115 results about "Phosphonic acid derivatives" patented technology

Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.

A field effect transistor includes a gate dielectric with a self-assembled monolayer of an organic compound, where the organic compound includes a phosphonic acid group. The phosphonic acid group additionally has an organic radical selected from the group consisting of (a) an alkyl chain including 1 to 20 carbon atoms, (b) oligo(thio)ether chains and / or c) aromatic or heteroaromatic compounds. In addition, a method for fabricating a field effect transistor includes forming a self-assembled monolayer of an organic compound as a gate dielectric, where the organic compound includes a phosphonic acid group.

The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halophosphorous compound is selected from the group comprising of PCl3, PCl5, POCl3, PBr3, POBr3, and PBr5 in presence of diphenyl ether.

Method of performing condensation reactions, acylations or of preparing heterocycles comprising forming cyclic phosphonic anhydride of the formula (III) by a) reacting phosphonic acid derivatives of formula (I) with acetic anhydride at a temperature ranging between 30 and 150° C. while separating a mixture of ethanoic acid and acetic anhydride by means of distillation, b) then reactively distilling the oligomeric phosphonic acid anhydrides of formula (II) obtained in step a) and transforming the same into the corresponding cyclic trimeric phosphonic acid anhydrides of formula (III), wherein n represents a number between 0 and 300 while R represents allyl, aryl, or open-chain, cyclic, or branched C1 to C8 alkyl radicals, aryloxy, allyloxy, or alkoxy comprising open-chain, cyclic, or branched C1 to C8 alkyl radicals. Preferably the cyclic trimeric phosphonic acid anhydrides formed in step b) are immediately dissolved in an organic solvent that exhibits an inert behavior relative thereto.

Method of performing condensation reactions, acylations or of preparing heterocycles comprising forming cyclic phosphonic anhydride of the formula (III) by a) reacting phosphonic acid derivatives of formula (I) with acetic anhydride at a temperature ranging between 30 and 150° C. while separating a mixture of ethanoic acid and acetic anhydride by means of distillation, b) then reactively distilling the oligomeric phosphonic acid anhydrides of formula (II) obtained in step a) and transforming the same into the corresponding cyclic trimeric phosphonic acid anhydrides of formula (III), wherein n represents a number between 0 and 300 while R represents allyl, aryl, or open-chain, cyclic, or branched C1 to C8 alkyl radicals, aryloxy, allyloxy, or alkoxy comprising open-chain, cyclic, or branched C1 to C8 alkyl radicals. Preferably the cyclic trimeric phosphonic acid anhydrides formed in step b) are immediately dissolved in an organic solvent that exhibits an inert behavior relative thereto.

Metal pigment particles are treated with a product resulting from the reaction between an organic phosphonic acid with an amine having at least one organic group containing at least six carbon atoms to inhibit their reactivity to water. The treated metal particles can be used in coating and ink compositions. Additionally, the treated metal particles can be used to formulate pastes and dispersions that are provided to a coatings manufacturer.

The present invention relates to phosphoric acid / phosphonic acid derivatives shown by formula (I), wherein R1 and R2 represent the following structures: (Q1), or (Q2), or (Q3). Q1 represents ester derivatives of L-amino acids, wherein R3 is alkyl or cycloalkyl with 1-6 carbon atoms, and R4 is H or alkyl with 1-6 carbon atoms; Q2 represents hydroxyl substituted benzodioxane derivatives; Q3 represents hydroxyl substituted benzodioxolane derivatives; R1 and R2 are the same or different, but at least one of them is Q2 or Q3; D represents residues of pharmacologically active molecules containing a phosphoric acid / phosphonic acid group, i.e. formula (II) represents pharmacologically active molecules containing a phosphoric acid / phosphonic acid group; and when R1 and R2 are different, the configuration of the P atom connected to R1 and R2 is of R or S type.

