Abstract: The present invention is related to a method for the synthesis of ethane-1-hydroxy-1,1-diphosphonic acid or its salt which includes the steps of reacting tetraphosphorus hexaoxide and acetic acid under controlled reaction conditions; hydrolyzing the formed ethane-1-hydroxy-1,1-diphosphonic acid condensates to form ethane-1-hydroxy-1,1-diphosphonic acid; further processing the ethane-1-hydroxy-1,1-diphosphonic acid solution. The process according to the method of the present invention is highly controllable and further is characterized by a high selectivity.

Abstract: There is provided a process for preparing a perfluorovinyl ether sulfinate, comprising: a) providing a perfluorovinyl ether sulfonyl halide; and (b) reducing the perfluorovinyl ether sulfonyl halide with a reducing agent in an organic protic solvent.

Abstract: Endosseous implant to be applied to a human or animal bone, wherein the surface of the implant is made from titanium or a titanium alloy, said implant having a smooth or rough surface texture, which is characterized in that said surface has been treated with at least one selected organic phosphonate compound or a pharmaceutically acceptable salt or ester or an amide thereof; process for producing said implants.

Abstract: The invention relates to a method for preparing a bisphosphonate covalently bonded to a nanostructure. This invention also relates to a bisphosphonate having incorporated therein a radioisotope selected from 32p or 33P, preferably 33p, wherein the bisphosphonate is covalently bonded to a nanostructure directly or by way of a linker, and to the use thereof in a method of treating calcific tumours in a patient.

Abstract: The present invention relates to novel polymorphs of (2E)-1-hydroxy-2-methylpent-2-enyl-pyrophosphonate disodium (CHDMAPP-Na2), to the process for preparing them and to the pharmaceutical compositions containing them.

Abstract: Endosseous implant to be applied to a human or animal bone, wherein the surface of the implant is made from titanium or a titanium alloy, said implant having a smooth or rough surface texture, which is characterized in that said surface has been treated with at least one selected organic phosphonate compound or a pharmaceutically acceptable salt or ester or an amide thereof; process for producing said implants.

Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

Abstract: An absorption medium for the removal of acid gases from a fluid stream comprises an aqueous solution a) of at least one amine and b) at least one phosphonic acid, wherein the molar ratio of b) to a) is in the range from 0.0005 to 1.0. The phosphonic acid is, e.g., 1-hydroxyethane-1,1-diphosphonic acid. The absorption medium exhibits a reduced regeneration energy requirement compared with absorption media based on amines or amine/promoter combinations, without significantly decreasing the absorption capacity of the solution for acid gases.

Abstract: Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3) wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 groups are linked to form a C1-C3 alkylene group; and R2 is hydrogen, a C1-C6 alkyl group, a C1-C6 alkoxy group, or is linked together with R to form a C3-C7 carbon ring.

Abstract: This invention relates to compounds of formulae (1a) and (1b) wherein R means H or C1- to C6-alkyl, X is a structural unit selected from the formulae wherein m and k mean independently from each other a number from 1 to 12 for (4) and (5) and from 1 to 11 for (6), Y is a structural unit selected from the formulae wherein a, b independently from each other are integers from 1 to 10 R means hydrogen or C1- to C6-alkyl R2 means an alkylene or alkylidene group having 1 to 6 carbon atoms or an arylene or alkylarylene group having from 6 to 20 carbon atoms R3, R4, R5, R6 independently from each other mean an alkylene or alkylidene group having 1 to 6 carbon atoms or an arylene or alkylarylene group having from 6 to 20 carbon atoms, Z means a cation, and n means an integer being two or higher.

Abstract: An adduct of 1-hydroxyethylidene-1,1-diphosphonic acid and from 0.5 to 10 moles of ethylenediamine disuccinic acid or a salt thereof per mole of 1-hydroxyethylidene-1,1-5 diphosphonic acid, wherein said adduct is in the form of a solid.

Abstract: N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products.

Abstract: A process for the preparation of biphosphonic acids and pharmaceutical acceptable salts thereof, comprises reacting a carboxylic acid with phosphorous trichloride and phosphorous acid in the presence of an aprotic polar solvent.

Abstract: Disclosed herein is a process for producing bisphosphonic acids and salts thereof. The process comprising reacting a carboxylic acid of Formula [I] with phosphorous acid and halophosphorus compound in the presence of a solvent selected from aliphatic hydrocarbon or water miscible cyclic ether. Further, the present invention also provides novel forms of bisphosphonic acids and process for preparation thereof.

Abstract: The present invention relates to a composition for prevention and/or treatment of metabolic diseases of bones comprising at least one bisphosphonate; viscosity agents comprising carboxymethylcellulose and xanthan gum; at least one flavoring agent; and purified water; a process for preparing a composition according to the present invention; and use of such a composition for prevention, treatment and/or diagnosis of metabolic diseases of bones, especially for children.

Abstract: This invention relates to the process of making geminal bisphosphonic acids and pharmaceutically acceptable salts and/or hydrates thereof which have the formula (I): wherein X1, X2, X3, X1R1 and R2 are described herein.

Abstract: This invention relates to a process for producing a substantially pure disulfide compound of Formula II as disclosed herein, such as disodium 2,2?-dithiobis ethane sulfonate, by an efficient procedure from available, relatively inexpensive raw materials.

