Abstract: The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use.

Abstract: Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: This invention relates generally to polyisoprenyl phosphonate derivatives pharmaceutical compositions comprising polyisoprenyl phosphonate derivatives, and uses thereof.

Abstract: The present invention generally relates to methods of modulating Cav1.2 channels and Cav1.2 channel activators.

Abstract: The invention relates to a compound described by a general formula (1), wherein each X independently can be OPO32?, OPSO22? or OSO3?; R1 comprises a solubility function such as a polyethylene glycol moiety and each X independently can be OPO32?, OPSO22?, ? or OSO3?; and Z is an alkyl chain comprising 1 to 3 carbon and/or hetero atoms. The invention further relates to polysulfate derivatives or mixed polyphosphate/sulphate derivatives of six-membered cyclic polyols for use in the therapy of infection by Clostridium difficile.

Abstract: Disclosed are oligomeric phosphonates including oligophosphonates, random or block co-oligo(phosphonate ester)s and co-oligo(phosphonate carbonate)s produced using a condensation process terminated with hydroxyl, epoxy, vinyl, vinyl ester, isopropenyl, isocyanate groups, and the like. These materials can be used as a reactive additive to other polymers, oligomers or monomer mixtures to impart flame resistance without diminishing melt processability which is important in the fabrication of polymers for many applications.

Abstract: Embodiments of the invention include a phosphorus containing flame retardant which may be the reaction product of a reaction mixture where the reaction mixture includes at least one active hydrogen-containing compound and at least one phosphorus containing compound. The at least one active hydrogen-containing compound is selected from the group of a first polyol having a hydroxyl functionality of at least 3, a polyamine having an amine functionality of at least 2, and an amino alcohol having a combined amine and hydroxyl functionality of at least 2.

Abstract: Disclosed are oligomeric phosphonates including oligophosphonates, random or block co-oligo(phosphonate ester)s and co-oligo(phosphonate carbonate)s produced using a condensation process terminated with hydroxyl, epoxy, vinyl, vinyl ester, isopropenyl, isocyanate groups, and the like. These materials can be used as a reactive additive to other polymers, oligomers or monomer mixtures to impart flame resistance without diminishing melt processability which is important in the fabrication of polymers for many applications.

Abstract: The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.

Abstract: Provided herein are analog and derivative compounds of inositol hexakisphosphate effective to treat a Clostridium difficile infection and to neutralize the bacterial toxins produced by the same. In addition, methods of treating the C. difficile infection and for neutralizing its toxins with the compounds are provided.

Abstract: Mixtures of three types of linear, branched or cyclic phosphates are useful flame retardants, especially for thermoplastic resins or as functional additives in polymer matrices.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: The present invention relates to a method of producing a polymerizable phosphate containing at least one selected from polymerizable phosphates represented by formula (II), (III) or (IV) by a batch reaction, including a step of adding a compound represented by formula (I) into a mixture of a polymerizable phosphate reaction product containing at least one selected from polymerizable phosphates represented by formula (II), (III) or (IV), obtained by a pre-batch reaction, and phosphoric acid anhydride to react them: wherein R1 represents H or a C1-4 alkyl group, R2 represents a C2-6 alkylene group and n denotes an integer from 1 to 3.

Abstract: An object of the present invention is to provide an antibacterial medical equipment which has sufficient antibacterial activity in vivo and is excellent in compatibility with living tissues, and also can maintain antibacterial activity over a long period and has high safety. An antibacterial medical equipment characterized in that inositol phosphate is bonded to a Ca compound of a medical equipment whose surface is at least coated with a layer of the Ca compound, or a medical equipment comprising the Ca compound. The antibacterial medical equipment as described above, wherein silver ions are bonded to the inositol phosphate. A method for producing an antibacterial medical equipment, which comprises bringing a medical equipment whose surface is at least coated with a layer of a Ca compound, or a medical equipment comprising a Ca compound into contact with an aqueous solution of inositol phosphate to obtain an antibacterial medical equipment in which inositol phosphate is bonded to the Ca compound.

