylhydroquinone, such as tetrakis-(2,5-di-tert-butyl-4-hydroxyphenyl)-2,5-di-tert-butyl-hydroquinonediyl diphosphite.

Abstract: The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.

Abstract: This invention is directed to alkyl cobalt (II) dioximates and methods for making these dioximates.

Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such resins may be used in dental restorative materials to help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.

Abstract: A novel antioxidant has the advantages of both the hindered phenols and the phosphite antioxidant is prepared from phosphorus trichloride and 2,5-di-tert-butylhydroquinone, such as tetrakis-(2,5-di-tert-butyl-4-hydroxyphenyl)-2,5-di-tert-butyl-hydroquinonediyl diphosphite.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.

Abstract: The invention relates to polyurethane materials, cross-linked by silane polycondensation, containing alkoxylsilane functional polyurethanes, alkaline fillers, phosphorous compounds aminosilanes, organometallic compounds and optionally additional auxiliary agents, to a method for their production and to the use thereof.

Abstract: The invention relates to a process of preparing glycol carboxyethylmethylphosphinate, which comprises

Abstract: Novel compounds are provided in the form of nucleoside pyrophosphate and triphosphate analogs. In these analogs, the pyrophosphate or triphosphate group is replaced with a moiety that is isosterically and electronically identical thereto, but is hydrolytically and enzymatically more stable. The compounds are useful as therapeutic agents, e.g., as antiviral agents, anticancer agents, metabolic moderators and the like. The invention also provides pharmaceutical compositions containing a compound of the invention as an active agent, and in addition provides methods of treating disease, including viral infections, cancer, bacterial infections, inflammatory and/or autoimmune diseases, and the like, by administering a compound of the invention to a patient in need of such treatment.

Abstract: Novel P(III) bisamidite reagents as phosphorus protecting groups, nucleoside phosphoramidite intermediates, and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared through the protection of one or more internucleosidic phosphorus functionalities, preferably followed by oxidation and cleavage of the protecting groups to provide oligonucleotides.

Abstract: A process for preparing amphiphilic compounds having at least two hydrophilic and at least two hydrophobic groups by reacting an olefinic substrate having at least two double bonds with an organic hydroperoxide to form an oxirane ring, opening, the oxirane ring with an alcohol in the presence of a catalyst system comprising a molybdenum compound as a first catalyst component and a second catalyst component selected from the group consisting of boron trifluoride, alumina, 1,8-diazzabicyclo-(5.4.0)-undec-7-ene, 1,4-diazabicyclo-(2,2,2)-octane.

Abstract: The invention concerns a halogenation in position meta of a phenol fuction. Said halogenation comprises a step which consists in halogenating an aromatic derivative of a medium or advantageously strong acid, the aromatic radical being a phenyl substituted in ortho and in para by functions attracting electrons by inductive effect. The invention is applicable to organic synthesis.

Abstract: A pharmaceutically acceptable salt of 2-methyl-3-butenyl-1-pyrophosphoric acid; an agent for treating lymphocytes which comprises at least one of 2-methyl-3-butenyl-1-pyrophosphoric acid, a pharmaceutically acceptable salt thereof, and a hydrate thereof; V&ggr;2V&dgr;2 type T cells treated by the same; and a medicine containing the same specifically stimulate and proliferate the human V&ggr;2V&dgr;2 type T cells, and also induce and enhance an antitumor activity thereof.

Abstract: Methods for the preparation of oligonucleotides having bioreversible phosphate blocking groups are disclosed. The oligonucleotides are prepared utilizing amidite type chemistry wherein the bioreversible phosphorus protecting group is formed as an integral part of the amidite reagent.

Abstract: Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.

Abstract: Novel thyroid receptor ligands are provided which have the general formula (I) where R1 is alkyl of 1 to 4 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 3 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; n is an integer from 0 to 4; R4 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, cyano, or a phosphonic acid or an ester thereof, or a pharmaceutically acceptible salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a T3 regulated gene, such as obesity, hypercholesterolemia, osteoporosis, hypothyroidism, and goiter, is also provided.

Abstract: An oligophosphate of general formula 1

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: Biphenyl and phosphorus trichloride are reacted in the presence of aluminum chloride, a hydrogen chloride gas generated is removed, a pyridine is added, excess phosphorus trichloride is removed, a resulting reaction product containing the obtained phosphine compound of the formula: and a phenol compound of the formula: wherein R is a hydrogen atom or methyl and R1 and R2 are each a hydrogen atom or alkyl having 1 to 5 carbon atoms, are reacted in the presence of a base as a deacidifying agent, and hydrochloride of this base and a pyridine-aluminum chloride complex are removed. By this method, a high quality phosphonite compound containing phosphinobiphenylene of the formula: can be produced safely in a high yield.

Abstract: Immunoregulatory compounds are disclosed of the formula: as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

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: Bisphenol-phosphorus compound complexes represented by the following general formula (1) are disclosed (R1 to R4 represent hydrogen atom or a group that can be a substituent on a benzene ring; L represents —S— group or a —CHR5— group where R5 represents hydrogen atom or an alkyl group; and R6 to R8 represent an alkyl group, an aryl group, a heterocyclic group etc.). The present invention provides reducing agents that can realize thermally processed image recording materials that can provide sufficient image density at a practical reaction temperature (specifically 100-140° C.) and within a practical reaction time (specifically 1-30 seconds), and can sufficiently suppress the coloration of white portions when the materials are stored in a dark place after the development.

Abstract: This invention relates to water soluble phosphines of the following structural formula and method of preparing these phosphines: Wherein A is a moiety which is stable to the reaction conditions and does not interfere with solubility of the compound in the preparation reaction. R1 and R2 are selected from hydroxyl groups, dialkylamino group, and alkoxide groups.

Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.

Abstract: Nucleotide compositions containing aminooxy moieties are provided. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligonucleotide is modified to include an aminooxy moiety.

Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.