Abstract: Disclosed is a process for the preparation of compounds of formula (I) wherein R1 is C1-C4 alkoxy; R2 is hydrogen or a group of formula —CH2—PO3H2 or is a group of formula R1-O—(CH2—CH2O)n—CH2—CH2—; R3 is an alkylene, optionally substituted with one or more —NR2-groups; R4 and R5 are both a group of formula —CH2—PO3H2 or one of them is a group of formula —CH2—PO3H2 and the other is a group of formula R1-O—(CH2—CH2—O)-CH2-CH2-; n is an integer between 4 and 50; which comprises: a) reacting a compound of formula R1-O—(CH2—CH2—O)n—CH2—CH2—OH with SOCl2 or a similar reagent to give a compound of formula R1-O—(CH2—CH2—O)n—CH2—CH2—Cl; b) reacting the compound obtained in a) with an amine of formula NH2—R3?-NH2 wherein R3? is an alkylene optionally substituted with one or more —NH-groups; c) reacting the compound obtained in b) with formaldehyde and phosphorous acid.

Abstract: A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR', NH2, NHR?, N(R?)2, NH, N, S, S—S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0° C. or higher.

Abstract: A trimethylolpropane core, phosphonic acid terminated dendrimer and its preparation method are provided, And a preparation method thereof comprises steps of processing Michael addition reaction on trimethylolpropane triacrylate (CH3CH2C(CH2OCOCH2?CH2)3) and alkylidene diamine (NH2CH2(CH2)nNH2), wherein n is an integer from 1 to 5, so as to obtain trimethylolpropane core, amino group terminated dendrimer, and modifying the amino group by methylene phosphonic acid to obtain the trimethylolpropane core, phosphonic acid terminated dendrimer having a chemical formula of CH3CH2C[CH2OCOCH2CH2N(CH2PO3H2)CH2(CH2)nN(CH2PO3H2)2]3, wherein n is an integer from 1 to 5.

Abstract: A preparation method of octamethylenephosphonic acid terminated, PAMAM dendrimer and application thereof is provided, the dendrimer is prepared by modifying amino groups of 0 generation PAMAM dendrimer with methylene phosphonic acid, a constitutional formula thereof is: (CH2)n{N[CH2CH2CONHCH2CH2N(CH2PO3H2)2]2}2, wherein n is a positive integer between 2˜6. The octamethylenephosphonic acid terminated, PAMAM dendrimer has an excellent performance to inhibit scales of CaCO3, CaSO4 and Ca3(PO4)2, a very high calcium tolerance, and excellent dispersing performance. The octamethylenephosphonic acid terminated, PAMAM dendrimer is used as an antiscalant in industrial water treatment, and is suitable for the industrial water treatment of boiler, cooling, desalination, and oil production, etc., especially for the industrial water treatment under high calcium concentration.

Abstract: A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR?, NH2, NHR?, N(R?)2, NH, N, S, S—S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0° C. or higher.

Abstract: In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions. Also provided are a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement agent I.

Abstract: Scale control agents comprising organic phosphonates, either alone or in mixtures with inorganic phosphonates and also optionally polymers, such as low molecular weight polymeric dispersants. The scale control agents may be applied to inhibit scale formation or deposition in highly acidic aqueous systems by adding these agents to such systems in amounts effective to inhibit metal sulfate scale formation.

Abstract: The disclosure provides anionic Gemini surfactants comprising at least two carbonyl moieties and at least two aliphatic moieties. In some aspects, at least two of the aliphatic moieties comprise at least seven carbon atoms and at least one pair of conjugated carbon-to-carbon double bonds. The anionic Gemini surfactants are polymerizable and may be used to prepare triply periodic multiply continuous lyotropic phase and polymers thereof that substantially retain triply periodic multiply continuous lyotropic phase structure.

Abstract: A method for the manufacture of aminoalkylene phosphonic acids broadly is disclosed. In the essence, an amine corresponding to a specific formula is reacted in aqueous medium with phosphorous acid and formaldehyde to thereby yield a medium insoluble reaction product. The insoluble product formed i.e. the aminoalkylene phosphonic acid can be separated, optionally washed, and recovered. This process yields high purity and selectivity reaction products. The excess phosphonic acid can be recycled into the processing sequence.