Abstract: The present invention relates to timber materials rendered flame-retardant by using halogen-free organophosphorus compounds, to means and processes for producing these materials, and also to their use.

Abstract: A fluorinated dicarbonyl fluoride FOCCF(CF3)[OCF2CF(CF3)]lOCF2CF2O[CF(CF3)CF2O]mCF(CF3)COF (l+m is 30-130) is reacted with an aromatic amine XC6H4NHR1 (R1 is H, alkyl, or phenyl and X is I or Br) to obtain a fluorinated polyether compound of the following formula. The compound obtained is mixed with an aromatic boric ester, an organopalladium compound, and a basic inorganic or organic compound (and organophosphorus compound) to form a curable fluorinated polyether composition. This curable fluorinated polyether composition has satisfactory processability including moderate flowability at room temperature. It is applicable to various molding techniques including injection molding and RIM.

Abstract: A composition and method for the treatment of Alzheimer's disease and related amyloid plaque development and reduction of amyloid plaque, amyloidosis and amyotrophic lateral sclerosis, as well as neuro-degenerative diseases and protein aggregation diseases, includes an effective amount of a compound selected from the group consisting of phytic acid (inositol hexakisphosphate), a phytate salt, an isomer or hydrolysate of phytic acid or a phytate salt, or a mixture of any combination thereof, being administered to a person in an amount from about 0.5 grams to about 18.75 grams per day, with or without a dephosphorylating enzyme.

Abstract: There is disclosed a salt of a sulfur-containing, phosphorus-containing compound. There is also disclosed a method of making the salt.

Abstract: Fuel additives, fuel formulations, and processes for their preparation and use are provided. The additives improve the combustion properties of hydrocarbon fuels. The enhanced combustion indicates reductions in certain emissions.

Abstract: A fluorine-containing polyether phosphonic acid ester compound represented by the following general formula: (R2O)(R1O)P(O)(CH2)aCF(CF3)[OCF2CF(CF3)]bO(CF2)CO[CF(CF3)CF2O]dCF(CF3)(CH2)eP(O)(OR3)(OR4) (where R1, R2, R3 and R4 are hydrogen atoms, alkyl groups, cycloalkyl groups, aryl groups, alkylaryl groups, aralkyl groups, or any of the foregoing groups substituted with halogen atoms, and subscripts a, b, c, d, and e are in conditions of 2?a+e?8, b+d?28, and 1?c?10, and subscripts b and d may be 0). The fluorine-containing polyether phosphonic acid ester compound is produced by reaction of a fluorine-containing polyether dialkyl halide represented by the following general formula: X(CH2)aCF(CF3)[OCF2CF(CF3)]bO(CF2)cO[CF(CF3)CF2O]dCF(CF3)(CH2)eX (X: Cl, Br or I) with a phosphite compound represented by the following general formula: (R1O)(R2O)P(OR) and/or (R3O)(R4O)P(OR) (R: a hydrogen atom or a lower alkyl group).

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: There is disclosed a salt of a sulfur-containing, phosphorus-containing compound. There is also disclosed a method of making the salt.

Abstract: A fluorine-containing polyether phosphonic acid ester compound represented by the following general formula: (R2O)(R1O)P(O)(CH2)aCF(CF3)[OCF2CF(CF3)]bO(CF2)CO[CF(CF3)CF2O]dCF(CF3)(CH2)eP(O)(OR3)(OR4) (where R1, R2, R3 and R4 are hydrogen atoms, alkyl groups, cycloalkyl groups, aryl groups, alkylaryl groups, aralkyl groups, or any of the foregoing groups substituted with halogen atoms, and subscripts a, b, c, d, and e are in conditions of 2?a+e?8, b+d?28, and 1?c?10, and subscripts b and d may be 0). The fluorine-containing polyether phosphonic acid ester compound is produced by reaction of a fluorine-containing polyether dialkyl halide represented by the following general formula: X(CH2)aCF(CF3)[OCF2CF(CF3)]bO(CF2)cO[CF(CF3)CF2O]dCF(CF3)(CH2)eX (X: Cl, Br or I) with a phosphite compound represented by the following general formula: (R1O)(R2O)P(OR) and/or (R3O)(R4O)P(OR) (R: a hydrogen atom or a lower alkyl group).

