Abstract: Disclosed are ceramide derivatives represented by the following formula 1 or 2, a method for preparing the same, and a therapeutic agent for treating atopic dermatitis including the ceramide derivatives as active ingredients: wherein, R1 and R2 are each independently straight or branched alkyl groups having 4 to 22 carbon atoms. The therapeutic agent for treating atopic dermatitis including the ceramide derivatives as active ingredients according to the present invention may be useful to treat atopic dermatitis, or treat other skin diseases that are required for improving skin inflammations or suppressing epidermal proliferation, by suppressing or improving inflammatory conditions in the atopic dermatitis in addition to giving immunoregulatory functions, and suppressing or improving skin disorders, for example epidermal proliferation that is generally observed in the atopic dermatitis.

Abstract: The invention relates to diorganylphosphinic salts of the formula (I) and/or diorganyldiphosphinic salts of the formula (II) and/or any of their polymers where R1 and R2 are identical or different and are C1-C6-alkyl, linear or branched, and/or aryl; R3 is C1-C10-alkylene, linear or branched, C6-C10-arylene, -alkylarylene, or -arylalkylene; M is Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Li, Na, K, and/or a protonated nitrogen base; m is from 1 to 4; n is from 1 to 4; x is from 1 to 4, wherein the total content of partially water-soluble, ionizable compounds and the water-soluble content of the partially water-soluble, ionizable compounds is from 8200 to 100 ppm, preferably from 7000 to 200 ppm.

Abstract: Described herein are methods for producing phosphonic compounds and compounds thereof.

Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.

Abstract: Described herein are methods for producing phosphonic compounds and compounds thereof.

Abstract: The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative by a radical initiated reaction. The invention also relates to compounds obtainable by the method of the invention.

Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R? and R? are each independently C1-C10 alkyl; R1 is CH3; and X is O; or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

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: A flame retarded thermoplastic polymer composition comprising a thermoplastic polymer and a metal salt of phosphinic acid possessing a desired degree of volatility.

Abstract: Provided are an additive to an electrode for a fuel cell that is a proton conductive compound having at least one phosphate group, an electrode for a fuel cell including the same, a method of manufacturing the electrode for a fuel cell, and a fuel cell using the electrode. The additive to an electrode for a fuel cell improves the durability of a fuel cell and reduces the amount of phosphoric acid discharged during operation of the fuel cell by fixing the phosphoric acid. Accordingly, a fuel cell having improved efficiency may be prepared using the additive because of improved proton conductivity and durability.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: The present invention relates to a process for the preparation of bis(perfluoroalkyl)phosphinic acids comprising at least the reaction of at least one difluorotris(perfluoroalkyl)phosphorane or at least one trifluorobis(perfluoroalkyl)phosphorane with hydrogen fluoride in a suitable reaction medium, and heating of the resultant reaction mixture. The invention also relates to salts of bis(perfluoroalkyl)phosphinic acids and to the use 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 above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: The invention relates to a process for preparing N-phosphono-methylglycine by reacting a hexahydrotriazine compound with a triacyl phosphite in an organic solvent, hydrolyzing the resulting phosphono compound after prior extraction into an aqueous phase and separation from the organic phase. The process avoids decomposition of the organic solvent during hydrolysis.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: A process for preparing vinylphosphonic acid compounds and silyl esters thereof in which a bis(haloalkyl)vinylphosphonate is reacted with an organosilyl halide to produce a silyl ester which can then be converted to the acid by reaction with a proton donor.

Abstract: In a process for the production of dialkylphosphinic acids, especially branched, dialkylphosphinic acids in high purity via the reaction of an alpha olefin with a hypophosphorous acid or a salt thereof, the improvement comprising conducting the reaction in the presence of a stoichiometric excess of the olefin and isolating and purifying the desired dialkylphosphinic acid product by neutralizing the monoalkylphosphinic acid by-product with an aqueous base; removing the aqueous phase in which the neutralized monoalkylphosphinic acid is preferentially solubilized; acidifying the dialkyl product in the organic phase; and isolating the purified product.

Abstract: The present invention relates to novel water-soluble, stable derivatives of combretastatin A-4, and novel synthesis methods therefore. The combretastatin A-4 prodrugs described herein appear to be useful in the treatment of neoplastic disease.

Abstract: This invention is related with the preparation of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof. The reaction of 4-aminobutyric acid with phosphorous acid and phosphorus trichloride in the presence of aralkyl or alkyl ethoxylates or triglycerides such as plant or animal oils or their derivatives; and recovering of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof are described. The main feature of the invention is in the use of the above defined non-ionic emulgators in the phosphonylation reaction.