Abstract: Disclosed are novel ring containing phospholipids represented by the structural formula A-X—PO3—W and physiologically acceptable salts thereof and a process for the preparation of these compounds. The compounds can be used for the treatment of protozoal diseases and especially leishmaniasis.

Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.

Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.

Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.

Abstract: A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR?, NH2, NHR?, N(R?)2, NH, N, S, S—S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0° C. or higher.

Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.

Abstract: This invention is directed to a process for making a salt of a carboxylic acid. The process comprises contacting a catalyst with an alkaline mixture comprising a primary alcohol. In one embodiment, for example, the catalyst comprises a metal support (preferably a metal sponge support) having a copper-containing active phase at the surface thereof. The support is resistant to deformation under the conditions of the dehydrogenation reaction. In another embodiment, the catalyst comprises a metal sponge having a copper-containing active phase at the surface thereof and a supporting structure containing at least 10% non-copper metal. This invention is also directed to copper-containing catalysts which may, for example, be used in the above process. This invention is further directed to processes for making such catalysts.

Abstract: Compounds of the formula wherein the substitutents are defined as in the specification useful for modulating immune responses in warm-blooded animals.

Abstract: In one embodiment, a scale inhibitor comprising at least one polymethylenephosphonate derivative having the following formula: wherein n is a number, wherein M is hydrogen or a cation, wherein R1, R2, and R3 are each independently selected from the group consisting of CH2PO3M2, CH2R4, wherein R4 is CHOHCH3, CHOHCH2Cl, or CHOHCH2OH, (CH2)mSO3M, wherein m is 3 or 4, and CH2CH2R5, wherein R5 is CONH2, CHO, COOR6, COOX, or CN, wherein R6 is CH3 or C2H5, and wherein X is an alkali metal or ammonium, and wherein at least one of R1, R2, and R3 is not CH2PO3M2. In another embodiment, a method for inhibiting scale formation in water, and in still another embodiment, a method for sequestering iron ions in a water systems, each of the methods comprising the step of providing the water with the above described polymethylenephosphonate derivative.

Abstract: The present invention relates to a process for the preparation of N-phosphonomethyliminodiacetic acid by reacting an alkali metal salt of iminodiacetic acid with phosphorus trichloride in aqueous solution with formation of the hydrochloride of iminodiacetic acid, phosphorous acid and of the corresponding alkali metal chloride, followed by reaction with a formaldehyde source and, if desired, recovery of the N-phosphonomethyliminodiacetic acid from the reaction mixture, in which water, which may comprise HCl, is removed from the reaction mixture during and/or after reacting the alkali metal salt of iminodiacetic acid with phosphorus trichloride until the concentration of iminodiacetic acid hydrochloride is at least 40% by weight, based on the weight of the reaction mixture minus the weight of alkali metal chloride. The process makes possible the preparation of N-phosphonomethyliminodiacetic acid in a simple fashion and in high yield.

Abstract: The present invention relates to an enantioselective cation-exchange material, comprising a chiral selector (1), composed of a chiral component (2) and at least one cation-exchange group (X), a spacer (3) and a carrier (4). The cation-exchange material is characterized in that the chiral component (2) has a molecular weight of less than 1,000 and the at least one cation-exchange group (X) is an acid group having a pKa<4.0.

Abstract: Novel compounds, N,N′-bis(phosphonomethyl)-N,N′-bis(hydroxycarbonylmethyl)urea and N,N,N′,N′-tetrakis(hydroxycarbonylmethyl)urea, suitable for use in preparing N-acyl aminocarboxylic acids that can be readily converted to N-(phosphonomethyl)glycine are provided. The compounds may be formed by the reaction of bis-(phosophonomethyl)urea or urea respectively with carbon monoxide and formaldehyde in the presence of a carboxymethylation catalyst precursor and solvent.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.

Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.

Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.

Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Abstract: Chelating agents (chelants) of the general structure: wherein: n=2-4 X=—CR1R2—, or whereby at least two of X are of formula III Y=COOH, —PO3H2 or o-hydroxyphenyl R1, R2 and R3 are independently H or C1-C8 alkyls m=1, 2 or 3 and most preferably m=1 Z and Z1 are unsubstituted or substituted C C*=C or CH or N Z1, Z2, Z′1, and Z′2 are independently selected from H (or nothing for Z2 and Z′2 if C* is N) and C1-C10 groups that optionally contain one or more N atoms (optionally attached directly to C*), whereby one of the pairs Z/Z1, Z/Z2 and Z1/Z2 and one of the pairs Z′/Z′1, Z′1/Z′2 and Z′/Z′2 may be connected to form substituted or unsubstituted (hetero)(poly)cyclic structures of less than 20 atoms. C* is either part of an aromatic (hetero)(poly)cyclic structure or linked by a double bond to Z or Z2 and/or Z′ or Z′2.