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: The compounds of formula (I) are hydrophilic aryl phosphate, thiophosphate, and aminophosphate intestinal apical membrane Na-mediated phosphate co-transportation inhibitors. The compounds can be administered orally, where they act to inhibit Na-dependent phosphate uptake in the intestines, or internally, where they interact with the phosphate control functions of the kidneys and parathyroid. They are therefore useful for inhibiting sodium-mediated phosphate uptake, reducing serum PTH, calcium, calcitriol, and phosphate, and treating renal disease in an animal, including a human.

Abstract: An interleukin-6 production inhibitor is provided containing a methanebisphosphonic acid derivative as an active component, which has inhibitory effects on interleukin-6 production and is useful in prevention and treatment of diseases due to abnormal production of the interleukin-6. This pharmaceutical is anticipated to have effects in prevention and treatment of diseases related to the interleukin-6, for example, thrombocytosis, inflammatory diseases, abnormal immune response diseases, osteoporosis, rheumatoid arthritis, hypercalcemia, multiple myeloma, cachexia, and nephritis.

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: This invention provides analogues of phosphatidylinositol-phosphates modified at one or more selected inositol-hydroxyls and optionally carrying reporter or anchoring groups attached in the lipid or the inositol residues, and, the synthetic intermediates and methods for the preparation of these analogues. The analogues are useful as research reagents in biomedical studies related to structure, function and therapeuticals, including reference materials for analyzing the metabolic products in safety and efficacy studies of 2- and/or 3-hydroxyl modified inositols and phosphatidylinositols as drug candidates.

Abstract: The present invention provides novel compounds comprising cellular phosphoinositides and analogues tagged with stable or radioactive isotopes. The present invention also provides novel methods for the preparation of the said phosphoinositides by syntheses, and novel key intermediates of synthesis; the novel methods of synthesis are applied also for the preparation of the phosphoinositides in non-labelled form. In addition, the present invention discloses a class of novel compounds as isotope labelled key precursors of labelled phosphoinositides. These precursors are derivatives of the target phosphoinositides, labelled with stable or radioactive isotopes, wherein OH and phosphate groups are blocked with temporary protecting groups.

Abstract: The compounds of formula (I) are hydrophilic aryl phosphate, thiophosphate, and aminophosphate intestinal apical membrane Na-mediated phosphate co-transportation inhibitors. The compounds can be administered orally, where they act to inhibit Na-dependent phosphate uptake in the intestines, or internally, where they interact with the phosphate control functions of the kidneys and parathyroid. They are therefore useful for inhibiting sodium-mediated phosphate uptake, reducing serum PTH, calcium, calcitriol, and phosphate, and treating renal disease in an animal, including a human.

Abstract: Hydrolysis-stable and polymerizable acrylophosphonic acid with the general formula (I) 1

Abstract: A method for the preparation of a fluorinated Phosphonate having the formula (RO)2PO CFR′R″ comprises treating a phosphonate of the formula (RO)2PO CHR′R″, or a metal salt thereof, with fluorine. R is an alkyl group R′ is hydrogen or alkyl and R″ is hydrogen, alkyl or another group.

Abstract: This invention provides analogues of phosphatidylinositol-phosphates modified at one or more selected inositol-hydroxyls and optionally carrying reporter or anchoring groups attached in the lipid or the inositol residues, and, the synthetic intermediates and methods for the preparation of these analogues. The analogues are useful as research reagents in biomedical studies related to structure, function and therapeuticals, including reference materials for analyzing the metabolic products in safety and efficacy studies of 2- and/or 3-hydroxyl modified inositols and phosphatidylinositols as drug candidates.