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: The invention relates to processes for preparing and purifying zoledronic acid.

Abstract: The invention relates to the isolation of etidronate disodium whereby

Abstract: A process for the preparation of salts of substituted or unsubstituted methylene bisphosphonic acids by hydrolysing the corresponding acid ester with hydrochloric acid, removing water from the acid azeotropically prior to addition of an amine or a base to produce the resultant salt in good yield.

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: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.

Abstract: A method for the preparation of alkene phosphonic acids and salts thereof, such as VDPA (vinylidene diphosphonic acid) is disclosed. The products can be produced in a stable, substantially pure form and in high yield. The method includes the azeotropic removal of water from salts of &agr;-hydroxy-alkane diphosphonic acid dimer or corresponding acids thereof, and the pyrolysis of the dehydrated reactant at a temperature of from 170° C. to 300° C. There may be included a step to convert anhydrides which have been formed during the pyrolysis. The method may include the use of heat transfer agents and/or bases, and may be carried out at elevated or reduced pressure.

Abstract: A process for preparing aluminum salts (I) of dialkylphosphinic acids or (formula (II)) of alkylated diphosphinic acids where R1 and R2 are a linear or branched C1-C8-alkyl radical and R3 is a linear or branched C1-C10-alkylene radical or an arylene radical or an alkylarylene radical or an arylalkylene radical, which comprises reacting a dialkylphosphinic acid ester of the formula (III) or a diphosphinic acid ester of the formula (IV) where R1, R2 and R3 are as defined above and R4 is a linear or branched C1-C8-alkyl radical, in the presence of a saturated aliphatic monocarboxylic acid having a total of from 1 to 7 carbon atoms, with aluminum hydroxide at a temperature of from 150 to 350° C.

Abstract: A process for manufacturing 1-hydroxyalkylidene-1,1-diphosphonic Acid (HADP) by introducing phosphorus trihalide (PX.sub.3) into a reactor containing aqueous acid of the formula RCOOH at a temperature of 60-200.degree. C. and a pressure of 15-150 psig. Water is added to hydrolyze the intermediate formed to obtain HADP.

Abstract: The present invention relates to disodium 4-chlorophenylthiomethylenebisphosphonate monohydrate.The invention further relates to the method of preparing this monohydrate.The invention further relates to the pharmaceutical compositions in which disodium tiludronate monohydrate is present as the active principle.

Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.

Abstract: The present invention concerns a novel process for the preparation of methylenebisphosphonic acids of the formula I ##STR1## wherein Q.sup.1 and Q.sup.2 are independently hydrogen or halogen, by hydrolyzing the corresponding methylenebisphosphonic acid tetraester of the formula ##STR2## wherein R has the meaning of a straight or branched alkyl group containing 1 to 4 carbon atoms, and Q.sup.1 and Q.sup.2 have the same meaning as above.

Abstract: 3-R.sup.1 -3-oxoprop-1-ene-1,1-diphosphonic acids corresponding to the following general formula ##STR1## in which R.sup.1 is a tertiary substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl or heteroaryl group, andM is hydrogen or the cation of a base;to a process for their production in which 3-R.sup.1 -3-oxo-1-aminopropane-1,1-diphosphonic acids corresponding to the following general formula ##STR2## in which R.sup.1 is as defined above, are reacted with an aqueous or alcoholic alkali metal hydroxide solution; then water followed by an alcohol infinitely miscible with water is added to the reaction mixture, and the pure olefinic diphosphonic acids are obtained by addition of an acid; to the use of the above compounds of formula III as complexing agents and as thresholders; and to compositions containing one or more compounds of formula (III).

Abstract: The present invention relates to 1-hydroxy-.omega.-(alkyl- or arylphosphinico)alkane-1,1-diphosphonic acids of the general formula I ##STR1## and to the salts of these acids of the general formula II ##STR2## where, in these formulae, R.sup.1 denotes an alkyl radical having 1 to 6 carbon atoms, a cycloalkyl radical having 5 to 7 carbon atoms or an aryl radical having 6 to 10 carbon atoms, R.sup.2 denotes a straight-chain or branched alkylene radical having 1 to 6 carbon atoms and A denotes a monovalent equivalent of a cation of an inorganic or organic base. In addition, processes are described for the preparation of these novel compounds.

Abstract: 3-R.sup.1 -3-oxoprop-1-ene-1,1-diphosphonic acids corresponding to the following general formula ##STR1## in which R.sup.1 is a tertiary substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl or heteroaryl group, andM is hydrogen or the cation of a base;to a process for their production in which 3-R.sup.1 -3-oxo-1-aminopropane-1,1-diphosphonic acids corresponding to the following general formula ##STR2## in which R.sup.1 is as defined above, are reacted with an aqueous or alcoholic alkali metal hydroxide solution; then water followed by an alcohol infinitely miscible with water is added to the reaction mixture, and the pure olefinic diphosphonic acids are obtained by addition of an acid; to the use of the above compounds of formula III as complexing agents and as thresholders; and to compositions containing one or more compounds of formula (III).

Abstract: Chemical compounds of the formula: ##STR1## in which R.sub.1 and R.sub.2 can be identical or different and represent hydrogen or alkyl having from 1 to 4 carbon atoms. The compounds are used in hair dyeing, and a process for their preparation is disclosed.