The present invention relates to methods of treating psoriasis by inhibiting one or more matrix metalloproteinase enzymes ("MMPs"). It is based, at least in part, on the discovery that the expression patterns of certain MMPs and related molecules are altered in patients suffering from psoriasis, relative to normal subjects. Certain expression patterns are altered even in unaffected skin of psoriasis-afflicted patients, although aberrancies are more pronounced in psoriatic lesions. In various non-limiting embodiments, the present invention provides for methods of treating psoriasis, including preventing the development of new psoriatic lesions, comprising administering, to subjects in need of such treatment, effective concentrations of compounds which inhibit the enzymatic activity of one or more MMP. Suitable inhibitors include tetracycline and its derivatives and various hydroxymate, carboxylic acid, and phosphonic acid derivatives. Therapy may comprise systemic and / or local administration of inhibitor. In additional embodiments, the present invention provides for methods of diagnosing MMP inhibitor responsive skin lesions, for evaluating the level of disease activity in a subject, and for transgenic animal and tissue culture models of psoriasis.

This invention discloses a composition for stabilizing ascorbic acid derivative and the application thereof. The mentioned composition comprises ascorbic acid derivative, buffer, phosphonic acid derivative and at least one alcohol. The yellowish and degradation of ascorbic acid derivative can be efficiently decreased by the mentioned composition. Moreover, the mentioned composition can be used in topical composition, such as toner, serum, lotion, cream.

Disclosed is a radioactive bone diagnostic agent which gives a high ratio of radioactivity accumulation in bone to that in blood from an early stage after administration of the agent and allows capturing an image in a short time after administration. Also disclosed is a bisphosphonic acid derivative represented by the following chemical formula (II) or a salt thereof, wherein X represents —(CH2)mCO—, Y represents —(CH2)n—, R represents H, OH, or a halogen atom, m and n are independent of each other and m represents an integer of 1 to 3, and n represents an integer of 0 to 4.

The present invention provides a non-aqueous electrolyte solution which contains a silyl ester group-containing phosphonic acid derivative.

The present invention provides methods for the preparation of aralkyl phosphonic acids and aryl phosphonic acids. In a first method of the invention, an aralkyl dialkyl phosphonate is contacted with an aqueous acidic solution under reflux conditions. Upon cooling, solid crystals of the corresponding aralkyl phosphonic acid are obtained, which can be collected via filtration. In a second method of the invention, an aryl phosphorous dihalide is added to a pot containing an aqueous nitric acid solution while maintaining the pot temperature below about 50° C. and then allowing the reactants to self-reflux. Upon cooling, crystals of the corresponding aryl phosphonic acid are obtained, which can be collected via filtration.

The invention provides a binuclear platinum (II)-diphosphonic acid coordination compound, a preparation method and an application thereof, and belongs to the field of anti-cancer drugs. The binuclear platinum (II)-diphosphonic acid coordination compound has the structural formula shown in the description, wherein n is 2, 3, 4 or 5. The preparation method of the binuclear platinum (II)-diphosphonic acid coordination compound comprises the following steps: diphosphonic acid derivative and Pt(en)(OSO3)(H2O) are reacted under the function of Ba(OH)2 to obtain the binuclear platinum (II)-diphosphonic acid coordination compound. According to the compound, a link arm of C between diphosphonates is expanded; quinary aromatic amine (namely imidazole) is introduced in, so that at the initial usage stage of the coordination compound, the coordination compound has high intake in tumour cells and long residence time; and the aggregation concentration of the coordination compound in other non-targeted tissues is greatly reduced.

The present invention relates to methods of treating psoriasis by inhibiting one or more matrix metalloproteinase enzymes ("MMPs"). It is based, at least in part, on the discovery that the expression patterns of certain MMPs and related molecules are altered in patients suffering from psoriasis, relative to normal subjects. Certain expression patterns are altered even in unaffected skin of psoriasis-afflicted patients, although aberrancies are more pronounced in psoriatic lesions. In various non-limiting embodiments, the present invention provides for methods of treating psoriasis, including preventing the development of new psoriatic lesions, comprising administering, to subjects in need of such treatment, effective concentrations of compounds which inhibit the enzymatic activity of one or more MMP. Suitable inhibitors include tetracycline and its derivatives and various hydroxymate, carboxylic acid, and phosphonic acid derivatives. Therapy may comprise systemic and / or local administration of inhibitor. In additional embodiments, the present invention provides for methods of diagnosing MMP inhibitor responsive skin lesions, for evaluating the level of disease activity in a subject, and for transgenic animal and tissue culture models of psoriasis.