Abstract: A phosphonic acid ester compound of the formula: R1C(SR3)═CHP(═O)(OR2)2 or [P(═O)(OR2)2]CH═C(SR3)—R4—C(SR3)═CH[P(═O)(OR2)2] wherein R1 represents a monovalent group selected from hydrogen, alkyl, cycloalkyl, cycloalkenyl, aryl, aralkyl, alkenyl and silyl, R2 and R3 each represent aryl and R4 represents alkylene or cycloalkylene. The ester compound is produced by reaction of an acetylene compound, R1C≡CH or HC≡C—R4—C≡CH, with with a phosphorothioate, (R2O)2P(═O)SR3, in the presence of a palladium complex catalyst.

Abstract: The present invention provides crosslinking, conjugating and reducing agents which are functional with at least one phosphorothioate monoester group (--SPO.sub.3.sup.--2). Crosslinking and conjugation methods as well as solid phase reagents and conjugates which are useful in immunoassays are also provided.Crosslinking and conjugating agents of the invention generally comprise a compound corresponding to the formula (I), shown below, wherein n at least 1 and Q is a straight or branched monomer, polymer or oligomer having an average molecular weight between about 200 and about 1,000,000. Additionally, when n is 1, Q comprises at least 1 additional reactive functionality.Q--(S--PO.sub.3.sup.-2).sub.n (I)The reducing agents that are provided conform to a compound of the formula (Y), shown below, wherein (A) and (Z) can be independently selected from C.sub.1 -C.sub.5 alkyl and CONH(CH.sub.2).sub.p wherein p is an integer between 1 and 5.

Abstract: A unique method for the synthesis of substantially pure .alpha.-keto bisphosphonate esters and the usage of these esters in reactions with C, N, O, or P nucleophiles for synthesis of .alpha.-functionalized bisphosphonates. The method starts with a reaction mixture formed of an .alpha.-diazo methanediphosphonate ester, including tert-butylchlorite, a polar aprotic organic solvent, and an effective amount of water. After synthesis is complete, a water trapping reagent may be added to remove any excess water. The present invention provides a versatile pathway to new .alpha.-substituted bisphosphonate derivatives and could be readily adapted to combinatorial drug discovery synthetic strategies. The .alpha.-keto bisphosphonate esters can be converted to the corresponding acids by acid hydrolysis or mild silyldealkylation.

Abstract: A novel class of anionic surfactants with improved surfact active properties is comprised of two hydrophilic and two hydrophobic groups represented by the formula: ##STR1## The surfactants exhibit unusually low critical micelle concentration (cmc) and pC-20 values in aqueous media.

Abstract: A process for the preparation of a compound of formula I, ##STR1## wherein R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, R.sup.3 is hydroxy and R.sup.4 and R.sup.5 are independently C.sub.1-6 alkyl is disclosed. The process comprises reacting a compound of formula II, ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in formula I and X is a leaving group, with a compound of formula III, ##STR3## wherein R.sup.4 and R.sup.5 are independently C.sub.1-6 alkyl, in the presence of a base.

Abstract: A phosphorus ester oligomer having the structure: wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, substituted or unsubstituted alkylamino, substituted or unsubstituted arylamino and aminoalkyl; B.sub.1 and B.sub.2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labeling group, a protecting group, a phosphoramidate or a phosphomonoester; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.

Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.

Abstract: A process for production of l-alkylthiomethanediphosphonic acid compound or 1-arylthiomethanediphosphonic acid compound characterized by removing a thiolate byproduct as an insoluble salt, in the condensation represented by the following formula: ##STR1## wherein R'.sub.1 represents a linear or branched alkyl group having 1 to 6 carbon atoms, R.sub.2 represents an alkyl or aryl group, R.sub.1 represents a pharmaceutically allowable cation, hydrogen atom, or linear or branched alkyl group having 1 to 6 carbon atoms. The present invention significantly improves the yield compared with conventional methods, and simplifies the purification process at the same time, thus is extremely useful in an economical and industrial points of view.