Abstract: This invention is directed to a process for making a salt of a carboxylic acid. The process comprises contacting a catalyst with an alkaline mixture comprising a primary alcohol. In one embodiment, for example, the catalyst comprises a metal support (preferably a metal sponge support) coated with copper. The support comprises at least about 10% (by weight) non-copper metal, and the copper-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises a metal support (preferably a metal sponge support) coated with silver. The support comprises at least about 10% (by weight) non-silver metal, and the silver-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises at least about 15% (by weight) non-copper metal, and at least about 10% (by weight) copper.

Abstract: Novel compounds, N,N′-bis(phosphonomethyl)-N,N′-bis(hydroxycarbonylmethyl)urea and N,N,N′,N′-tetrakis(hydroxycarbonylmethyl)urea, suitable for use in preparing N-acyl aminocarboxylic acids that can be readily converted to N-(phosphonomethyl)glycine are provided. The compounds may be formed by the reaction of bis-(phosophonomethyl)urea or urea respectively with carbon monoxide and formaldehyde in the presence of a carboxymethylation catalyst precursor and solvent.

Abstract: Tripodal chelating agents incorporating imine C.dbd.N bonds are disclosed for the formation of lanthanide and other metal complexes which are relatively stable in the presence of water at neutral pH.

Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

Abstract: Use of 1-amino-3-N,N-dimethylamino)-propyliden-1,1-bisphosphonic acid of the structural formula: ##STR1## or of its monosodium or other pharmaceutically acceptable salt, as a biological carrier for bone active substances or for the preparation of a medicament for the diagnosis, prophylaxis and/or treatment of bone and/or mineral metabolism disorders.

Abstract: A compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2, which may be identical or different, represent hydrogen or halogen, or alkyl, alkoxy, nitro or trihalomethyl,X represents CO, SO.sub.2 or CH.sub.2,A.sub.1 represents any one of the groups as defined in the description,A.sub.2 represents --(CH.sub.2).sub.n or --CH.dbd.CH--,R.sub.3, R.sub.4, which may be identical or different, represent hydrogen or alkyl,its isomers as well as its addition salts with a pharmaceutically acceptable base and medicinal product containing the same are useful as angiogenesis inhibitors.

Abstract: Concentrated aqueous hexamethylene phonic acid solutions are described containing, in addition to high levels e.g. 40%-50% of phosphonic acid a narrowly defined level of non-oxidizing mineral acid, preferrably hydrochloric acid.

Abstract: A process for the purification of aminophosphonic acids under non-alkaline conditions is described. In particular, aminophosphonic acids are slurred in neutral or acidic water, heated to reflux, cooled and then filtered. Product purities approaching 100% are thus obtained.

Abstract: Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.

Abstract: Certain N-bis(phosphonomethyl) amino acids are novel compounds and are useful in preventing calcium carbonate scale.

Abstract: The ampholytes are extracted from the reaction solution with a liquid cation exchanger which is immiscible with the acidic aqueous reaction solution, where the cation exchanger is dissolved in at least one organic solvent which is immiscible with water and forms an organic phase with the organic solvent. Subsequently the organic phase which is loaded with the ampholyte is separated from the reaction solution, and then the ampholytes are back-extracted from the organic phase with aqueous solvents. The product losses in the process are low, and the residual salt content is very low.

Abstract: The present invention is concerned with aniline derivatives of the general formula: ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl or aryl, R.sub.2 is hydrogen or a lower alkyl which can be substituted by hydroxyl, amino carboxyl, lower alkoxycarbonyl, lower alkanoylamide lower alkyl or aryl or by a group of the structure ##STR2## is which R.sub.5 and R.sub.6 have the meanings given hereinafter, R.sub.3 is a hydrogen or halogen atom or a carboxyl group, R.sub.4 and R'.sub.4, which can be the same or different, are hydrogen or halogen, carboxyl or lower alkoxy or lower alkyl radicals which are preferably in the m-position, R.sub.5 is hydrogen or a lower alkyl and R.sub.

