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 present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Abstract: The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.

Abstract: The invention provides novel phosphoantigen salts and novel crystalline phases of phosphoantigens salts, that the latter including non-solvated polymorphs, and solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, novel phosphoantigen crystalline phases. Methods of using such compositions for the treatment of disease, immunostimulatory or immune response modifying use are also provided. The invention also provides method for obtaining phosphoantigen crystals as well as highly pure phosphoantigen compositions.

Abstract: Novel synthetic oxidized lipids and methods utilizing oxidized lipids for treating and preventing an inflammation associated with an endogenous oxidized lipid are provided.

Abstract: Inhibitors of axillary malodour having the formula wherein R has the same meaning as given in the specification.

Abstract: Disclosed is a method for efficiently and highly selectively producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid, which is useful as a herbicide, through a catalytic asymmetric synthesis reaction. Specifically disclosed is a method for producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid which is characterized in that a dehydroamino acid is subjected to an asymmetric hydrogenation by using a rhodium catalyst represented by the formula (2) below and having an optically active cyclic phosphine ligand, and then the resulting product is subjected to hydrolysis: [Rh(R4)(L)]X ??(2) [where R4 represents 1,5-cyclooctadien or norbornadien; L represents a substance represented by the following formula (6): (wherein R5 and R8 respectively represent a C1-4 alkyl group; R6 and R7 respectively represent hydrogen atom or hydroxyl group; and Y represents a group selected from groups represented by the following formula (7): (where Me represents methyl group)).].

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: 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: The present invention is a phosphorylcholine-containing chemical compound represented by the following formula (1) or (2). (CH3)3N+CH2CH2PO4?CH2COOH ??(1) (CH3)3N+CH2CH2PO4?CH2COONa ??(2) The object of the present invention is to provide a new phosphorylcholine-containing compound that is useful as a surface treatment agent or a source material of a surface treatment agent. Another object is to provide a manufacturing method that has a high industrial utility value.

Abstract: The present invention relates to a process for the preparation of 3-amino-2-hydroxypropylphosphinic acid derivatives of the formula I, which are valuable pharmaceutical active ingredients and can be used, for example, as antidepressants. The process starts from O-ethyl phosphinates of the formula II into which, after silylation with hexamethyldisilazane, the 3-amino-2-hydroxypropyl moiety is introduced by reactions with epichlorohydrin and ammonia.

Abstract: Compounds of formula (I) or (II), wherein R1 is C1–C18alkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, and the radicals R2 to R13 are each independently of the others hydrogen; —NO2; dialkylamino; alkylthio; alkylsulfonyl; halogen; C1–C18alkyl; C1–C18alkoxy; C1–C18alkoxyalkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, are suitable as flame-proofing agents for thermoplastic or thermosetting polymers

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: The invention provides compounds of the formula II: wherein R represents propyl, butyl, pentyl, neo-pentyl or cyclohexyl, and salts thereof. These compounds are selective GABAC receptor antagonists. The invention also provides a method of enhancing the cognitive activity of an animal and a method of stimulating memory capacity in an animal, comprising administering to the animal an effective amount of a compound of formula II or a pharmaceutically acceptable salt thereof.

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

Abstract: In a process for preparing N-phosphonomethylglycine or a salt thereof by bringing phosphonomethyliminodiacetic acid or a salt thereof into contact with at least one oxygen-containing oxidant in the presence of a heterogeneous catalyst, the heterogeneous catalyst comprises at least one silicate.

Abstract: Thioketals and thioethers are provided that inhibit the expression of VCAM-1, and which can be used in the treatment of VCAM-1 mediated diseases including inflammatory disorders, cardiovascular diseases, occular diseases, autoimmune diseases, neurological disorders, and cancer. The compounds also can be used to treat hyperlipidemia and/or hypercholesterolemia.

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: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, 1

Abstract: Are described compounds of Formula (I) in which R, R′, R″, A, and D have the meanings described in the text, as useful agents in the cure of pathologies characterised by altered angiogenesis and as antitumorals.

Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: 1

Abstract: The present invention relates to a process for separating from an aqueous mixture one or more organic substances containing at least one positively charged and/or chargeable nitrogenous group by means of extraction via at least one porous membrane, wherein use is made of an extraction agent which contains at least partially relatively long-chain organic compounds and at least one liquid cation exchanger, and of a membrane that is wettable by either the aqueous mixture or by the extraction agent.

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

Abstract: The present invention relates to therapeutically active novel aminoindanes of formula (I). 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: Compounds of formula (i), wherein m, R, R1, and R3 to R6 are as defined in the specification, m, is 1, 2 or 3 and X is O or a direct bond, and the corresponding unphosporylated compounds have interesting properties, e.g. immunosuppressive properties.

Abstract: Thee present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in creating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: Use of phosphorous organic compounds of general formula (I) wherein B represents either an ether group of the formula (II) or a keto group of the formula (III) or is a 5 or 6 membered cyclic compound, and their use for preparing pharmaceutical compositions for the therapeutic and prophylactic treatment of infections in humans and animals due to viruses, bacteria, fungi, and parasites as well as their use as a fungicide, bactericide and herbicide in plants.

Abstract: Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can be used therapeutically and diagnostically for treatment and detection of tumors.

Abstract: This invention relates to attachment chemistries for binding macromolecules to a substrate surface or to other conjugation targets. More particularly, this invention relates to attachment chemistries involving branched or linear structures having one or more hydrazide attachment moieties for binding the macromolecules to a substrate surface, or for other conjugation reactions. Novel modifying reagents are provided for the introduction of protected hydrazide attachment moieties or precursor forms of such hydrazides to the macromolecule, either as a single hydrazide or as multiple hydrazides.

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

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 method is provided for making aromatic-imide and aromatic-methylidynetrissulfonyl species by reaction of aromatic species with a reactant according to formula (I): (X—SO2—)m—QH—(—SO2—R1)n  (I) wherein Q is C or N; wherein each X is independently selected from the group consisting of halogens, typically F or Cl; wherein each R1 is independently selected from the group consisting of aliphatic and aromatic groups, which may or may not be saturated, unsaturated, straight-chain, branched, cyclic, heteroatomic, polymeric, halogenated, fluorinated or substituted; wherein m is greater than 0; wherein m+n=2 when Q is N; and wherein m+n=3 when Q is C. Ar may be derived from an aromatic polymeric compound.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: the present invention provides novel compounds represented by formula I: 1

Abstract: Novel amines of formulas 1A and 1B 1

Abstract: Novel compounds of formula I, with the exception of

Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.

Abstract: Phospholipid-analogous compounds of the general formula (I) 1

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: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.

Abstract: The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

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

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: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.

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: The invention provides a compound of formula (I): 1

Abstract: Use of phosphorous organic compounds of general formula (I) 1

Abstract: Improved mud additive compositions are provided which are especially formulated to control hole enlargement due to salt bed erosion during drilling, and to assist in solubilization of deposited salt during well operations. The compositions include a first ingredient such as sodium or potassium ferrocyanide and mixtures thereof, and a second ingredient such as the a phosphonic acid, alkali or alkaline earth metal phosphonic acid salts, or mixtures thereof. The first ingredient is generally present at a level of from about 50-95% by weight in the particulate, dilutable form of the invention, whereas the second ingredient is present at a level of from about 5-50% by weight. The compositions hereof may be added to drilling mud during drilling operations or to fresh water for removing salt depositions.