Abstract: A composition that comprises a phosphatized alicyclic compound represented by the formulas (I), (II), (III), (VII) and (IX) as shown in the specification is described.

Abstract: Provided herein are novel syntheses of the phosphate-based inositol derivatives 1-O-?(+)-menthoxycarbonyl!-6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inos itol (D4P), D-myo-inositol 1,4,5-trisphosphate (D-IP.sub.3), 6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inositol H-phosphonate ((-)-3-HP) and L-myo-inositol 1,4,5-trisphosphate (L-IP.sub.3). These syntheses employ fewer column chromatography steps for the isolation of intermediates than do prior art syntheses, and hence, are more convenient, economical and efficient than are the previously known synthetic methods.

Abstract: The present invention relates to a methanediphosphonate derivative, its manufacturing process, and pharmaceutical applications, that is represented with the following formula: ##STR1## wherein, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2, or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to carbon atoms or pharmaceutically allowable cations. .function.The compounds of the present invention have excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and are useful as antiinflammatory agents, antirheumatic agents, bone metabolic disease drugs, autoimmune disease drugs, or osteoporosis drugs.

Abstract: A methane diphosphonic acid derivative represented by the general formula (I): ##STR1## wherein, X and Y are defined in the specification; m represents an integer of 0 to 3; n represents an integer of 0 to 4; and each X of the (X).sub.m and each Y of the (Y).sub.n may be either identical or different; . . . represents a double bond or single bond; A is --(CH.sub.2)a--(D)b--(CH.sub.2)c-- (wherein D is sulfur, oxygen, NH, alkyl-substituted N, or CH.sub.2, a and c are integers of 0 to 10 and b is 0 or 1), or --(CH.dbd.CH)d.dbd.CH= (wherein d is an integer of 0 to 2, and B does not exist when A represents --CH.dbd.CH)d--CH.dbd.), B refers to a hydrogen atom, alkyl group, amino group, monoalkylamino group, dialkylamino group, acylamino group, hydroxyl group, alkoxy group, trialkylsiloxy group or acyloxy group, and each of R.sup.1, R.sup.2, R.sup.3 and R.sup.

Abstract: Novel flame retardant compounds for polymers are disclosed that include 1,4-cyclohexanedimethanol bis(diphenyl phosphate)s. These can be synthesized by reacting 1,4-cyclohexanedimethanol and a diphenyl halophosphate, such as diphenyl chlorophosphate, in the presence of a catalyst, such as magnesium chloride, in an appropriate solvent, such as hexane.

Abstract: The present invention relates to a methanediphosphonate derivative, its manufacturing process and pharmaceutical applications, that is represented with the following formula: ##STR1## (wherein, B is either hydrogen, an alkyl group, hydroxyl group, alkoxy group or amino group, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2 or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to 7 carbon atoms or pharmaceutically allowable cations). The compound of the present invention has excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and is useful as an antiinflammatory agent, antirheumatic, bone metabolic disease drug, autoimmune disease drug, osteoporosis drug and so forth.

Abstract: Disclosed is a composition which comprises a phosphatized alicyclic compound represented by the formula (I), (II), (III), (VII) or (IX) shown in the specification.The composition of the present invention is useful as an antigassing agent for a water-based coating composition containing metallic, for example, aluminum powder, or flake pigments for coating automobile bodies, etc., a flame retardant for various resins, and a water-based ink, and the like.

Abstract: PIA.sub.2 inhibitors selected from the group consisting of ##STR1## wherein A is selected from the group consisting of ##STR2## and Z, W, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, X, X' and Y are as defined herein.