The present invention relates to phosphoric acid / phosphonic acid derivatives shown by formula (I), wherein, R1 or R2 represents the following structures: (Q1), or (Q2), or (Q3). Q1 represents ester derivatives of L-amino acid, wherein R3 is alkyl with 1-6 carbon atoms or cycloalkyl, R4 is H or alkyl with 1-6 carbon atoms; Q2 represents hydroxyl substituted benzodioxane derivatives; Q3 represents hydroxyl substituted benzodioxolane derivatives; R1 or R2 is the same or different, but at least one of them is Q2 or Q3; D represents residues of pharmacologically active molecules containing a phosphate / phosphonate group, i.e. formula (II) represents pharmacologically active molecules containing a phosphate / phosphonate group; and when R1 and R2 are different, the configuration of the P atom connected to R1 and R2 is of R or S type.

The invention discloses a method for preparing a surface phosphorylated water-soluble carbon nanotube and the prepared carbon nanotube. The method comprises the following steps of: purifying a carbon nanotube, performing calcination treatment on the purified carbon nanotube, and putting into aqueous solution of a phosphonic acid derivative of an aromatic compound; performing ultrasonic dispersion for 3 to 10 hours; filtering and repeatedly washing; and drying at the temperature of between 25 and 40 DEG C to obtain the surface phosphorylated water-soluble carbon nanotube. In the invention, a -PO3H2 functional group is modified on the surface of the carbon nanotube through nonconvalent binding under the action of pi-pi accumulation conjugation, so that the unique property of the carbon nanotube is maintained and the dispersion stability of the carbon nanotube in water is improved on the basis of high water solubility of the phosphonic acid functional group. The preparation method has definite and reliable mechanisms, is simple and practicable and is low in price; and the prepared carbon nanotube has high dissolution dispersibility in the water and has a wide application prospect in the field of material science and biomedicine.

The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halophosphorous compound is selected from the group comprising of PCl3, PCl5, POCl3, PBr3, POBr3, and PBr5 in presence of diphenyl ether.

Disclosed is a method of fabricating an array substrate for a liquid crystal display, including forming a copper-based metal layer on a substrate and etching the copper-based metal layer using an etchant composition thus forming gate wiring, and forming a copper-based metal layer on a semiconductor layer and etching the copper-based metal layer using the etchant composition thus forming source / drain electrodes, the etchant composition including based on the total weight of the composition, A) 5.0 ~ 25 wt% of hydrogen peroxide (H2O2), B) 0.01 ~ 1.0 wt% of a fluorine-containing compound, C) 0.1 ~ 5.0 wt% of an azole compound, D) 0.1 ~ 10.0 wt% of one or more compounds selected from among phosphonic acid derivatives and salts thereof, and E) a remainder of water.

The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and / or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).

A pigment grade corrosion inhibitor and a method of forming the inhibitor is disclosed. The inhibitor is comprised of a host species comprised of an inorganic compound having a layered structure and a guest species comprised an anionic species of a weak acid. The host species is preferably a double hydroxide having a structure of: [M(II)1-xM(III)x(OH−)2] [An−x / n.y H2O], where M(II) is a divalent metal cationic species, M(III) is a trivalent metal cationic species, and An− is an anionic species, preferably with the species present in a range of: 0.2≦M(III) / (M(II)+M(III))≦0.4. The guest species include: ortho-phosphoric, pyrophosphoric, tripoly-phosphoric, polyphosphoric acid; mono- and di-alkyl or aryl-esters of ortho-phosphoric and pyrophosphoric acid; metaphosphoric, trimeta-phosphoric, poly-metaphosphoric acid; phosphorous (phosphonic) acid; derivatives of phosphonic acid; alkyl and aryl esters of thio-phosphoric and dithio-phosphoric acid; molybdic, phospho-molybdic, silico-molybdic acid; boric acid; cyanamidic acid; nitrous acid; derivatives of thio- and dithiocarbonic acid, including o-alkyl esters; derivatives of dithiocarbamic acid, including N-alkyl dithiocarbamates; pyrrolidinecarbodithioic acid; thio-organic compounds functionalized with at least one —SH group of acidic character, including: 2,5-dimercapto-1,3,4-thiadiazole (DMTD), 2,4-dimercapto-s-triazolo-[4,3-b]-1,3-4 thiadiazole, trithiocyanuric acid (TMT), and dithiocyanuric acid, various N—,S— and N,N—, S,S— and N,S-substituted derivatives of the above DMTD and TMT compounds; various S-substituted derivatives of trithiocyanuric acid; dimer and polymer derivatives of the above DMTD and TMT compounds, including 5,5′ dithio-bis (1,3,4 thiadiazole-2(3H)-thione or (DMTD)2, and (DMTD)n, polymers of DMTD and (TMT)2, dimers and polymers of TMT; various combinations of all the above; soluble salts of DMTD and TMT; poly-ammonium salt of DMTD or (DMTD)n and TMT formed with polyamines; mercapto-benzothiazole, mercapto-benzoxazole, mercapto-benzimidazole, and combinations, thereof; di- and poly-mercapto compounds, including: di-mercapto derivatives of thiophene, pyrrole, furane, diazoles, and thiadiazoles; di- and tri-mercapto derivatives of pyridine, diazines, triazines, benzimidazole, and benzothiazole, including dimercaptopyridine, 2, 4-dithiohydantoine, and 2,4,-dimercapto-6-amino-5-triazine; and carboxylic and di-carboxylic acids, including ascorbic, salicylic acid, phthalic acid, nitro-phthalic acid, succinic acid, and derivatives of succinic acid, including 1-(benzothiazol-2-ylthio)succinic acid.

