Abstract: The subject invention is directed to tetradentate bis-(NHC carbenes) alkylene ligand Pt(II) complexes, tetradentate bis-(NHC carbenes) alkylene ligands, and its ligand precursors, for preparation of the Pt(II) complexes. The Pt(II) complexes show a deep blue emission with an improved quantum efficiency and can be used for fabrication of OLEDs with an electroluminescence layer that comprise the bis-(NHC carbenes) alkylene ligand Pt(II) complexes.

Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers arranged between the anode and the cathode; wherein at least one of the one or more layers is a light emitting layer and wherein the one or more layers, comprises an organic compound represented by a substituted 2,2?-biimidazole.

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: The present invention provides for methods and compositions for treating and/or preventing cardiac dysfunction by administering to subject a therapeutically effective amount of a bisphosphonate, functional analogue or a pharmaceutically effective salt thereof.

Abstract: The present invention relates to imidazolo-containing phosphinoborane compounds, to optically active ligands prepared using them, to transition metal complexes which comprise such ligands, and to catalysts which comprise such transition metal complexes. The present invention further relates to the particular processes for preparing the phosphinoborane compounds, the optically active ligands, the transition metal complexes and the catalysts, and to the use of the catalysts for organic transformation reactions. The present invention further relates to a process for preparing optically active ligands comprising imidazolo-containing phosphorus compounds using imidazolo-containing phosphinoborane compounds.

Abstract: 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.

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 novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.

Abstract: A process for the preparation of [1-hydroxy-2-(1H-imidazol-1-yl)-ethylidene]bisphosphonic acid consists of the reaction of aqueous solution of 1H-imidazole-1-acetic acid hydrochloride with phosphorus trichloride followed by removal of the excess of phosphorus trichloride, addition of water and hydrolysis of the reaction products. In order to isolate the product the post-reaction mixture is filtered and the anti-solvent is added to the aqueous filtrate in order to crystallize out [1-hydroxy-2-(1H-imidazol-1-yl)-ethylidene]bisphosphonic acid monohydrate.

Abstract: A process for the preparation of a polymer nanoparticle by a photoinduced emulsion polymerization includes preparing an emulsion comprising at least one surfactant, a dispersed phase and a continuous phase. The dispersed phase comprises at least one polymerizable monomer and the continuous phase comprises water and at least one photoinitiator. The at least one polymerizable monomer is polymerized by exposing the emulsion to an electromagnetic radiation having a wavelength so as to induce a generation of radicals from the at least one photoinitiator.

Abstract: Novel chemical compounds of the general formula K+A? useful as industrial solvents, especially as ligands, for efficient catalyst recycling.

Abstract: The present invention provides novel phospholipid derivatives. Furthermore, the present invention provides lipid membrane structures excellent in gene/nucleic acid introduction efficiency into a cell.

Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.

Abstract: The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.

Abstract: This invention relates to biomaterials, said biomaterials for use in methods to control and/or induce bone growth. Particularly, the invention relates to macroporous calcium phosphate biomaterials pre-loaded with certain amounts of osteoclastic activity inhibitors for use in methods to control and/or induce bone growth in primates.

Abstract: A compound having a formula II(a): wherein R1 and R2 are hydrogen lower alkyl, lower aliphatic acyl, or lower alkoxycarbonyl; R4 is C1-C4 alkyl; n is 2 or 3; X is a formula ?N-D, wherein D is hydrogen, C1-C6 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2—, —CH(OH)—CH2— or phenylene; Z is C1-C6 alkylene; R5 is C3-C10 cycloalkyl or C6-C10 aryl; R6 and R7 are hydrogen, lower alkyl, halogeno lower alkyl, lower alkoxy or lower alkylthio; and R10 and R11 are hydrogen or lower alkyl.

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: A phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified phosphocalcic compound is obtained by adding a gem-bisphosphonic acid or one of its alkali metal or alkaline earth salts to a suspension of a precursor phosphocalcic compound in ultras-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. The compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.

Abstract: (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula I, wherein one of R1 and R2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.

Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.

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: C2-C5-Alkyl-substituted [imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.

Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

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 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: C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.