Abstract: Vinyl phosphonic acid is produced by the hydrolysis of a vinyl phosphonic acid ester (e.g. “Bis Beta”) in the presence of a carbonyl compound (e.g. a monofunctional or difunctional aldehyde or a ketone).

Abstract: New hydrate forms of alendronate sodium, having water content of between about one and about twelve percent, and processes for their manufacture, are disclosed. New crystalline forms of alendronate sodium B, D, E, F, G and H, and processes for manufacturing them, are also disclosed. These new forms of alendronate sodium are suitable for incorporation into pharmaceutical compositions for combating bone resorption in bone diseases.

Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.

Abstract: Diphosphine of formula I R1R2P—H2C—Ar—CH2PR1R2??(I) are prepared by a process that comprises a) reacting a dimethyl compound of formula II H3C—Ar—CH3??(II) with a base and an N-substituted aminophosphorous halide to form bis(aminophosphinomethyl) compound of the formula III R3R4P—H2C—Ar—CH2—PR3R4??(III) b) reacting the compound of formula III with HCl to form bis(dichlorophosphinomethyl) compound of formula IV Cl2P—H2C—Ar—CH2—PCl2??(IV) and c) reacting the compound of formula IV with an organometallic reagent to give the product compound of formula I, wherein groups R1 and R2 are each, independently of one another, a substituted or unsubstituted aromatic, heteroaromatic or aliphatic hydrocarbon group and may have a covalent bond connecting them and Ar is a substituted or unsubstituted aromatic or heteroaromatic hydrocarbon group an R3 and R4 are each, independently of one another, an N-substituted alkylamino or arylamino group.

Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: Novel compounds of formula I, with the exception of i) the racemate of (3-amino-2-hydroxypropyl)phosphinic acid; and ii) (2R/S,3R)-(3-amino-2-hydroxybutyl)phosphinic acid, having affinity to one or more GABAB receptors, their pharmaceutically acceptable salts, solvates and stereoisomers, as well as processes for their preparation, pharmaceutical compositions containing said therapeutically active compounds and the use of said active compounds in therapy.

Abstract: Vinyl phosphonic acid is produced by the hydrolysis of a vinyl phosphonic acid ester (e.g. “Bis Beta”) in the presence of a carbonyl compound (e.g. a monofunctional or difunctional aldehyde or a ketone).

Abstract: Fluorinated phosphonic acid compounds, useful as treatments for substrate surfaces, have the formula: wherein: R1 is a straight chain alkylene group having from about 3 to about 21 carbon atoms, an oxa-substituted straight chain alkylene group having from about 2 to about 20 carbon atoms, or a thia-substituted straight chain alkylene group having from about 2 to about 20 carbon atoms; R2 is a perfluoroalkyl group having from about 4 to about 10 carbon atoms; R3 is hydrogen, an alkali metal cation, or an alkyl group having from about 1 to about 6 carbon atoms; and M is hydrogen or an alkali metal cation, with the proviso that if R1 is an unsubstituted straight chain alkylene group, then the sum of carbon atoms in R1 and R2 combined is at least 10.

Abstract: The invention relates to a process for the preparation of (metal) salts of alkylphosphonous acids, which comprises reacting elemental yellow phosphorus with alkyl halides in the presence of carbonates, bicarbonates, amides, alkoxides, amine bases and/or solid hydroxides as bases. The invention also relates to the use of the (metal) salts of alkylphosphonous acids prepared by this process.

Abstract: The invention relates to a process for the preparation of (metal) salts of alkylphosphonous acids, which comprises reacting elemental yellow phosphorus with halogen-free alkylating agents in the presence of at least one base. The invention also relates to the use of the (metal) salts of alkylphosphonous acids prepared by this process.

Abstract: This invention relates to salts of guanidine derivatives of formula R—X—C(═NH)NH3+Z−, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH═N—NH—; R represents a linear or branched C1-C30 alkyl, C3-C20 cycloalkyl, adamantyl, norbornyl, tricyclodecyl, benzyl, furyl, pyridyl, anthracyl, naphthyl, phenanthryl, perinaphthyl or quinuclidinyl residue, which can be substituted by one or more hydroxyl groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups; Z represents O—CO—Y, O—S(O)2—Y, or O—P(O)(OH)—Y; and Y represents a linear or branched C1-C12 alkyl, C3-C8 cycloalkyl, benzyl, furyl or pyridyl residue, which can be substituted by one or more hydroxyl groups, carboxylic acid groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups.