Abstract: Process for preparing N-phosphono-methyl-iminodiacetic acid by means of phosphonomethylation of iminodiacetic acid performed by reacting an aqueous solution of phosphoric acid and hydrochloric acid, obtained by hydrolysis of phosphorous trichloride, with iminodiacetic acid and formaldehyde, in which phosphorous trichloride is hydrolysed in step (a) with water or an aqueous solution or hydrochloric acid, the reaction temperature and amount of water are regulated such that an aqueous solution of hydrochloric acid and phosphoric acid in a molar ratio of 0.5:1 to 2:1 is formed, and gaseous hydrochloric acid is caused to develop from the reaction medium. The phosphonomethylation reaction is performed in the solution obtained in step (a) in the presence of iminodiacetic acid in a molar ratio of iminodiacetic acid to phosphoric acid between 1:1 and 1:1.2 with the addition of formaldehyde. The N-phosphono-methyl-iminodiacetic acid is then recovered from the reaction medium.

Abstract: Novel bisphosphonates comprise compounds of the formula (I) ##STR1## wherein m and l are independently 1 or 2; R.sub.1 represents hydrogen, a lower alkyl group, or an alkali metal cation; R.sub.2 represents hydrogen, a lower alkyl group or an alkali metal cation; Y represents .dbd.0 or .dbd.N--OH, or --OH and X represents --(CH.sub.2).sub.n --, a branched alkylene group, or a branched or straight alkenylene or alkynylene chain optionally substituted by one or more oxygen or nitrogen atoms, wherein n is an integer from 3 to 24. Further definitions of X are included in the description.

Abstract: Flameproofed thermoplastic polyester molding material comprising(A) one or more thermoplastic polyesters,(B) a nitrogen-containing diphosphinic acid compound of the formula (I), and(C) with or without an amine,(D) with or without inorganic reinforcing agents, and(E) with or without processing auxiliaries.The nitrogen-containing diphosphinic acid compounds are effective even in relatively low concentrations and thus do not adversely affect the mechanical and electrical properties of the flameproofed polyester molding materials. The latter are used in the production of molded articles.

Abstract: This invention relates to controlling corrosion in aqueous systems and more particularly to using certain calcium insensitive phosphonomethyl amine oxide compounds. The compounds of this invention are water soluble phosphonomethyl amine oxides having at least one oxidized tertiary amine group of the formula: ##STR1## and water soluble salts thereof and having a cloud point of at least about 25 ppm.

Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.

Abstract: The content of hydrogen chloride and phosphorous acid of crude amino organic phosphonic acids, especially diethylenetriaminepentakis (methylene phosphonic acid) is reduced by solvent extraction into an alcoholic phase leaving purified phosphonic acid behind.

Abstract: A method is disclosed for the sulfurization of a phosphorus containing compound, which comprises: solubilizing the phosphorous containing compound and then contacting the phosphorous containing compound, with a sulfur containing compound of the solution formula: ##STR1## wherein, B is selected from the group consisting of --CH.sub.2 --, --C(O)-- or --C(S)--;Q is a non-interfering moiety or radical; andm and n, same or different, are selected from the group consisting of zero or one.

Abstract: Preparation of a semi-crystalline catalyst for curing coating compositions wherein an isocyanate-sulfonate or -phosphonate is made by a Michael addition followed by chain extension with an isocyanate.

Abstract: High purity ethylenediaminetetra(methylenephosphonic acid) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetra(methylenephosphonic acid) are prepared by dissolving the aminomethylenephosphonic acid in an aqueous base, acidifying with a mineral acid at an elevated temperature to precipitate the crystals, maintaining the solution at an elevated temperature for a period of time sufficient to assure crystallization, cooling to a lower temperature and maintaining at that temperature for a time sufficient to precipitate the crystals and filtering the resulting crystals at that temperature, washing the crystals with water and recovering the desired high purity aminophosphonic acid. The ethylenediaminetetra(methylenephosphonic acid) is obtained in a purer state during its synthesis if the crystals are filtered hot without prior cooling.

Abstract: A class of phenyl glycine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phenyl glycine compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.