Abstract: Provided are a nanoparticle/dispersant complex having excellent dispersibility and long-term stability in a dispersion medium, a production method therefor, and a nanoparticle dispersion liquid and a nanoparticle/matrix-material complex which are colorless and transparent even at high concentrations. In the nanoparticle/dispersant complex, a nanoparticle is covered with a dispersant containing a heterocyclic cationic group and one of an oxo acid group containing a sulfur atom or a phosphorus atom and an anion moiety of the oxo acid group; in the nanoparticle dispersion liquid, the nanoparticle/dispersant complex is dispersed into a dispersion medium; in the nanoparticle/matrix-material complex, the nanoparticle/dispersant complex is dispersed into a matrix material; and the production method for a nanoparticle/dispersant complex comprises forming, under a presence of the dispersant, a nanoparticle covered with the dispersant from a nanoparticle precursor.

Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.

Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n—Z—(CH2)mPO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, —(CH2)n—Z—(CH2)m—OPO(OR7)R9, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.

Abstract: The invention relates to a method for the manufacture of substituted phosphanes and substituted phosphanes manufactured according to the method. Phosphanes, phosphane oxides, sulfides or selenides are used as ligands in coordination compounds. They play a central role in controlling the activity and selectivity of catalysts. The object is achieved by the invention by synthesizing heterocyclic substituents on aromatic groups by introducing acetyl groups. In this manner, previously unknown representatives of the families of phosphanes, phosphane oxides, sulfides and selenides are made accessible.

Abstract: 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.

Abstract: The present invention relates to depot formulations comprising a poorly water soluble salt of a bisphosphonate forming together with one or more biocompatible polymers, to poorly water-soluble salts of such bisphosphonates, to crystalline forms of the free compounds and the salts and to other related aspects, where the compounds are of the Formula (I), where R1 and R2 are as described in the specification. Compounds of the Formula (I) and their forms mentioned in the disclosure are useful for the treatment of bone-related disorders and cancer.

Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

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: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: The present invention relates to phosphorus compounds containing imidazole groups, to optically active ligands prepared using them, to transition metal complexes which comprise such ligands, and to catalysts which comprise such transition metal complexes. The present invention further relates to the particular processes for preparing the phosphorus compounds, the optically active ligands, the transition metal complexes and the catalysts, and also to the use of the catalysts for organic transformation reactions.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: There are provided compositions comprising a first compound selected from the group consisting of compounds of formulas (Ib), (III), (V), and (VII), and a second compound selected from the group consisting of compounds of formulas (IIb), (IV), (VI), and (VIII): Various chemical entities can be used for R4 to R11. These compositions can be particularly useful as anti-static agents or as electron activable precursors to a redox couple.

Abstract: A novel process of preparing tridentate ligands containing one or more of a diarylphosphine and/or dialkylphosphine electron donating groups are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing and dialkylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed. Novel precursor molecules useful for preparing the tridentate ligands and processes of preparing same are also disclosed.

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: The invention relates to a process for modifying an inorganic substrate, directed toward giving it antimicrobial properties, said process consisting in grafting in one or more steps onto a surface of said substrate groups with intrinsic antimicrobial properties or groups capable of releasing species with antimicrobial properties. The grafting is performed by means of an organophosphorus coupling agent. A subject of the invention is similarly a substrate obtained by this process, as well as diverse uses of such a substrate.

Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.

Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Abstract: The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1?n?20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.

Abstract: A new crystalline form of the Zoledronic acid, characterized by its X-rays diffractogram as well as by its spatial atomic distribution in the red crystalline and its curves of thermal analysis. There is also included a method to obtain this crystalline form, which includes the synthesis of the corresponding acid and the pharmaceutical composition this crystalline form comprises.

Abstract: A V?9V?2 T cell proliferation agent includes at least a bisphosphonate, interleukin 2, and interleukin 18. Since IL-18 has properties that improve cell viability by inhibiting cell death, IL-18 is presumably capable of acting as a cofactor for the bisphosphonate so as to significantly increase the effect of V?9V?2 T cell proliferation by the bisphosphonate and the IL-2. This allows providing a V?9V?2 T cell proliferation agent capable of growing V?9V?2 T cells with a proliferated efficiency significantly high compared to conventional methods so that the proliferated V?9V?2 T cells have a high antitumor activity and high cytokine productivity.