Abstract: A process for preparing vinylphosphonic acid compounds and silyl esters thereof in which a bis(haloalkyl) vinylphosphonate is reacted with an organosilyl halide to produce a silyl ester which can then be converted to the acid by reaction with a proton donor.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.

Abstract: This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.

Abstract: The invention relates to novel compounds of genera formula (I), with inhibitory properties for the type B botulism toxin activity, the methods for preparation thereof and corresponding pharmaceutical compositions. The invention further relates to corresponding pharmaceutical compositions.

Abstract: A novel class of compounds, i.e., 1,1-bis-H-phosphinates (or 1,1-bis-H-phosphinic acid derivatives) are provided. Also provided are novel methods for producing 1,1-bis-H-phosphinates and 1,1-bis-H-phosphinate conjugates. These compounds and conjugates are used are precursors of bisphosphonates and bisphosphonate conjugates, respectively, or as prodrugs directly for treating bone-related and various other diseases.

Abstract: Vinylphenylpropionic acid derivatives; processes for producing the derivatives; polymers of the same; and radiosensitive resin compositions containing the polymers. The above polymers exhibit low radiation absorption and are useful as the resin component of radiosensitive resin compositions particularly suitable for chemically amplified resists. For example, t-butyl 4-vinylphenylpropionate is produced by (1) reacting t-butyl bromoacetate with tri(n-butyl)phosphine to obtain a quaternary phosphonium salt, (2) reacting this salt with a base to obtain a phosphorus ylide, (3) reacting this ylide with 2,4,6-tris(3′,5′-di-t-butyl-4′-hydroxybenzyl)methyl-styrene to obtain a quaternary phosphonium salt, and (4) hydrolyzing this salt.

Abstract: The present invention relates to a process for the preparation of alkylphosphonous acid esters which comprises a) reacting elemental yellow phosphorus with alkylating agents in the presence of a base to give a mixture which comprises, as principal constituents, the (metal) salts of alkylphosphonous, phosphorous and hypophosphorous acids, b) esterifying the principal constituents of the mixture from a) to give an ester mixture, c) isolating the ester of the alkylphosphonous acid from the ester mixture. The invention likewise relates to the use of the alkylphosphonous acid esters prepared by this process as precursors for further syntheses, inter alia for the preparation of crop protection agents.

Abstract: The invention relates to solid phase processes for the systematic preparation of chemical compounds from the group of the phosphonous or phosphinic acids and/or derivatives thereof and the corresponding substance libraries which can be employed for test purposes, in particular tests for biological activity.

Abstract: The invention relates to a process for preparing diphosphines of the formula

Abstract: 1

Abstract: Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.

Abstract: A process for the production of an organic phosphorus-containing product, which comprises reacting a phosphorus-containing oxide with an unsaturated hydrocarbon in the presence of a boron-containing compound at a temperature of less than or equal to 50° C.

Abstract: The present invention relates to therapeutically active novel spiro[2,4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: An improved regiospecific synthesis of organic phosphonous acids, comprising of hydrophosphorylation of an olefin with hydrophosphorous acid in the presence of an inorganic persulfate, which acts as a source of free radicals at a pH ranging from 4.5 to 7.0, in which the orientation of addition is anti-Markonikoff. The process enables production of organic phosphonous acids at lower temperature and atmospheric pressure under milder pH conditions for better regioselectivity in hydrophosphorylation and obtain the phosphonous acid with good yield and purity following simple isolation procedure. Phosphonous acids obtained by the process are commercially valuable as effective detergents and wetting agents, lubricants and lubricant additives, plasticizers for plastics and resins, corrosion inhibitors, chemicals including insecticides and pesticides, cobalt extractants and as key intermediates for preparation of commercially important angiotensin converting enzyme (ACE) inhibitors.

Abstract: The present invention relates to a process for the preparation of phosphonomethylglycine, wherein N-phosphonomethyliminodiacetic acid N-oxide is brought into contact with a catalytically effective amount of thiocyanic acid or a salt thereof.

Abstract: A process for removing a phosphorus protecting group from a protected phosphate triester or phosphorothioate triester includes contacting a protected phosphate or phosphorothioate triester with a thiol compound that is not offensive to the olfactory senses.

Abstract: A single-stage method for producing &agr;-hydroxy ethers by oxidizing olefinic substrates with organic hydroperoxides and opening the resultant oxirane ring by means of monovalent or polyvalent alcohols wherein a molybdenum compound in combination with a compound selected from the group consisting of boron trifluoride, aluminum oxides, 1,8-diazabicyclo-[5.4.0]-undec-7-ene or 1,4-diazabicyclo-[2.2.2]-octane, and mixtures thereof is used as a catalyst system.

Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1

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.