The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and / or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).

The invention belongs to the field of medical chemistry, relates to phosphonic acid derivatives for treating virus infectious diseases and an application thereof, and in particular, relates to the compounds represented by the formula (I) or isomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method thereof, pharmaceutical compositions containing the compounds and an application of the compounds or the compositions in preparation of drugs for treating the virus infection diseases.

The present invention provides a method for producing a pastel rosin ester in high yield in a short period of time. The present inventors have found that by using a catalyst group that uses a phosphonic acid derivative having an alkaline earth metal compound and an alkyl group having a carbon number of at least 7 as a substituent or a reaction product of both (i.e., having a carbon atom number of at least a phosphonate and / or derivative of a phosphonic acid and / or a derivative of 7 and a salt of an alkaline earth metal compound) is used as a catalyst, and a rosin and an alcohol are reacted to produce a light-colored rosin ester in a short period of time with high efficiency .

An agent for periodontal disease includes, as an active component, a methanebisphosphonic acid derivative or a hydrate thereof represented by the general formula (I):[wherein X, Y, m, n,The methanebisphosphonic acid derivative represented by the general formula (I) or a hydrate thereof according to the present invention has activities such as inhibitory effect on cell infiltration to the affected part associated with periodontal disease, and is useful for the prophylaxis or treatment of periodontal disease.

This invention discloses a method for stabilizing ascorbic acid derivatives and the application thereof. The mentioned method comprises mixing ascorbic acid derivative with a non-water-in-oil composition, and the composition comprises buffer, phosphonic acid derivative and at least one alcohol. The yellowish and degradation of ascorbic acid derivative can be efficiently decreased by the mentioned method. Moreover, the mentioned method can be used in topical composition, such as toner, serum, lotion, cream.

The invention relates to a method for preparing F-Dopa and 18F-Dopa and intermediates that are useful in the method. The invention is a method that synthesizes F-Dopa and 18F-Dopa in good yield with high enantiopurity without the need for further transformations. The method includes the step of reacting a benzaldehyde derivative with a phosphonic acid derivative to produces an olefin intermediate that can be asymmetrically hydrogenated to produce the desired enantiomer.

The present invention provides methods and compositions for detecting, identifying and measuring the abundance of chemical nerve agents. Methods and compositions of the present invention are capable of providing selective detection of phosphorous based nerve agents, such as nerve agents that are esters of methyl phosphonic acid derivatives incorporating a moderately good leaving group at the phosphorus. Selectivity in the present invention is provided by a sensor composition having an alpha (α) effect nucleophile group that undergoes specific nucleophilic substitution and rearrangement reactions with phosphorus based nerve agents having a tetrahederal phosphorous bound to oxygen. The present invention includes embodiments employing a sensor composition further comprising a reporter group covalently linked to the alpha effect nucleophile group allowing rapid optical readout of nerve agent detection events, including direct visual readout and optical readout via spectroscopic analysis.