Abstract: The present invention relates to a new process for the preparation of the crystalline polymorph of sodium neridronate in form hemihydrate F, comprising the following steps: a) reacting the 6-aminohexanoic acid with a mixture of phosphorous acid and methanesulfonic acid at a temperature in the range from 60 to 80° C., under stirring, until a clear solution is obtained; b) adding phosphorus trichloride to said solution of step (a) under stirring at a temperature in the range of 60 to 80° C.; c) diluting with water the reaction mixture obtained from the previous step (b) and heating said water diluted mixture at a temperature in the range from 80 to 120° C.; d) cooling the heated mixture obtained in step (c) up to room temperature, diluting it with water, then slowly adding an aqueous sodium hydroxide solution up to a pH in the range from 4.2 to 4.6, to obtain a neutralized solution; e) bringing the neutralized solution of step (d) up to a temperature of about 70° C.

Abstract: The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance.

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 technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.

Abstract: Disclosed herein are high structured carbon blacks, methods of synthesis and treatment, and dispersions and inkjet ink formulations prepared therefrom. The carbon black can have the following properties: OAN?170 mL/100 g; and STSA ranging from 160 to 220 m2/g. The carbon black can also have the following properties: OAN?170 mL/100 g; and a ratio of STSA/BET surface area ranging from 0.7 to 1.

Abstract: Methods, compositions and kits are provided for enhancing remineralization of a tooth or bone containing hydroxyapatite and inhibiting caries progression or loss of hydroxyapatite using a bisphosphonate or pyrophosphonate. The tooth or tooth surface contains a trauma or defect, for example the tooth contains a caries that is identified using a detectable probe. The bisphosphonate or pyrophosphonate is contacted to the tooth and/or oral cavity and binds to the hydroxyapatite material in the tooth or bone and prevents loss of hydroxyapatite material or strengthens the hydroxyapatite. The amount and extent of enhanced remineralization or of inhibition of caries progression and loss of hydroxyapatite are determined by techniques including photography, light microscopy and fluorescence microscopy.

Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.

Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Abstract: The present invention discloses 18FDG conjugated positron emission tomography (PET) imaging agents. In particular, the present invention discloses a cancer specific 18FDG multimeric PET imaging agents.

Abstract: The present invention describes tripodal bisphosphonate derivatives with a flexible basic framework for the functionalisation of surfaces, and methods for their production and use. The central atom of the flexible framework is hereby a tertiary aliphatic carbon atom. A fourth remaining position of the flexible framework is suitable to be optionally functionalised by so-called click reactions, for example with biomolecules, polyethylene glycol or active agents.

Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.

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: The present invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.

Abstract: The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).

Abstract: This disclosure relates to compositions and methods including for the inhibition, prevention, and/or treatment of microbial infections, including infections from such pathogens as Staphylococcus aureus.

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: A process for preparing a bisphosphonate compound comprises reacting a carboxylic acid with a phosphonating agent, in a cresol solvent.

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: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallisation.

Abstract: The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: -n and m denote, independently of one another, an integer ranging from 1 to 4, —X denotes an oxygen atom or an N—R3 group, —R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and —R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.

Abstract: The invention relates to devices, methods and formulation for subcutaneous administration of a bisphosphonate. In such a device, a drug core, comprising a bisphosphonate, is disposed in a tube. The devices may be administered to a patient in need of subcutaneously wherein the release of the bisphosphonate is desired to provide sustained release of a therapeutically effective dose of the bisphosphonate.

Abstract: This document provides methods and materials related to hydroxyapatite particles. For example, hydroxyapatite particles, methods for making hydroxyapatite particles, and methods for using hydroxyapatite particles are provided herein.

Abstract: The invention relates to a novel multi step synthesis of 3-(N-methyl-N-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid, monosodium salt, monohydrate, of the formula

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: Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3?-pyridyl or 2?-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.

Abstract: A novel method of treating endometriosis is disclosed. The method comprises administering to a female subject in need thereof a therapeutically effective amount of particles comprising an agent capable of inhibiting phagocytic cells of the female subject.

Abstract: Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phosphorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, an inert support or ortho-phosphoric acid codiluent is advantageously included.

Abstract: A manufacturing process for the preparation of bisphosphonic acids and in particular zoledronic acid is provided wherein diglyme, monoglyme, or a mixture thereof, is utilized to produce a homogenous, water soluble, solid reaction mass that upon cooling, dissolving in water and stripping results in a high purity product and comparatively good yield.

Abstract: The present application describes deuterium-enriched alendronate sodium, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: An improved process for bisphosphonylation of acids, substituted acids to obtain compounds with the formula using phosphorus trihalide, phosphorus acid, in presence of phenolic compounds as diluent/solvent.

Abstract: Amorphous ibandronic acid is provided with methods for its preparation. The methods include dissolution of ibandronic acid in a solvent such as acetonitrile, DMSO, methanol, or water, and spray drying.

Abstract: Provided are crystalline forms of ibandronate sodium, as well as processes for the preparation thereof.

Abstract: 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.

Abstract: The invention concerns biphosphonic compounds of formula (I); microbiological anti-contamination compositions containing same, and their use for preventing or limiting fixing of macromolecules, micro-organisms and biofilm on solid surfaces, such as metal or mineral surfaces.

Abstract: The present invention provides a novel process for preparation of bisphosphonic acids or salts thereof, e.g. alendronic acid, by reacting a carboxylic acid, phosphorous acid and a halophosphorous compound in a water miscible neutral solvent.

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract: The present invention is to relate an improved process using anisole as solvent for the preparation of compound of formula (I) and its pharmaceutically acceptable salts thereof. wherein R represents —NR1R2, or a group n=1, 2, 3, 4 and 5, where R1 and R2 may be same or different and independently represents hydrogen, or C1-6 alkyl.

Abstract: A process for preparing alendronate sodium includes the reaction of gammabutyric acid with phosphorous acid and phosphorus trichioride and subsequent treatment with an aqueous solution of an alkali metal hydroxide, in which the reaction is conducted in liquid ionic solvents.

Abstract: A salt of substituted or unsubstituted methylene bisphosphonic acid of formula I wherein X1 and X2 are both chlorine or one of X1 and X2 is hydrogen and one is chlorine and the salt is selected from the group consisting of a C1-16 straight or branched primary, secondary or tertiary alkyl amine salt, an aralkyl amine salt, and a basic N-containing heterocycle salt. The salts are used for preparing pharmaceutically relevant compounds.

Abstract: An improved process for bisphosphonylation of acids, substituted acids to obtain compounds with the formula using phosphorus trihalide, phosphorus acid, in presence of phenolic compounds as diluent/solvent.

Abstract: The invention relates to a novel multi step synthesis of 3-(N-methyl-N-pentyl) amino-1-hydroxypropane-1,1-diphosphonic acid, monosodium salt, monohydrate, of the formula

Abstract: Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1–C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl.

Abstract: In a method for preparing 1-hydroxy-1,1-diphosphonic acid compounds of the general formula I and/or of their pharmacologically compatible salts a compound of the formula II is reacted with a compound P(OSiR53)3-pR6p and the reaction product is hydrolyzed.

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: The present invention relates to derivatives of 1-hydroxymethylene-1,1-bisphosphonic acid, the pharmaceutical compositions comprising them, and their application in therapeutics, particularly for the treatment of cancerous tumors. It is also directed to a methods of preparation of such derivatives.

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: In a method for making bisphosphonates by reacting a carbonyl compound with a phosphorus halide, the reaction is carried out in a solvent/carrier system which is a mixture of an amine hydrochloride, phosphorous acid and optionally phosphoric acid.

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: 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.