Abstract: This invention relates to overcharge protection and molecular redox shuttles in rechargeable lithium-ion cells. For this, specific nitroxyls or oxoammonium salts are used in the electrolyte. This invention also relates to a method of producing such lithium-ion cells and to a method of recharging such lithium-ion cells. This invention also pertains to some nitroxyls compounds and oxoammonium salts.

Abstract: Processes for making zoledronic acid can be advantageously carried out in a solvent/diluent that comprises a mixture of (i) a polyalkylene glycol and (ii) a cyclic carbonate of the formula (3) wherein n is an integer from 2 to 4, and R1 and R2 each independently represent a hydrogen or a C1-C4 alkyl group.

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 invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.

Abstract: The invention relates to compounds of the formula I A-B-Z ??I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.

Abstract: The invention relates to new crystalline forms of low water soluble salts of zoledronic acid, the process for preparation of these crystalline forms, compositions containing these crystalline forms, and the use of these crystalline forms in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the crystalline form of the free acid monohydrate of zoledronic acid, the process for preparation of the crystalline form of the free acid monohydrate of zoledronic acid, compositions containing the crystalline form of the free acid monohydrate of zoledronic acid, and the use of crystalline form of the free acid monohydrate of zoledronic acid in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.

Abstract: A V?9V?2 T cell proliferation agent includes at least a bisphosphonate, interleukin 2, and interleukin 18. Since 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.

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: Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds of Formula (I) wherein: Z is a porphyrinic macrocyclic, Alk1 and Alk2 are each independently an alkylidene chain; L is a linking group or is absent; R1 is preferably an ionic group or polar group; R2 is an ionic group, polar group, bioconjugatable group, or targeting group: R3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk1 and Alk2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.

Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.

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: 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: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.

Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.

Abstract: This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R?, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.

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 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: The present invention relates to processes and reagents for oligonucleotide synthesis and purification. One aspect of the present invention relates to compounds useful for activating phosphoramidites in oligonucleotide synthesis. Another aspect of the present invention relates to a method of preparing oligonucleotides via the phosphoramidite method using an activator of the invention. Another aspect of the present invention relates to sulfur-transfer agents. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to a method of preparing a phosphorothioate by treating a phosphite with a sulfur-transfer reagent of the invention. In a preferred embodiment, the sulfur-transfer agent is a 3-amino-1,2,4-dithiazolidine-5-one. Another aspect of the present invention relates to compounds that scavenge acrylonitrile produced during the deprotection of phosphate groups bearing ethylnitrile protecting groups.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Diazonamide A analogs, and the salts, esters and conjugates thereof, having improved aqueous solubility are provided. Also provided are pharmaceutical compositions, and methods for preparing and using such compounds and compositions for the treatment of proliferative diseases.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

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: 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 invention concerns 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 ultra-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. Said compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.

Abstract: The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect.

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

Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas IV, IV?, I?, II?, or IVa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.

Abstract: The present invention relates to prodrugs and compositions thereof useful for treating or preventing Hepatitis C virus (HCV) infections. In particular, the present invention relates to prodrugs of substituted diphenyl-, diheteroaryl- and mixed phenyl heteroaryl substituted five-membered heterocycle compounds, compositions comprising the compounds and the use of such compounds and compositions to inhibit HCV replication and/or proliferation as a therapeutic approach towards the treatment and/or prevention of HCV infections in humans and animals.

Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.

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: Ac-Phe-Tyr-phosphoSer-?[CH?C]-Pro-Arg-NH2AND Fmoc-bis(pivaloylmethoxy)phosphoSer-?[CH?C]-Pro-2-aminoethyl-(3-indole); and their Phospho-(D)-serine stereoisomers are novel compounds. ? refers to a pseudo amide. Such novel compounds advantageously may be used as alkene mimics.

Abstract: The present invention relates to inositol phosphate derivatives, in which the inositol phosphate is substituted with one or two reactive groups G or one or two conjugated substances or molecules M, said reactive group(s) G or said substance(s) or molecule(s) M being linked to IP1 via a linkage group L, M being chosen from the following group: a tracer, an immunogen, a member of a binding partner pair, a solid support. Application: tools allowing the study of the inositol phosphate cycle and therefore, indirectly, the study of seven transmembrane domain receptors coupled to phospholipase C, receptors having a tyrosine kinase activity, and in general enzymes involved in the variations of the intracellular concentration of IP1.

Abstract: Zoledronic acid trihydrate, processes for its preparation, and conversion into zoledronic acid monohydrate.

Abstract: The invention relates to polymorphs of zoledronic acid and zoledronate sodium salts, amorphous zoledronate sodium salt, processes for making the polymorphs and amorphous zoledronate sodium salt, and pharmaceutical compositions containing the polymorphs and amorphous zoledronate sodium salt.

Abstract: The invention is related to phosphorus substituted IMPDH inhibitory compounds, 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: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.

Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.

Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.

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: The present invention relates to ligands of the general formula (I). In addition, a process for the production thereof and the use thereof are demonstrated.

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: The present invention relates to novel metathesis catalysts with an imidazolidine-based ligand and to methods for making and using the same.

Abstract: This invention relates to a process for controlling the hydrate mix of a compound, or a composition comprising the compound, the compound being capable of forming a plurality of hydration forms of differing stability and also of dissolution to give a solution that, when frozen below the eutectic point, is a eutectic mixture. This invention further relates to disodium salt of fosfluconazole in the form of its trihydrate, its hexahydrate, or as a mixture of tri- and hexahydrates.

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

Abstract: Novel phosphonium salts of benzotraizoles, which are highly reactive coupling agents, and are particularly useful in peptide synthesis, are disclosed. Further disclosed is a process of preparing the novel phosphonium salts and methods utilizing same for preparing peptides.

Abstract: The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.

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: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.